Studies by year 2230
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2026 46
- CETP variants rs2033254 and rs12708980 associate with lower intestinal cholesterol absorption markers in a European GWAS (Nutrients 2026)
- Review highlights CETP inhibition improving survival in a mouse model of sepsis (Curr Opin Lipidol 2026)
- Dalcetrapib reduces red blood cell sickling in sickle cell disease and boosts the effect of voxelotor when combined (Clin Hemorheol Microcirc 2026)
- Reducing CETP activity with evacetrapib preserves memory in an Alzheimer's mouse model, independent of amyloid or tau markers (EMBO Mol Med 2026)
- CETP is over-expressed in non-small cell lung cancer and obicetrapib restores ferroptosis sensitivity in xenografts and organoids (Clin Transl Med 2026)
- Mendelian randomisation suggests genetically proxied CETP inhibition may lower intracranial aneurysm risk (Neurosurg Rev 2026)
- A turmeric compound, calebin A, binds CETP nearly as tightly as torcetrapib in a computational drug-discovery screen (Res Pharm Sci 2026)
- Hepatic overexpression of the hepatokine Tsukushi impairs HDL-mediated reverse cholesterol transport in hamsters without changing CETP activity (J Lipid Res 2026)
- Obicetrapib lowers Lp(a) by 37% in a 2,356-patient pooled analysis, with similar absolute reduction across baseline strata (Eur Heart J 2026)
- A meta-analysis of 62,565 patients confirms CETP inhibitors raise HDL cholesterol by 130 percent yet still fail to reduce cardiovascular events (J Cardiovasc Pharmacol 2026)
- Liver-targeted CETP expression improves glucose tolerance in female mice but worsens it and drives fatty liver in males (bioRxiv 2026)
- Meta-analysis of 3,512 patients: obicetrapib added to ezetimibe nearly doubles LDL-C lowering seen with obicetrapib alone, but adds nothing to statins (Cardiol Rev 2026)
- Meta-analysis of three RCTs in 3,286 patients confirms obicetrapib effects on LDL-C, apoB and HDL-C with no excess adverse events (Ann Med Surg 2026)
- Taiwan Biobank GWAS of 40,773 people finds a three-way APOA5-LPL-CETP gene interaction behind metabolic syndrome susceptibility (Genome Biol 2026)
- A review positions CETP alongside PCSK9 and ANGPTL3 as emerging lipid-regulatory targets in cancer, though CETP-specific oncology research remains scarce (Biomolecules 2026)
- CETP inhibitors reframed: from raising HDL to lowering atherogenic lipoproteins and improving glycaemic control, with obicetrapib the current lead (Circ Res 2026)
- CETP shows the most consistent gene-diet interaction evidence of any lipid gene, especially with dietary fat composition (Curr Issues Mol Biol 2026)
- Unlike LBP, its structural relatives BPI, CETP and PLTP show no expression difference in necrotizing enterocolitis, isolating LBP as the disease-associated biomarker (J Pediatr Surg 2026)
- CETP inhibitor trials reframe the HDL hypothesis around apoB lowering rather than HDL-C raising (Drugs 2026)
- Preclinical safety battery clears the anti-CETP intranasal vaccine HB-ATV-8 for cardiac, mutagenic and metabolic risk (Arch Med Res 2026)
- Bayesian network meta-analysis of 84,134 patients ranks evacetrapib and anacetrapib best for cardiovascular outcomes among CETP inhibitors (Medicine 2026)
- Cis-Mendelian randomization finds CETP modification reduces both coronary disease and type 2 diabetes risk (Cardiovasc Diabetol 2026)
- In liver cells, miR-30b-3p cuts CETP reporter activity by 86% at the mRNA level, but CETP protein itself does not budge (Mol Biol Rep 2026)
- A review traces how CETP-inhibitor design evolved from first-generation scaffolds plagued by off-target toxicity to optimized late-generation clinical candidates (Eur J Med Chem 2026)
- Molecular dynamics show mixed cholesteryl-ester and triglyceride cargo twists CETP into strained, asymmetric conformations (Phys Chem Chem Phys 2026)
- CETP renaissance: a review maps obicetrapib reach beyond LDL-C into dementia, glycaemic control, sepsis and kidney function (Curr Atheroscler Rep 2026)
- CETP activity, but not mass, is independently linked to coronary disease in patients with high HDL cholesterol (Anatol J Cardiol 2026)
- From torcetrapib failure to obicetrapib promise: a full review of the mechanism and trial programme through PREVAIL (J Am Heart Assoc 2026)
- Network meta-analysis of 9,248 patients ranks obicetrapib plus ezetimibe plus statin best overall, obicetrapib plus statin safest among CETP-inhibitor combinations (J Cardiovasc Pharmacol 2026)
- In CETP mice, obicetrapib plus ezetimibe on top of atorvastatin regresses established atherosclerosis by 44% via LDL-receptor-driven VLDL clearance (J Lipid Res 2026)
- Post hoc BROADWAY/BROOKLYN analysis: obicetrapib attenuates kidney function decline, tracking with achieved HDL-C (Am J Prev Cardiol 2026)
- Pooled phase 3 safety data on 2,880 patients show obicetrapib matches placebo for adverse events, with no blood pressure signal (Am J Prev Cardiol 2026)
- BROOKLYN: obicetrapib cuts LDL-C by 36.3% and Lp(a) by 45.9% in 354 patients with heterozygous familial hypercholesterolaemia (Nat Med 2026)
- Meta-analysis of 3,088 patients: obicetrapib cuts LDL-C by 32% and Lp(a) by 36% with no excess adverse events (Vasc Dis 2026)
- Network meta-analysis of 6,025 patients: obicetrapib outperforms bempedoic acid for LDL-C lowering on top of statins by 15 percentage points (J Clin Lipidol 2026)
- In BROADWAY, obicetrapib slows p-tau217 progression, most in APOE4 carriers, positioning CETP inhibition against Alzheimer's disease (Am J Prev Cardiol 2026)
- A tunnel-like hydrophobic channel enables CETP bidirectional neutral lipid transfer, structurally distinct from other lipid-binding proteins (J Mol Graph Model 2026)
- Early-phase MACE signals predicted outcomes-trial results in 6 of 7 cholesterol drugs, dalcetrapib the exception (Am Heart J Plus 2026)
- Network meta-analysis of 2,937 patients: obicetrapib outperforms anacetrapib on LDL-C, HDL-C and overall adverse events (Daru 2026)
- CETP inhibitors, state of the science: why torcetrapib, dalcetrapib, anacetrapib and evacetrapib failed and why obicetrapib is different (Curr Cardiol Rep 2026)
- CETP rs3764261 genotype modifies the HDL-C lowering effect of a vegetarian diet in 9,263 adults (Taiwan Biobank) (Front Nutr 2026)
- Review surveys how current and emerging lipid therapies, including CETP inhibitors, affect lipoprotein(a) levels (Eur Cardiol 2026)
- Mendelian randomization finds genetically proxied CETP inhibition sharply raises the risk of primary Sjögren's syndrome (Curr Pharm Biotechnol 2026)
- Reduced CETP activity accompanies an atherogenic small dense LDL profile in long-standing type 1 diabetes (Front Endocrinol 2026)
- Phospholipid plugs inside two side pores of CETP accelerate triglyceride transfer through a newly described 'gliding' mechanism (Comput Struct Biotechnol J 2026)
- Meta-analysis of 657 patients: obicetrapib combination therapy, especially with ezetimibe at 10mg, beats obicetrapib monotherapy for LDL-C lowering (Semergen 2026)
2025 57
- Review weighs CETP-expressing hamsters against mice and rats for translational relevance in atherosclerosis modeling (Int J Mol Sci 2025)
- Obicetrapib review: an amphipathic CETP inhibitor cutting LDL-C 30-51%, apoB 20-33% and Lp(a) 30-57% across BROOKLYN, BROADWAY and TANDEM (Cardiol Rev 2025)
- Proteomics plus Mendelian randomisation could have flagged the blood-pressure toxicity of torcetrapib before ILLUMINATE, a proof-of-concept analysis argues (medRxiv preprint 2025)
- Splice-site CETP mutations are found in 10% of a South Indian familial hypercholesterolemia cohort (Cureus 2025)
- Higher CETP concentration is linked to coronary plaques in familial hypercholesterolemia, but not independently after adjustment (J Clin Lipidol 2026)
- GRADE-assessed meta-analysis of 3,399 patients: obicetrapib raises the odds of reaching an LDL-C target under 55 mg/dL more than sixfold (Diabetes Obes Metab 2026)
- Review surveys the evolving landscape of lipid-lowering drug targets, from statins to CETP and Lp(a) inhibition (Eur Heart J 2025)
- Children with obesity show reduced CETP activity alongside broader HDL antioxidant breakdown and higher oxidative stress (J Clin Lipidol 2026)
- The EUROASPIRE IV survey finds lower CETP activity in coronary patients with elevated triglycerides and residual apoB-driven risk (Clin Chim Acta 2026)
- BROADWAY substudy: obicetrapib cuts p-tau217 rise by a placebo-adjusted 20% in ApoE4/E4 carriers with cardiovascular disease (J Prev Alzheimers Dis 2026)
- Meta-analysis of nine RCTs in 3,516 patients confirms obicetrapib lowers LDL-C by 37% and Lp(a) by 41% with no excess adverse events (Cardiol Rev 2025)
- dal-GenE: the MI benefit of dalcetrapib in ADCY9 AA-genotype patients survives adjustment for an 18-variable risk prediction index (Eur J Prev Cardiol 2025)
- The two faces of CETP inhibitors: a review argues the therapeutic case has shifted from raising HDL-C to lowering apoB, with obicetrapib as proof (Curr Opin Lipidol 2025)
- Machine learning and molecular dynamics show why obicetrapib binds the CETP hydrophobic tunnel more tightly than the failed torcetrapib (ChemMedChem 2025)
- Genetically lower CETP activity reduces dementia risk in a 1,091,775-person Mendelian randomization meta-analysis (Alzheimers Dement 2025)
- Updated meta-analysis of 3,381 patients: obicetrapib cuts LDL-C by 37% and, unexpectedly, new-onset diabetes by 12% (Am J Prev Cardiol 2025)
- Network meta-analysis of 33 RCTs in 120,292 adults: atorvastatin plus obicetrapib ranks best for LDL-C, rosuvastatin plus obicetrapib best for HDL-C (Clin Cardiol 2025)
- Pooled analysis of 2,884 patients: obicetrapib cuts coronary events by 32% (HR 0.68) beyond 6 months, ahead of the PREVAIL readout (J Am Coll Cardiol 2025)
- Cross-trait GWAS links hearing loss to HDL and triglyceride genetics, flagging CETP as a candidate druggable target (Mol Genet Genomics 2025)
- Largest paediatric lipid GWAS to date confirms CETP as a robust HDL locus in Indian schoolchildren, with rare CETP variants also implicated (J Hum Genet 2025)
- Review surveys why raising HDL with CETP inhibitors and apoA1 infusion has failed to cut cardiovascular events (Clin Med Res 2025)
- Blood gene-expression signature of ITGB3, VEGFA and CETP tracks the extent of coronary artery stenosis, odds ratio 7.49 (Biochemistry (Mosc) 2025)
- REMBRANDT trial design: 300 ASCVD patients to test whether obicetrapib plus ezetimibe shrinks coronary plaque on CT angiography (Am Heart J 2025)
- Mouse mechanism study: CETP inhibition raises HDL, which blocks IL-1beta activation via SR-B1 and cuts endotoxaemia mortality (J Lipid Res 2025)
- CETP protein-truncating variants cut coronary artery disease risk even in Japanese patients with severe familial hypercholesterolemia (Atherosclerosis 2025)
- CETP inhibitors cut lipoprotein(a) by 46 percent, the largest reduction among all lipid-lowering drug classes in a 147-trial meta-analysis (Atherosclerosis 2025)
- CETP rs3764261 T allele, a known atherosclerosis-protective variant, is linked to protection against eye inflammation after brolucizumab (Genes 2025)
- Drug-drug interaction study finds no clinically meaningful effect of obicetrapib on atorvastatin or rosuvastatin exposure in healthy volunteers (Am J Cardiovasc Drugs 2025)
- A mathematical model extends CETP-mediated triglyceride flux estimation to chylomicrons in postprandial lipemia (J Lipid Res 2025)
- In Tangier disease, CETP activity drives an LDL-triglyceride buildup on top of near-total HDL loss, a four-patient case series shows (J Clin Endocrinol Metab 2025)
- CETP inhibitors reduce disease severity in experimental colitis by reprogramming macrophages and boosting gut barrier function (J Lipid Res 2025)
- Mendelian randomization links CETP inhibition to lower lacunar stroke risk via cerebral small vessel disease genetics (Brain 2025)
- Genetic CETP deficiency review: heterozygotes have lower ASCVD risk, homozygotes show no excess risk, and very high HDL-C raises AMD questions (J Atheroscler Thromb 2025)
- TANDEM: obicetrapib plus ezetimibe fixed-dose combination cuts LDL-C by 48.6% versus placebo in 407 high-risk patients (Lancet 2025)
- BROADWAY: obicetrapib lowers LDL-C by 29.9% versus 2.7% with placebo in 2,530 high-risk patients (N Engl J Med 2025)
- Predicted CETP and LPL cardiovascular risk genotypes are most prevalent in populations with Native American ancestry (Mol Biol Rep 2025)
- Mendelian randomization finds genetically proxied CETP inhibition reduces sepsis-related critical care admission and death (World J Emerg Med 2025)
- CETP inhibition is identified as the optimal target for managing dyslipidemia in systemic lupus erythematosus (Int Immunopharmacol 2025)
- Endothelial dysfunction develops earlier in male than female CETP-humanised hyperlipidaemic mice, preceding atherosclerosis (Geroscience 2025)
- Machine learning flags CETP as an immune biomarker for diabetes-tuberculosis comorbidity, AUC 0.804 (Microorganisms 2025)
- A hierarchical transformer model identifies an APOA4-CETP epistatic interaction underlying triglyceride to HDL cholesterol ratio (bioRxiv 2025)
- CETP promoter and coding variants predict HDL cholesterol levels in a Bangladeshi population (Biochem Biophys Rep 2025)
- Chikungunya virus is sensitive to evacetrapib in cell culture, but through an off-target effect independent of CETP itself (Viruses 2025)
- CETP expression raises body metabolism and leanness in female mice during both cold exposure and thermoneutrality (FASEB J 2025)
- Indian patients with high HDL cholesterol are more active, leaner, and at lower cardiovascular risk, with numerically but not significantly lower CETP levels (Ir J Med Sci 2025)
- Mendelian randomization links CETP inhibition and elevated LDL cholesterol to Lewy body dementia risk (Prog Neuropsychopharmacol Biol Psychiatry 2025)
- Beyond small-molecule inhibitors: a review surveys CETP-targeted immunotherapy and vaccines as an emerging route to raising HDL (Hum Vaccin Immunother 2025)
- Genetic proxies for CETP inhibition are linked to lower preeclampsia risk in a Mendelian randomization study (Int J Womens Health 2025)
- Chlorinated diaryl sulfonamides identified as potent new CETP inhibitors reaching 100 percent inhibition (Curr Comput Aided Drug Des 2025)
- Tofacitinib raises CETP and atherogenic lipids in rheumatoid arthritis patients naive to prior biologic therapy (J Clin Lipidol 2025)
- Case report finds pemafibrate paradoxically lowers HDL cholesterol in a patient with CETP deficiency (J Clin Lipidol 2025)
- CETP genetic variants shape the lipid response to statins in Alzheimer's disease patients (Sao Paulo Med J 2025)
- Mendelian randomisation study finds no genetic link between CETP-mediated LDL-C and pulmonary vascular disease, unlike NPC1L1 and PCSK9 (Pulm Circ 2025)
- Systematic review finds PCSK9, CETP and CDKN2B-AS1 polymorphisms among the strongest genetic contributors to myocardial infarction in Saudi Arabia (J Saudi Heart Assoc 2025)
- Meta-analysis of seven studies: adding a CETP inhibitor to high-intensity statins significantly raises HDL-C and lowers LDL-C with no added adverse events (Front Endocrinol 2025)
- Evacetrapib more than doubled circulating ApoA5 in the ACCELERATE and ACCENTUATE trials, explaining how CETP inhibitors lower triglycerides (J Clin Lipidol 2025)
- Meta-analysis of nine RCTs in 3,706 patients: obicetrapib plus ezetimibe adds a further 17.8% LDL-C reduction over obicetrapib alone (J Clin Lipidol 2025)
2024 61
- Meta-analysis of five early RCTs in 288 patients: obicetrapib reduces LDL-C by 41% and raises HDL-C by 157% (J Clin Lipidol 2025)
- Lp(a) review names obicetrapib the only drug besides apheresis to meaningfully lower Lp(a), cutting it by 40% (Nutr Metab Cardiovasc Dis 2025)
- Mendelian randomisation finds genetically proxied CETP inhibition associated with lower uterine fibroid risk (Heliyon 2025)
- Repurposed as a cancer drug: evacetrapib blocks a CEA-KRT1 interaction that drives oxaliplatin resistance in gastric cancer (Drug Resist Updat 2025)
- Unlike anacetrapib, obicetrapib clears completely from the body and does not accumulate in fat, monkey and human data show (Pharmacol Res Perspect 2024)
- CETP expression rises with obstructive sleep apnoea severity in obese young rats (Sleep Breath 2024)
- Two CETP gene variants independently predict worse outcomes after ischemic stroke, alongside HMGCR and PCSK9 variants (J Am Heart Assoc 2024)
- Genome-wide meta-analysis of myopic macular neovascularisation finds the AMD-linked CETP locus rs12720922 also protects against this retinal disease (Ophthalmol Retina 2025)
- CETP rs708272 GG genotype blunts the benefit of a dietary intervention when trans fatty acid intake is high, secondary analysis finds (Nutrients 2024)
- A wild valerian relative and beta-sitosterol inhibit CETP and lower lipids in triton-induced hyperlipidemic rats (Food Sci Nutr 2024)
- CETP variants show BMI-dependent associations with atherogenic lipids and glucose traits in gestational diabetes (J Matern Fetal Neonatal Med 2024)
- CETP inhibition as a longevity pathway: apoB lowering, not HDL raising, is the mechanism, with signals in diabetes, dementia and kidney disease (Curr Opin Lipidol 2024)
- Drug-target Mendelian randomization finds lower CETP concentration cuts Lewy body and Parkinson's dementia risk, especially in APOE-e4 carriers (Alzheimers Res Ther 2024)
- Mendelian randomisation study centred on HMGCR also finds CETP-mediated LDL-C consistently associated with lower aortic aneurysm risk (Nutr Metab 2024)
- Is obicetrapib a game changer? A review reframes CETP inhibition around apoB and LDL-C lowering rather than raising HDL-C (Expert Opin Pharmacother 2024)
- Correcting hyperglycemia does not restore apoC1 inhibition of CETP activity in type 1 diabetes (Metabolites 2024)
- CETP TaqIB genotype shows no association with the effect of dulaglutide on HbA1c or hepatic steatosis, unlike PNPLA3 (Endocrine 2024)
- Mendelian randomization finds genetically raised HDL via CETP predicted to lower small vessel stroke risk (J Am Heart Assoc 2024)
- PK/PD trial in 48 healthy Chinese volunteers shows obicetrapib behaves like it does in White participants, supporting the global phase 3 programme (J Clin Pharmacol 2024)
- Obicetrapib, the rebirth of CETP inhibitors? A review of ROSE and ROSE2 phase 2 data ahead of four ongoing phase 3 trials (Curr Atheroscler Rep 2024)
- CETP-driven HDL lowering, unlike ApoE knockout, does not worsen muscle wasting in dysferlin-deficient mice (Lipids Health Dis 2024)
- CETP gene polymorphisms are linked to blunted heart rate response to exercise, first study of its kind reports (Int J Mol Sci 2024)
- Mendelian randomisation: genetically proxied CETP inhibition cuts abdominal aortic aneurysm risk (OR 0.127) but shows no benefit for calcific aortic valve stenosis (Rev Cardiovasc Med 2024)
- Drug-target Mendelian randomization finds genetically proxied CETP inhibition protects against subarachnoid hemorrhage with no safety signal (Eur Stroke J 2025)
- Mendelian randomisation finds higher genetically predicted CETP, alongside HMGCR and PCSK9, associated with greater aortic aneurysm risk (Eur J Prev Cardiol 2024)
- The CETP rs708272 G/G genotype is significantly linked to dyslipidemia in Chinese patients with diabetes (World J Clin Cases 2024)
- CETP damages perivascular fat function in male mice through oxidative stress and inflammation, but preserves it in females (Function (Oxf) 2024)
- Mendelian randomisation across ancestries: CETP inhibition should protect against cardiovascular disease equally in East Asian and European populations (Nat Commun 2024)
- A review positions CETP alongside PCSK9 and CYP7A1 as the three central druggable regulators of cholesterol homeostasis (Life Sci 2024)
- CETP expression abolishes the atheroprotective effect of large HDL particles in mouse models of type 1 diabetes (Circ Res 2024)
- First meta-analysis of nine CETP-inhibitor RCTs finds a class-wide reduction in cardiovascular mortality and myocardial infarction (J Cardiovasc Dev Dis 2024)
- Knocking down CETP shrinks triple-negative breast cancer xenografts by 86% and restores tamoxifen sensitivity in resistant cells (IUBMB Life 2024)
- Population PK/PD model predicts obicetrapib ceiling effect: a maximum 51.1% LDL-C fall and 224% HDL-C rise (J Clin Pharmacol 2024)
- Rationale and design of BROADWAY and BROOKLYN: 2,886 participants randomised to test obicetrapib on top of maximally tolerated therapy (Am Heart J 2024)
- Multi-stage virtual screening identifies five novel CETP inhibitor lead compounds, confirmed active by biochemical assay (BMC Chem 2024)
- CETP variant rs5817082 is individually linked to extramacular drusen independent of overall AMD genetic risk (Invest Ophthalmol Vis Sci 2024)
- Ginseng compound Ginsenoside Re protects rat hearts from hypertrophy partly by suppressing CETP, matching the classical inhibitor anacetrapib (Cureus 2024)
- Anacetrapib reduces mortality from pneumococcal sepsis in mice by priming monocytes and speeding bacterial clearance (JCI Insight 2024)
- Phase 2 trial in 102 Japanese patients: obicetrapib 10mg on background statin cuts LDL-C by 45.8% and raises HDL-C by 159% (J Atheroscler Thromb 2024)
- CETP Taq1B polymorphism shows no association with cardiovascular risk factors or angiographic severity in Iranian angiography patients (Iran J Med Sci 2024)
- Unlike statins and ezetimibe, CETP inhibitors show only a slight, non-significant rise in CRP across a 53-trial meta-analysis (Cardiovasc Res 2024)
- Mendelian randomization links the LDL-lowering effect of CETP to reduced obstructive sleep apnea risk (Toxicol Appl Pharmacol 2024)
- Mendelian randomization finds CETP inhibition uniquely associated with increased breast cancer risk among lipid-lowering drug targets (Cancer Causes Control 2024)
- The CETP rs708272 AA genotype is linked to higher HDL cholesterol in an Iranian coronary artery disease cohort (J Clin Lab Anal 2024)
- CETP and apoA1 levels rise in blood during recovery from COVID-19, opposite to the acute-phase pattern (Sci Rep 2024)
- CETP-derived peptide Seq-1 directly suppresses pro-fibrotic gene expression in liver cells beyond its role in the anti-CETP vaccine (Arch Med Res 2024)
- Walnut kernel polyphenols are proposed to improve metabolic syndrome partly by inhibiting SREBPs, PCSK9 and CETP (Food Sci Nutr 2024)
- Review questions whether elevated HDL cholesterol truly protects against cardiovascular disease (J Clin Endocrinol Metab 2024)
- CETP variant rs708272 emerges as a candidate screening marker for type 2 diabetes risk in Filipinos, genomic study finds (PLoS One 2024)
- Review links HDL dysfunction in type 2 diabetes to impaired glycaemic control and highlights CETP inhibitors as a candidate therapy (Curr Med Chem 2024)
- Novel trifluoromethyl benzamides identified as potent CETP inhibitors with sub-micromolar activity (Curr Comput Aided Drug Des 2024)
- Combining CETP and SGLT2 inhibition genetically improves glycaemic control beyond either alone (Front Endocrinol (Lausanne) 2024)
- CETP gene variants help explain HDL cholesterol levels in children with sickle cell disease (Braz J Med Biol Res 2024)
- A methodology review highlights the APOE*3-Leiden.CETP mouse as a model that closely mimics human lipoprotein metabolism (Vasc Biol 2024)
- First Mendelian randomisation of lipid drug targets and diabetic retinopathy finds a PCSK9 signal but no CETP association (J Lipids 2024)
- Mendelian randomisation flags genetically proxied CETP inhibition as associated with higher male infertility risk, partly via vitamin D (Front Endocrinol 2024)
- Mendelian randomisation finds genetically higher CETP levels associated with increased non-endometrioid endometrial carcinoma risk (Front Endocrinol 2024)
- A validated mass spectrometry assay quantifies anacetrapib in fat tissue across three animal species and humans (Bioanalysis 2024)
- Newly synthesised fluorinated diaryl sulfonamides reach 100% CETP inhibition in vitro, guided by molecular modelling (Curr Comput Aided Drug Des 2024)
- CETP variants, an update: a review maps how CETP structure, animal models and SNPs shape lipid profiles and cardiovascular risk (Curr Pharm Des 2024)
- CETP-expressing mice heal cutaneous leishmaniasis lesions faster, shifting macrophages toward a healing M2 phenotype (Front Immunol 2024)
2023 59
- Reversing the tide of CETP inhibitor disappointments: a review of obicetrapib and its ROSE2 data ahead of pivotal phase 3 outcomes trials (Curr Atheroscler Rep 2024)
- Drug-target Mendelian randomization links genetically lower CETP to longer human lifespan (Aging 2023)
- Bioinformatics and molecular docking identify the soy isoflavone genistein as binding CETP among three key HDL-raising natural-product targets (J Transl Med 2023)
- Traditional dietary pattern adherence modulates the CETP Taq1B link to triglyceride levels in angiography patients (Nutr J 2023)
- Mendelian randomisation across nine drug targets and half a million lifespans finds genetically proxied CETP inhibition extends life expectancy (Lipids Health Dis 2023)
- A CETP variant predicts who loses the most weight with a digital lifestyle-modification program (Sci Rep 2023)
- A four-protein urinary panel including CETP, combined with tumor diameter and AFP/GGT levels, predicts microvascular invasion in liver cancer with concordance indices up to 0.809 (BMC Med 2023)
- HDL as a treatment target: a review says the obicetrapib outcomes trial will help decide whether to abandon the HDL hypothesis for good (Curr Atheroscler Rep 2023)
- A CETP variant is one of four factors in a nomogram predicting behavioral symptoms in Alzheimer's disease (Chin Med J 2024)
- Dietary antioxidant intake does not interact with the CETP Taq1B polymorphism to affect lipid profile or coronary stenosis severity (Food Sci Nutr 2024)
- Systematic review of 49 cardiovascular calcification trials finds dalcetrapib among the singleton agents showing no benefit (J Am Heart Assoc 2023)
- Small-quantity lipid-based nutrient supplements do not alter maternal HDL enzyme activity in pregnancy, but CETP and LCAT activity vary by season in Ghana (Curr Dev Nutr 2023)
- Genome-wide interaction analysis pinpoints a CETP variant that modifies how sedentary behavior affects HDL cholesterol (Nutrients 2023)
- Review examines how CETP and peripheral lipoproteins may contribute to vascular cognitive impairment and dementia (Mol Neurodegener 2023)
- A genome-wide association study identifies protective CETP gene variants underlying cardiovascular resilience in older adults (J Am Heart Assoc 2023)
- Beyond the heart: a review finds no excess macular degeneration risk across over 70,000 CETP-inhibitor trial patients, and surveys links to dementia, diabetes and sepsis (Pharmacol Res 2023)
- CETP expression in bone-marrow-derived immune cells reduces inflammatory features of atherosclerosis, helping explain trial failures (Biomolecules 2023)
- In a highly admixed population, four CETP gene variants explain part of the HDL-cholesterol variation across adolescents, adults and older adults (Clin Nutr ESPEN 2023)
- In REVEAL, new stroke, heart failure or cancer each cut quality of life and add thousands in hospital costs, but MI and coronary revascularisation alone do not (J Am Heart Assoc 2023)
- CETP activity rises stepwise from underweight to overweight/obese children, tracking with visceral-adiposity and lipid-accumulation indexes (Nutr Metab Cardiovasc Dis 2023)
- Whole-genome sequencing of unexplained severe familial hypercholesterolaemia turns up a novel CETP deletion variant (Vavilovskii Zhurnal Genet Selektsii 2023)
- A purple perilla extract lowers plasma CETP and reduces atheroma formation in apoE-deficient mice (Nutr Res Pract 2023)
- CETP is one of only three lipid-metabolism proteins strongly enriched in pre-beta-HDL, the small, highly active HDL subspecies (Basic Res Cardiol 2023)
- CETP is among seven cholesterol-handling genes up-regulated in peripheral blood of coronary artery disease patients (Curr Issues Mol Biol 2023)
- Molecular dynamics explains why the R201S and double I443W/V198W mutations cripple lipid transfer through CETP by warping its tunnel geometry (Biophys Chem 2023)
- CETP expression preserves endothelial function in female mice via enhanced estrogen receptor-alpha and eNOS signaling, unlike its harmful effect in males (Am J Physiol Heart Circ Physiol 2023)
- A probiotic strain lowers CETP expression alongside cholesterol-lowering effects in cell and animal models (J Med Food 2023)
- Simulating CETP as it really is, not the crystallography mutant, finds a new lead compound that jams its tunnel shut (Int J Mol Sci 2023)
- Late-onset preeclampsia blunts the normal second-trimester decline in HDL cholesterol, apoA-I, and CETP activity seen in low-risk pregnancies (Int J Mol Sci 2023)
- Cholesterol efflux capacity, but not CETP-mediated cholesterol ester transfer, correlates inversely with peripheral plaque volume (Biomedicines 2023)
- Dietary acid load interacts with CETP TaqB1 genotype to worsen lipid profile in B1B1 carriers with type 2 diabetes (BMC Endocr Disord 2023)
- A CETP variant is significantly associated with pentosan polysulfate (Elmiron) maculopathy, a genetic study of a drug-induced retinal disease finds (Retina 2023)
- Combined GIPR/GLP1R agonism additively lowers triglycerides, hepatic steatosis and Kupffer-cell-driven liver inflammation in CETP-humanised NAFLD mice (EBioMedicine 2023)
- Time-restricted eating reduces atherosclerotic lesion size and inflammatory cell content in CETP-humanised mice during simulated shift-work (EBioMedicine 2023)
- CETP gene haplotypes raise cardiovascular risk partly through mechanisms independent of triglycerides and HDL cholesterol (Int J Mol Sci 2023)
- Bound phospholipids bend cholesteryl esters into a transferable shape inside CETP, with the N-terminal lipid doing most of the work (J Chem Inf Model 2023)
- A Polynesian-specific CETP missense variant lowers CETP activity by 27.9% and improves the lipid profile (HGG Adv 2023)
- A probiotic normalises diet-induced CETP gene upregulation in a rabbit model of fatty liver disease (Sci Rep 2023)
- Review names CETP among four validated targets for novel lipid-lowering therapies to prevent cardiovascular disease (Nat Rev Cardiol 2023)
- Adcy9 gene inactivation shrinks infarct size and preserves cardiac function after MI, but mainly when CETP is absent (Can J Cardiol 2023)
- The CETP rs708272 genotype predicts statin response only in women with hyperlipidaemia (Malays J Med Sci 2023)
- Serum amyloid A is required for CETP to promote atherosclerosis in mice, suggesting CETP inhibition may help patients with high inflammation (J Lipid Res 2023)
- A multiancestry Mendelian randomization study suggests CETP inhibition may protect against preeclampsia via HDL cholesterol (Hypertension 2023)
- How CETP moves cholesterol between lipoproteins: a structural review of the mechanism behind torcetrapib, anacetrapib and obicetrapib (Curr Atheroscler Rep 2023)
- Mendelian randomization identifies CETP inhibition as a potential heart failure prevention strategy, acting mainly through apoB (Eur J Prev Cardiol 2023)
- Mendelian randomization finds HDL cholesterol protective against diabetic retinopathy, but genetically proxied CETP inhibition shows no effect (Atherosclerosis 2023)
- Sex and BMI modify how much genetically lower CETP raises HDL-C and lowers LDL-C, though not cardiovascular outcomes (Genet Epidemiol 2023)
- Genetic evidence suggests the HDL cholesterol-sepsis association is not causally mediated through CETP (Clin Transl Sci 2023)
- A review of HDL biology in atherosclerotic cardiovascular disease highlights the shift from HDL quantity to HDL quality, with attention to CETP inhibitor trial outcomes (Clin Investig Arterioscler 2023)
- Meta-analysis of 70 studies confirms CETP rs708272 is linked to lower coronary artery disease risk and higher HDL cholesterol (Front Cardiovasc Med 2023)
- Mendelian randomization finds genetically proxied CETP inhibition, mediated through HDL cholesterol, reduces Crohn's disease risk (Front Immunol 2023)
- Review proposes probucol as an alternative stroke-prevention therapy for patients at high haemorrhage risk (Brain Circ 2023)
- Abdominal obesity combines with the CETP TaqIB variant to raise cholesterol in Mexican women (Lifestyle Genom 2023)
- CETP missense variants raise HDL cholesterol mainly by reducing protein secretion, not intrinsic lipid-transfer activity (PLoS One 2023)
- The CETP rs708272 risk allele is linked to higher cardiac gene expression and interacts with diet and smoking to triple the risk of low HDL (Front Nutr 2023)
- Evacetrapib crosses the blood-brain barrier within 30 minutes, positioning CETP inhibitors as candidates for Alzheimer's disease (Front Pharmacol 2023)
- Mendelian randomisation finds genetically proxied CETP inhibitors protect against sepsis, an effect explained largely by ApoA-I (Front Cardiovasc Med 2023)
- Trifluoromethylated sulfonamides reach 100% CETP inhibition in vitro, guided by induced fit docking and pharmacophore mapping (Med Chem 2023)
- Phase 2 trial: obicetrapib plus ezetimibe on top of high-intensity statins cuts LDL-C by 63.4%, with 87% of patients reaching under 55 mg/dL (J Clin Lipidol 2023)
2022 61
- A specific CETP isoform tracks disease severity and may help neutralize bacterial toxin in Gram-negative sepsis (Mol Med 2022)
- Review notes that impaired apoC1 inhibition of CETP in diabetes may explain elevated CETP activity in diabetic patients (Cardiovasc Diabetol 2022)
- miR-16 simultaneously suppresses CETP alongside five other atherosclerosis-related genes in liver cells without toxicity (Sci Rep 2022)
- Korean GWAS of 72,298 people finds a CETP variant significant for dyslipidaemia overall and a second one only in men (Lipids Health Dis 2022)
- Increased fecal fatty acid and bile acid excretion, not cholesterol absorption, explains triglyceride-response heterogeneity in CETP-humanised mice (Nutrients 2022)
- Review asks whether CETP inhibitors are still worth pursuing after two decades of disappointing trials (Curr Atheroscler Rep 2022)
- Dalcetrapib and anacetrapib generate large apoE-containing HDL particles that can bind the hepatic LDL receptor (J Lipid Res 2023)
- A trans-ancestry GWAS in pregnant women finds the CETP locus approaches genome-wide significance for HDL cholesterol (J Clin Lipidol 2023)
- From raising HDL-C to lowering LDL-C: a review argues Mendelian randomisation and anacetrapib recast the whole CETP-inhibitor class (Cardiovasc Res 2022)
- The CETP TaqIB B1B2/B2B2 genotype raises the risk of fatty liver disease in Mexican women with gallstones (Metab Syndr Relat Disord 2023)
- Review proposes CETP inhibition among potential HDL-directed treatments for sepsis (Int J Mol Sci 2022)
- A review asks whether genomic analyses and post hoc trial insights can revive CETP inhibitors for cardiovascular prevention after past disappointments (Curr Opin Lipidol 2022)
- dal-GenE: dalcetrapib misses its primary endpoint in ADCY9 AA-genotype patients (HR 0.88), even after a genetically pre-selected retest of dal-OUTCOMES (Eur Heart J 2022)
- CETP is identified as a candidate serum biomarker for diagnosing sarcopenia in older adults (BMC Musculoskelet Disord 2022)
- In two large Korean cohorts, whether CETP raises cholesterol with alcohol depends on a person's ALDH2 genotype (Sci Rep 2022)
- Updated meta-analysis confirms CETP inhibitors cut new-onset diabetes risk by 16 percent (Eur Heart J Cardiovasc Pharmacother 2022)
- A 425,354-person UK Biobank Mendelian randomization study finds genetically lower CETP cuts coronary artery disease risk with additive benefit alongside PCSK9 (JAMA Cardiol 2022)
- CETP expression in macrophages curbs mitochondrial oxidant production and dampens pro-inflammatory, cholesterol-laden phenotypes (Antioxidants 2022)
- Targeted sequencing finds low-HDL-linked variants in CETP and three other genes in one in six people with metabolic syndrome (Diabetol Metab Syndr 2022)
- Systematic review names CETP-TaqIB as one of the most consistently studied gene-diet interactions in cardiovascular disease research (BMC Cardiovasc Disord 2022)
- CETP inhibition reduces major cardiovascular events through apoB lowering, a review argues, with obicetrapib cutting apoB by up to 30% (Int J Mol Sci 2022)
- In the multi-ethnic MESA cohort, higher HDL cholesterol, HDL particle number, and CETP mass predict lower long-term aortic valve calcification (Arterioscler Thromb Vasc Biol 2022)
- CETP-overexpressing mice develop worse psoriasis-like skin lesions with higher inflammatory cytokines than normal mice (Lipids Health Dis 2022)
- In ACCELERATE, a rising hsCRP trajectory over follow-up predicts MACE better than a single baseline reading, even when levels stay under 2 mg/L (Am J Cardiol 2022)
- CETP gene promoter hypomethylation is associated with coronary artery disease risk in a Chinese Han cohort (Mol Biol Rep 2022)
- Phase 2 trial in 120 patients: obicetrapib on top of high-intensity statins cuts LDL-C by up to 51% and raises HDL-C by up to 165% (Nat Med 2022)
- CETP activity raises brain cholesterol levels by reducing cholesterol efflux in transgenic mice (J Lipid Res 2022)
- A mathematical model of triglyceride lipolysis explains why cholesterol acquisition by HDL is maximal at intermediate HDL concentrations (Metabolites 2022)
- Two CETP gene variants raise coronary artery disease risk but do not predict restenosis after stenting (Arch Cardiol Mex 2022)
- Iranian case-control study finds no direct link between CETP polymorphism rs708272 and coronary artery disease, but flags a CETP-activity/HDL-C interaction (BMC Cardiovasc Disord 2022)
- Bacterial iron-chelating pigments called ferroverdins turn out to be potent CETP inhibitors, with 43 new structural variants identified (Biomolecules 2022)
- In APOE3-Leiden.CETP mice with diet-induced NASH, the oxysterol Oxy210 reduces adipose tissue IL-6, MCP-1 and macrophage markers (Int J Mol Sci 2022)
- CETP genetic variants predict baseline LDL cholesterol but not atorvastatin response in Jordanian patients (Drug Metab Pers Ther 2022)
- Walnut supplementation as a statin adjuvant lowers CETP activity and raises HDL cholesterol in hypertensive patients (Clin Exp Hypertens 2022)
- CETP activity correlates with atherogenic VLDL levels in women with anorexia nervosa (Biomedicines 2022)
- CETP levels track liver enzymes and metabolic markers in psoriasis patients on systemic therapy (Metabolites 2022)
- Rare CETP missense variants are linked to male-specific metabolic syndrome across five ancestries, transethnic exome study finds (Genes Genomics 2022)
- REVEAL extended follow-up: the coronary benefit of anacetrapib grows over time, 12% overall, with no long-term safety signal (Eur Heart J 2022)
- A systematic review finds no clear link between CETP genetic variation and intestinal cholesterol absorption (Prog Lipid Res 2022)
- CETP variant rs3764261 has a bigger population-level impact on low HDL cholesterol than smoking, Japanese cohort study finds (J Epidemiol 2022)
- Drug-target Mendelian randomization finds CETP and other lipid drug targets have distinct metabolomic signatures despite similar CAD benefit (PLoS Biol 2022)
- Review of 49 studies finds the TaqIB CETP variant is the most widely studied gene-diet interaction affecting blood lipids (Curr Atheroscler Rep 2022)
- Eating up to two eggs daily downregulates CETP mRNA in blood cells without affecting overall cholesterol balance in young Chinese adults (Food Sci Nutr 2022)
- LDL particle size governs how the natural CETP inhibitor ApoF binds and activates in hyperlipidaemic plasma (J Lipid Res 2022)
- CETP mutations are identified for the first time in South Indian patients with familial hypercholesterolemia (Clin Chim Acta 2022)
- Unlike three other newly identified EGPA biomarkers, CETP is selectively downregulated and negatively correlates with eosinophil count, aiding diagnosis versus severe asthma (Front Immunol 2022)
- A randomized trial finds lycopene supplements boost HDL PON-1 antioxidant activity and lower CETP activity in HDL2 and HDL3 without changing particle size (Front Nutr 2022)
- Abdominal aortic aneurysm patients show 49% higher CETP activity and altered HDL cholesterol efflux compared with atherosclerosis controls (Front Immunol 2022)
- CETP variant rs1532624 is among the five most prevalent clinically relevant pharmacogenomic markers found in Pakistani ethnic groups (Evol Bioinform Online 2022)
- CETP variant rs3764261 emerges as a lean-mass protective marker in a Pakistani obesity genetics cohort (PLoS One 2022)
- Bis(trifluoromethyl) benzylamino benzamides identified as potent new CETP inhibitor lead compounds (Med Chem 2022)
- EPA, but not DHA, significantly lowers CETP activity in a crossover trial of omega-3 fatty acid supplementation (J Clin Lipidol 2022)
- A novel hypothesis links high East Asian CETP deficiency prevalence to historical resistance against a liver-damaging parasite (Front Cell Dev Biol 2022)
- CETP haplotypes predict whether lipophilic statins help or harm cognition in Alzheimer's disease (J Alzheimers Dis 2022)
- Evacetrapib suppresses colorectal cancer cell growth by blocking Wnt/beta-catenin signaling and activating JNK (Biol Pharm Bull 2022)
- Proteomic profiling flags CETP as one of three ELISA-confirmed markers elevated in stent restenosis (Front Cardiovasc Med 2022)
- Plasma CETP, alongside EPCR, is an independent MACE risk factor in older men with chronic coronary syndrome and improves on the Framingham score (Front Cardiovasc Med 2022)
- Atorvastatin exposure is about twice as high in healthy Korean volunteers as in Caucasians, partly explained by eight variants including one in CETP (Front Genet 2022)
- Exome study in an underrepresented Mexican cohort finds a novel CETP variant, rs11076176, linked to higher risk of low HDL cholesterol (Front Genet 2022)
- Genetic CETP deficiency, mimicking a lifetime of CETP inhibition, trades a lower cardiovascular death and MI risk for a matching rise in AMD (JAMA Cardiol 2022)
- HDL and CETP: a textbook chapter surveys the tunnel structure, reverse cholesterol transport role and the still-unsettled case for inhibitors versus agonists (Adv Exp Med Biol 2022)
2021 51
- Why raising HDL with CETP inhibitors did not help: evacetrapib and torcetrapib both boosted the harmful apoC3-containing HDL subspecies most (Arterioscler Thromb Vasc Biol 2022)
- A systematic review of 118 randomized trials finds unsaturated fats, antioxidants, and moderate alcohol improve HDL functional traits including CETP activity (J Clin Med 2021)
- The CETP TaqIB polymorphism interacts with diet quality to shape metabolic markers in type 2 diabetes (J Hum Nutr Diet 2022)
- CETP promotes triglyceride storage in liver and intestinal cells, unlike its fat-reducing effect in adipocytes (Lipids 2021)
- The CETP rs5883 T allele is linked to higher HDL cholesterol and lower risk of low HDL in postmenopausal obese women (Eur Rev Med Pharmacol Sci 2021)
- ADCY9 and CETP show signs of having coevolved under sex-specific selection, offering a biological explanation for the pharmacogenomic signal of dalcetrapib (eLife 2021)
- Beyond failed HDL trials: a review argues the dal-GenE genomic-test approach to dalcetrapib and ADCY9 is the key to actionable HDL therapy (J Cardiovasc Pharmacol 2021)
- Drug-target Mendelian randomization confirms CETP as an effective target for coronary heart disease with an on-target macular degeneration risk (Nat Commun 2021)
- Hibernating brown bears raise CETP activity by 36% to stabilize HDL lipid composition and avoid atherogenic dyslipidemia (Sci Rep 2021)
- An ABCG1 gene variant is linked to higher CETP activity in a Brazilian population study (Biochem Genet 2022)
- Viewpoint charts efforts to optimize anacetrapib into a best-in-class CETP inhibitor (J Med Chem 2021)
- Long-term matcha green tea worsens reverse cholesterol transport and fails to prevent diet-induced arteriosclerosis in rabbits (Mol Nutr Food Res 2021)
- A genome-wide significant signal near CETP is linked to doubled HDL cholesterol in youth with type 2 diabetes (J Endocr Soc 2021)
- Human CETP transgene boosts macrophage reverse cholesterol transport in mice, but cannot rescue PLTP deficiency (J Physiol Biochem 2021)
- MK-8262 is invented as a best-in-class CETP inhibitor backup to anacetrapib after its 9% added cardiovascular risk reduction (J Med Chem 2021)
- CETP TaqB1 polymorphism interacts with dietary insulin index to shape cardiovascular risk in type 2 diabetes (Sci Rep 2021)
- Lower plasma CETP tracks with milder depression severity, including anhedonia and guilt, in a preliminary mood-disorder proteomics study (J Psychiatr Res 2021)
- A CETP isoform, CETPI, is highlighted as a newly described contributor to LPS inactivation in the gut-liver axis of sepsis (Biomed Pharmacother 2021)
- CETP concentration does not differ between peripheral artery disease patients with or without type 2 diabetes (Vasc Med 2021)
- The same cysteine-binding chemistry that makes dalcetrapib a CETP inhibitor also lets it block the SARS-CoV-2 3CL protease (ACS Omega 2021)
- Anacetrapib pharmacokinetics in healthy Chinese subjects closely match those seen in black and white populations (Adv Ther 2021)
- A high triglyceride to HDL cholesterol ratio predicts elevated CETP activity in children (Indian J Pediatr 2021)
- Dalcetrapib (JTT-705) blocks SARS-CoV-2 cell fusion by disrupting spike protein disulfide bonds (FASEB J 2021)
- A new palladium-catalysed C-H fluorination reaction offers a concise late-stage route to anacetrapib (Chem Commun 2021)
- Molecular dynamics simulations reveal how sugar chains on CETP shape its lipid-transfer tunnel (J Chem Inf Model 2021)
- Meta-analysis of nearly 13,000 patients confirms evacetrapib lowers LDL-C by 34 mg/dL and raises HDL-C substantially (Prostaglandins Leukot Essent Fatty Acids 2021)
- Feed efficiency correlates with distinct hepatic gene-expression patterns across diet duration in CETP-humanised mice, per a new dynamic model (Physiol Rep 2021)
- How ADCY9 and CETP might interact inside arterial macrophages to explain the genotype-dependent effect of dalcetrapib, with dal-GenE poised to test it (Circ Genom Precis Med 2021)
- Fetal HDL carries reduced CETP activity despite similar enzyme levels to the mother, review finds (Biomedicines 2021)
- CETP pathophysiology and inhibition, an update: the drug class biology, trial status and adverse effects surveyed before obicetrapib phase 3 (Drug Discov Today 2021)
- Low CETP activity late in pregnancy, in mother and placenta alike, is linked to giving birth to small-for-gestational-age infants (Sci Rep 2021)
- CETP is used to illustrate why Mendelian randomization of drug targets differs methodologically from randomization of biomarkers (Nat Rev Cardiol 2021)
- HDL-cholesterol predicts carotid atherosclerosis only when CETP concentration is low, in the IMPROVE study (Biomedicines 2021)
- Trivalent implant vaccine targets PCSK9, ApoB, and CETP as "cholesterol checkpoint" proteins (Adv Ther (Weinh) 2021)
- Elafibranor reduces steatosis, hepatic inflammation and fibrosis progression in CETP-humanised NASH mice, with 87% pathway overlap to human NASH (Sci Rep 2021)
- Obesity alters LCAT and CETP activities and shifts HDL toward smaller, less anti-oxidative particles in young women (Biomedicines 2021)
- Advanced mass spectrometry reveals that CETP is secreted in medium-large HDL and stays there, unlike LCAT which appears on HDL only after a delay (JCI Insight 2021)
- The low-density lipoprotein receptor is required for CETP to control triglyceride metabolism in mice of both sexes (Physiol Rep 2021)
- GWAS of 49,915 Koreans finds CETP among the lipid genes shared by metabolically unhealthy normal-weight and obese phenotypes (Sci Rep 2021)
- Human ApoC1 transgene reduces atherosclerosis in rabbits partly by inhibiting CETP activity (Atherosclerosis 2021)
- CETP inside endothelial cells directly causes oxidative stress and vascular dysfunction, independent of its effect on HDL (Biomolecules 2021)
- eMERGE Network study fails to replicate the CETP-triglyceride association found in prior smaller studies (BMC Med Genomics 2021)
- Sepsis rapidly suppresses LCAT and CETP activity while raising PLTP and endothelial lipase, with LCAT activity predicting mortality (Front Cell Dev Biol 2021)
- A randomized trial finds omega-3 supplementation significantly lowers CETP activity and shrinks small HDL in high-cardiovascular-risk patients (Front Nutr 2021)
- Swapping hamster CETP for human CETP cuts HDL by 60% and boosts hepatic cholesterol 1.8-fold in a human-like hamster model (J Lipid Res 2021)
- A human CETP minigene improves insulin sensitivity and reduces fatty liver in female but not male mice on a high-fat diet (Front Physiol 2021)
- Review names the CETP TaqIB polymorphism as one of three gene variants that heighten cardiovascular risk in heavy drinkers (Curr Neurovasc Res 2021)
- Desmodium gyrans extract raises HDL-promoting SR-B1 and apoA-I while lowering CETP expression in liver cells (Indian J Pharmacol 2021)
- CETP gene variants predict residual atherogenic dyslipidaemia in Thai patients on statin therapy (Pharmgenomics Pers Med 2021)
- Three months of water-based exercise moved body weight in obese older men but left CETP activity and blood lipids unchanged (Diabetes Metab Syndr 2021)
- CETP pushes macrophages toward the M2 phenotype and worsens elastase-induced emphysema in mice, an unexpected lung-disease link (Front Immunol 2021)
2020 64
- ApoC-II and apoC-III move from VLDL preferentially into larger HDL3 particles, and a CETP inhibitor does not change this transfer (Biol Chem 2021)
- Despite no direct LPS-binding activity, human CETP raises mortality in mouse models of endotoxemia and sepsis by impairing lipoprotein-mediated protection (J Lipid Res 2020)
- Anacetrapib raises macrophage cholesterol efflux capacity in men, with the effect modified by haptoglobin genotype in diabetes (JAHA 2020)
- Genetic and drug-based CETP inhibition preserves HDL and improves survival in sepsis, in humans and humanized mice (Circulation 2021)
- Intensive insulin therapy in newly diagnosed type 1 diabetes progressively suppresses serum CETP and PLTP over the first year (Nutr Metab Cardiovasc Dis 2021)
- Cyclic and bicyclic urea and sulfamide cores yield new CETP inhibitors effective in vivo (Bioorg Med Chem Lett 2020)
- A novel anti-adipogenic role for CETP: it boosts brown fat activity and lipolysis to reduce body fat, across three animal models (Metabolism 2021)
- A loss-of-function CETP variant raises HDL cholesterol without raising ApoA1 or protecting against heart attack in Chinese patients (Nutr Metab Cardiovasc Dis 2021)
- CETP shifts HDL toward small, immature particles in coronary heart disease patients (Clin Lab 2020)
- Roux-en-Y gastric bypass lowers CETP activity alongside other markers of HDL function in severe obesity (Obes Surg 2020)
- An acoustic-fusion formulation of torcetrapib boosts drug exposure roughly 8-fold over a crystalline suspension in rats (Int J Pharm 2021)
- Gut metabolite TMAO shows no link to genetically determined CETP levels in coronary artery disease patients (Sci Rep 2020)
- GWAS confirms CETP as one of only three genome-wide loci for Lp(a) levels while discovering a novel APOH locus (Arterioscler Thromb Vasc Biol 2020)
- A new ELISA for oxidized HDL finds the highest levels in patients with CETP-deficiency-related hyperalphalipoproteinemia, and lower levels with probucol treatment (J Atheroscler Thromb 2021)
- CETP variant rs3764261 is linked to polypoidal choroidal vasculopathy in a Portuguese population, but not in a Singaporean cohort (Br J Ophthalmol 2021)
- In ACCELERATE, elevated Lp(a) only predicted death, MI and stroke when hsCRP was also 2 mg/L or higher (JAMA Cardiol 2020)
- CETP inhibitors in precision medicine: a review ties three phase 3 failures, the shelving of anacetrapib over fat accumulation, and the ADCY9 pharmacogenomic clue together (Clin Chim Acta 2020)
- Prolonged bedrest suppresses HDL cholesterol efflux capacity without affecting CETP or LCAT activity (Sci Rep 2020)
- Fine-mapping in two Kuwaiti Arab cohorts flags rs1864163 in CETP as a candidate causal variant for HDL cholesterol (Hum Genet 2021)
- Mendelian randomisation links genetically raised HDL and LDL cholesterol, including a CETP locus signal, to higher breast cancer risk (PLoS Med 2020)
- Swapping dietary palmitic acid for stearic acid raises CETP mass without changing its activity (Clin Nutr 2020)
- Repeated dosing shows dalcetrapib does not accumulate in rats despite forming covalent disulfide bonds with tissue thiols (Xenobiotica 2021)
- A PBPK model correctly predicts higher exposure to the active thiol form of dalcetrapib in chronic kidney disease (Xenobiotica 2021)
- CETP impairs triglyceride clearance in male mice through androgen receptor signalling (Lipids 2020)
- First Samoan genome-wide association study confirms CETP-HDL cholesterol link in a previously unstudied Polynesian population (J Hum Genet 2020)
- Apolipoprotein F emerges as a natural, LDL-selective inhibitor of CETP (Curr Opin Lipidol 2020)
- In a north Indian CAD study, CETP rs708272 alone was not significant, but showed a synergistic interaction with physical inactivity (BMC Cardiovasc Disord 2020)
- CETP variant rs5882 carries a 25-fold higher risk of atrophic age-related macular degeneration in a Lithuanian case-control study (Mol Genet Genomic Med 2020)
- Diet-induced metabolic syndrome triggers 1396 differentially expressed adipose transcripts, revealing immune and remodeling gene signatures in CETP-humanised mice (Genomics 2020)
- Swapping hamster CETP for human CETP in chow-fed hamsters humanizes their lipoprotein profile, cutting HDL up to 50% (J Lipid Res 2020)
- Population pharmacokinetic-pharmacodynamic model recommends a 200 to 400 mg dose of the CETP inhibitor CKD-519 (Pharmaceutics 2020)
- CETP promoter variant rs1800775 reduces the odds of essential hypertension in a Mexican population (Genet Test Mol Biomarkers 2020)
- Neither ad libitum nor time-restricted voluntary wheel running altered atherosclerotic lesion size in CETP-humanised mice or lipid profile in obese men (Obesity (Silver Spring) 2020)
- LDL receptor enables a CETP-independent route for macrophage cholesterol to reach faeces, mouse study finds (Circ Res 2020)
- The largest cohort study on the topic finds physical activity boosts HDL cholesterol efflux capacity, and shows a U-shaped CETP response in people with diabetes (Eur J Prev Cardiol 2021)
- QSAR models predict CETP inhibitory potency of 108 oxazolidinone derivatives (SAR QSAR Environ Res 2020)
- An undesirable postprandial triglyceride response enhances CETP-mediated cholesteryl ester transfer to chylomicrons and reduces hepatic HDL cholesteryl ester uptake (Biomolecules 2020)
- CETP mass and activity vary only slightly across apoE- and apoC-III-defined HDL subtypes, while LCAT concentrates in apoE/apoC-III-free HDL (Lipids Health Dis 2020)
- A review commits to covering PCSK9, ANGPTL8, sortilin and CETP as candidate molecular links between psoriasis and cardiometabolic syndrome risk (Int J Mol Sci 2020)
- CETP variant rs708272 ranks among the top ten SNPs in a 24-gene model predicting childhood and adolescent obesity, alongside diet and gut microbiota (Sci Rep 2020)
- CETP variant rs708272 shows a striking association with childhood HDL cholesterol and triglycerides in a pan-European cohort (Sci Rep 2020)
- Diet-controlled type 2 diabetes speeds catabolism of several HDL proteins, and CETP activity tracks inversely with plasma adiponectin (Biomolecules 2020)
- Liver-humanized mice show a human-like cholesterol lipoprotein profile without needing CETP (Hepatology 2020)
- Carriers of the CETP Taq1B B2 allele only show worse cholesterol with a high-sucrose diet or physical inactivity, a gene-environment study finds (J Hum Nutr Diet 2020)
- Higher serum CETP levels are linked to acute coronary syndrome, with the association modified by TaqIB genotype (Lab Med 2020)
- Red yeast rice supplement linked to extreme HDL cholesterol via apparent CETP downregulation in a case report (Lab Med 2020)
- dal-OUTCOMES secondary analysis: dalcetrapib cuts new-onset diabetes by 23% after acute coronary syndrome, NNT of 40 (Diabetes Care 2020)
- A review argues the failure of CETP inhibitors and niacin to reduce cardiovascular events undermines the HDL cardioprotection hypothesis (Drugs 2020)
- Elevated CETP activity in early pregnancy predicts prediabetes five years later, tracking with monocyte activation (J Clin Endocrinol Metab 2020)
- In 8,236 diabetes patients from ACCELERATE, evacetrapib raised HDL by 131% and lowered LDL by 32%, yet produced no clinical benefit (BMJ Open Diabetes Res Care 2020)
- Ellagic acid from unripe Rubus coreanus extract lowers hepatic CETP and HMG-CoA activity while raising LCAT activity, reducing cholesterol in rats (Nutrients 2020)
- Higher preoperative plasma CETP is one of four protein signals linked to atrial fibrillation after bypass surgery (J Thorac Cardiovasc Surg 2021)
- Landmark hypothesis proposes CETP as an immunological gatekeeper that could be repurposed to treat sepsis (Trends Endocrinol Metab 2020)
- Genetic variants at the CETP inhibitor target show split effects on ischaemic small vessel stroke and brain haemorrhage (Brain 2020)
- Exon-9-deleted CETP isoform blocks full-length CETP secretion and redirects cells toward storing triglyceride (J Lipid Res 2020)
- In hypertensive rats made to express human CETP, blood pressure rose and fatty liver accelerated, yet atherosclerosis did not (Hypertens Res 2020)
- dal-GenE trial design: only patients with the ADCY9 AA genotype will be enrolled, testing whether the benefit of dalcetrapib is genetically confined (Am Heart J 2020)
- Certain CETP gene haplotypes raise the triglyceride to HDL cholesterol ratio more often in Roma than Hungarian populations (Genes 2020)
- Korean GWAS discovers six novel CETP SNPs associated with low HDL cholesterol (PLoS One 2020)
- CETP variant rs5882 interacts with monounsaturated fat intake to affect triglyceride levels in overweight and obese adults (Lifestyle Genom 2020)
- Book chapter reviews CETP research from its discovery to the disappointing clinical-trial era (Adv Exp Med Biol 2020)
- CETP TaqIB genotype shapes how plant oils affect metabolic markers in people with diabetes (J Cardiovasc Thorac Res 2020)
- In 1,855 Ghanaian adults, CETP variant rs17231520 is the leading genetic signal for HDL cholesterol, replicating a finding rare in West African cohorts (Front Genet 2020)
- Meta-analysis of 62,431 patients across 11 RCTs finds CETP inhibitors do not reduce major adverse cardiovascular events (RR 0.97) (Cardiology 2020)
2019 55
- Homozygous B4GALT1 mutations cause CETP hypoglycosylation and reduced activity, yielding larger HDL particles (J Inherit Metab Dis 2020)
- Liposomal CETP vaccine protects rabbits against atherosclerosis where the failed clinical peptide vaccine did not (Pharm Dev Technol 2019)
- In the ACCELERATE diabetes cohort, higher baseline HbA1c independently predicted cardiovascular events despite statin therapy (J Am Heart Assoc 2020)
- Calcitriol raises CETP levels alongside HDL-C in a rabbit model of atherosclerosis (Int J Vitam Nutr Res 2019)
- Even NMR-measured HDL particle concentration, not just HDL-C, failed to predict cardiovascular risk in dal-Outcomes (Am Heart J 2020)
- LXR and PPAR-alpha agonists suppress ApoF, the natural CETP regulator, via a shared hormone response element (Biochim Biophys Acta Mol Cell Biol Lipids 2019)
- CETP genetic variants predict how much LDL cholesterol falls with statin therapy (Pharmacogenomics J 2020)
- Genetic CETP inhibition doesn't touch particle-size-defined LDL-C the way statins do, but lowers remnant, VLDL and HDL-triglyceride content instead (PLoS Biol 2019)
- Unlike torcetrapib, evacetrapib left plasma aldosterone unchanged in ACCELERATE, and aldosterone did not predict cardiovascular events (J Am Heart Assoc 2019)
- Ursolic acid ester derivatives designed as novel plant-based CETP inhibitors (Bioorg Med Chem Lett 2019)
- Anacetrapib accumulates to 0.6 mmol/L in mouse adipose tissue without impairing adipose function, even after weight loss (Pharmacol Res Perspect 2019)
- CETP variant rs708272 doubles the risk of myocardial infarction in men from Western Siberia (Biomolecules 2019)
- An anacetrapib analog cuts CETP activity by 89% and reduces neointimal hyperplasia in bypassed rabbit veins by 38% (Sci Rep 2019)
- Comparative genomics finds widespread natural loss of the CETP gene across placental mammals (NAR Genom Bioinform 2019)
- Alternating light-dark cycles mimicking shift work roughly double atherosclerotic lesion size and severity in CETP-humanised mice (J Pineal Res 2019)
- CETP promoter variants that raise HDL cholesterol also lower the risk of type 2 diabetes and diabetic kidney disease in Taiwanese adults (Genes 2019)
- Hydrocarbon-stapled peptides jam the self-binding switch of CETP more than fivefold better, a new route to blocking the protein (J Mol Graph Model 2020)
- ApoF knockdown boosts CETP-mediated cholesterol ester transfer to LDL and impairs cholesterol clearance in fat-fed hamsters (J Lipid Res 2019)
- Meta-analysis of 332,912 patients: lowering apoB only cuts cardiovascular risk when it works through the LDL receptor, not via CETP inhibitors or fibrates (Eur J Prev Cardiol 2020)
- CETP variant rs6499861 lowers HDL cholesterol more strongly in obese Korean men and women with a family history of diabetes (J Lipid Atheroscler 2019)
- CETP redirects cholesterol elimination away from the gut and toward bile, steering HDL cholesteryl esters differently than those from LDL (Arterioscler Thromb Vasc Biol 2019)
- Steered molecular dynamics show torcetrapib and anacetrapib block CETP by physically plugging its lipid-transfer tunnel (Biochemistry 2019)
- Four weeks of oral Akkermansia muciniphila lowers cholesterol and reshapes immune cell populations in CETP-humanised mice, but does not reduce cuff-induced neointima formation (Mol Nutr Food Res 2019)
- GWAS of 10,093 Indians finds CETP the primary genetic locus for metabolic syndrome, with a seven-variant haplotype as the strongest signal (Biomolecules 2019)
- Rare CETP variants found in most Korean adults with extremely high HDL cholesterol, but do not alter cholesterol efflux (Sci Rep 2019)
- REVEAL, the largest ADCY9 pharmacogenetic study yet, finds no genotype interaction with the benefit of anacetrapib, unlike the dalcetrapib hypothesis (Circulation 2019)
- Preclinical pharmacokinetic modeling predicts a human dose of the CETP inhibitor CKD519 before phase 1 data revealed a gap (Pharmaceutics 2019)
- Neither a liraglutide RCT nor a 1,611-person cohort finds any link between liver fat content and circulating CETP, despite CETP's hepatic Kupffer-cell origin (Sci Rep 2019)
- Genetically determined CETP concentration shows only a weak link to clotting factor VII and no link to venous thrombosis risk (J Thromb Haemost 2019)
- QSAR modelling and molecular docking chart a path to new CETP inhibitor compounds for coronary heart disease (J Biomol Struct Dyn 2020)
- A reformulated version of the CETP inhibitor DRL-17822 reduces its food-driven exposure spike (Clin Pharmacol Drug Dev 2019)
- Do CETP inhibitors have a role in treating cardiovascular disease? A review weighs harm, futility and modest benefit against emerging genomic clues (Am J Cardiovasc Drugs 2019)
- CETP variant rs708272 GG genotype cuts the odds of optic neuritis with multiple sclerosis by 62% in a Lithuanian case-control study (Ophthalmic Genet 2019)
- Lead triphenylethanamine CETP inhibitor shows clean blood pressure profile and robust efficacy (ACS Med Chem Lett 2019)
- Simvastatin lowers HMGR but not CETP expression in bovine adipocytes (Anim Biotechnol 2020)
- Review of new oral dyslipidaemia drugs names anacetrapib the only CETP antagonist that reduces cardiovascular events (Eur J Prev Cardiol 2020)
- CETP Taq1B genotype shifts HDL and LDL subclass distribution in African-American men (Future Cardiol 2019)
- CETP variant rs708272 is linked to reduced risk of pituitary adenoma and its recurrence (Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub 2020)
- Evacetrapib raises large and medium HDL but cuts the functionally important preβ-1 HDL by 36%, a clue to why raising HDL-C didn't help (Atherosclerosis 2019)
- CETP activity does not track carotid intima-media thickness once diabetes control is poor, unlike in well-controlled patients (Acta Diabetol 2019)
- Cynanchum wilfordii extract lowers CETP alongside cholesterol and apoB in adults with high LDL cholesterol (Nutrients 2019)
- Shrinking anacetrapib nanoparticles below 100 nm boosts bioavailability in dogs beyond what dissolution rate alone explains (J Pharm Sci 2019)
- A rare CETP variant lowers HDL cholesterol and predicts worse survival in sepsis, with Mendelian randomization suggesting causation (Am J Respir Crit Care Med 2019)
- High-dose PFOA raises HDL cholesterol by suppressing cholesteryl ester transfer activity in mice (Toxicol Sci 2019)
- In ACCELERATE, higher baseline fasting insulin independently predicted MACE and future revascularisation in diabetes patients (Diab Vasc Dis Res 2019)
- JACC review: four CETP inhibitors reached phase 3, one died, two were stopped for futility, and the survivor was shelved over fat accumulation (J Am Coll Cardiol 2019)
- Fish intake and dietary fat modify how two CETP gene variants affect cholesterol and triglyceride changes over time (Eur J Clin Nutr 2019)
- A simple diffusion-like mathematical model estimates how much triglyceride CETP shuttles between lipoproteins from routine lipid measurements (BMC Syst Biol 2019)
- A year of higher legume and fish intake lowers CETP activity in a large cardiovascular-risk cohort (Mol Nutr Food Res 2019)
- Multi-model computational study of 140 benzoxazole compounds maps the structural requirements for potent CETP inhibition (J Biomol Struct Dyn 2019)
- Review questions whether HDL cholesterol is a modifiable treatment target after disappointing CETP inhibitor trials (JRSM Cardiovasc Dis 2019)
- CETP rs5883 polymorphism does not distinguish coronary artery disease patients from controls in a Turkish cohort (In Vivo 2019)
- Kiwifruit raises adipose CETP gene expression but not serum CETP activity in hamsters (Avicenna J Phytomed 2019)
- Review asks whether anacetrapib, the fourth CETP inhibitor tested, finally outperforms its predecessor drugs (Cardiol Rev 2019)
- Genetic CETP deficiency loads HDL with apoE, apoC-III, ANGPTL3 and complement proteins, offering a clue why high HDL-C doesn't protect these patients (J Clin Lipidol 2019)
2018 65
- Anacetrapib parks itself in the lipid droplets of fat cells without needing active transport, explaining its long half-life and shelving (Drug Metab Dispos 2019)
- Meta-analysis of 154,601 patients: HDL-raising drugs including CETP inhibitors do not cut cardiovascular or all-cause mortality, and any MI benefit traces to fibrates (Eur J Prev Cardiol 2019)
- CETP rs708272 raises HDL cholesterol and lowers atherogenic index in men but not women, without affecting coronary disease risk (Medicine 2018)
- Colorectal cancer patients have higher CETP activity and lower LCAT and PON-1 activity, with CETP mass an independent risk predictor (Clin Biochem 2019)
- CETP variant rs1800777 predicts low HDL cholesterol and acute kidney injury risk during sepsis, replicated across two cohorts (Sci Rep 2018)
- Mendelian randomisation upends the textbook story: the causal effects of CETP fall mainly on large HDL and small VLDL, not LDL, hinting anacetrapib works by cutting VLDL (Eur J Hum Genet 2019)
- High-dose dietary inulin shifts gut bacteria and raises short-chain fatty acids without reducing cholesterol or atherosclerosis in CETP-humanised mice (Sci Rep 2018)
- A review of dalcetrapib pharmacokinetics finds no clinically significant drug interactions across over 13,000 patients and volunteers (Clin Pharmacokinet 2018)
- Lower CETP levels track with more severe heart failure and higher natriuretic peptide (Lipids Health Dis 2018)
- ADCY9 inactivation cuts atherosclerosis by 65 percent in mice, but only when CETP is absent (Circulation 2018)
- CETP TaqIB genotype shapes HDL cholesterol but not diabetes risk in Southern Thai adults (Arch Med Res 2018)
- Review contrasts disappointing CETP antagonists with the anti-inflammatory promise of the CETP agonist probucol (Atherosclerosis 2018)
- Unlike statins, anacetrapib lowers rather than raises new-onset diabetes risk on top of a coronary benefit, a review argues for a statin-plus-CETP-inhibitor combination (Atherosclerosis 2018)
- In obese CETP-transgenic mice, anacetrapib improved HDL function but drove fatty liver and insulin resistance, a clue to trials where two-thirds of patients were obese (Diabetes 2018)
- Two CETP polymorphisms and a three-locus haplotype raise coronary artery disease risk in a Polish population (Mol Biol Rep 2018)
- CETP genotype does not modify how DHA supplementation lowers triglycerides, randomized feeding trial finds (Lipids 2018)
- Early formulation work solves the poor solubility of the CETP inhibitor CKD-519 ahead of phase 1 testing (Int J Pharm 2018)
- CETP I405V variant shows a strong, first-reported association with ischemic stroke risk in a Caucasian population (J Stroke Cerebrovasc Dis 2018)
- CETP promotes exchange of the inflammatory apolipoprotein serum amyloid A between lipoproteins (Arterioscler Thromb Vasc Biol 2018)
- What the cetrapib trials taught us: torcetrapib, evacetrapib and anacetrapib all raised atherogenic apoproteins, muddying the HDL-raising story (Curr Opin Lipidol 2018)
- The lipid-lowering effect of anacetrapib is smaller in Black subjects than White subjects despite identical pharmacokinetics (J Clin Pharmacol 2018)
- CETP Taq1B combined with an NOS3 variant multiplies the risk of type 2 diabetes and cardiovascular disease eightfold (Cardiovasc Diabetol 2018)
- Anacetrapib reproduced the CETP-deficiency phenotype and showed a highly significant, if moderate, coronary benefit in REVEAL, a review on HDL and atherogenic inflammation notes (Atherosclerosis 2018)
- Update on novel lipid drugs: anacetrapib cut coronary events by 7% but not wider CVD outcomes, leaving CETP inhibitors without further development (Curr Opin Cardiol 2018)
- CV risk, CV benefit, or both? A review takes stock of CETP inhibitors after preclinical promise met mostly disappointing outcome trials (Clin Pharmacol Ther 2018)
- A randomized trial finds baru almonds reduce waist circumference and CETP expression while raising HDL in overweight women (Nutrition 2018)
- Metabolic liver inflammation in obesity does not clearly lower CETP, unlike bacterial-endotoxin activation of Kupffer cells (Atherosclerosis 2018)
- Dietary fat intake modifies how CETP variant rs5882 affects HDL cholesterol and blood pressure risk (Iran J Basic Med Sci 2018)
- Existing CETP inhibitors were designed against an unglycosylated crystal structure, but simulations show four sugar chains reshape the tunnel dynamics of the protein (Proteins 2018)
- For lipid management in diabetes, CETP inhibitor trials have generally underwhelmed and are no longer being developed, a review concludes (Diabet Med 2018)
- Combining policosanol with 10-dehydrogingerdione strengthens CETP inhibition and lowers platelet activation in dyslipidaemic rabbits (Appl Biochem Biotechnol 2018)
- First genome-wide association study identifies genetic determinants of circulating CETP concentration (Circ Genom Precis Med 2018)
- ACCELERATE nested case-control study finds no significant ADCY9 genotype interaction with evacetrapib, unlike the dalcetrapib signal (JAMA Cardiol 2018)
- Diet-induced weight loss fails to improve HDL cholesterol efflux or cholesteryl ester transfer in obese men (Atherosclerosis 2018)
- The C-terminal bound phospholipid grips CETP more tightly than the N-terminal one, keeping it bent and ready to carry lipids (J Phys Chem B 2018)
- Review ranks CETP and ANGPTL3 inhibition among the most promising novel LDL-lowering strategies (Curr Opin Lipidol 2018)
- Were the benefits of REVEAL with anacetrapib really major? A critical evaluation says not significant in years one or two, and modest overall (Expert Opin Pharmacother 2018)
- CETP markers show strong associations with HDL cholesterol across obesity phenotypes in an Iranian cohort, unlike most FTO variants (Eat Weight Disord 2020)
- Bacterial LPS lowers CETP by switching off resting Kupffer cells, an anti-inflammatory response that raises HDL during infection (J Am Heart Assoc 2018)
- Torcetrapib increases large HDL particles more than a novel FXR antagonist in a hamster model of dyslipidemia (Pharmacol Res Perspect 2018)
- Weight gain prevention counteracts the HDL-lowering effect of CETP variant rs3764261 in young adults, randomized trial finds (Nutr Metab Cardiovasc Dis 2018)
- A review of PLTP and CETP in atherogenesis weighs the mixed record of CETP inhibitors against open questions about PLTP (Adv Clin Exp Med 2018)
- CETP and its inhibitors, a foundational review: structure, mechanism, non-lipid functions and the full outcomes-trial record for four small-molecule inhibitors (J Lipid Res 2018)
- Meta-analysis finds CETP inhibitor therapy cuts diabetes incidence by 12 percent (Diabetes Metab 2018)
- CETP inhibitors as agents to reduce coronary heart disease risk: after earlier trial failures, REVEAL showed anacetrapib actually works (Cardiol Clin 2018)
- Patent review tracks CETP inhibitor development from 2009 to 2017 despite four phase 3 drugs falling short on cardiovascular outcomes (Expert Opin Ther Pat 2018)
- CETP inhibitors do not appear to raise new-onset diabetes risk unlike LDL-receptor-acting drugs (J Cardiovasc Pharmacol Ther 2018)
- CETP variant rs708272 raises acute coronary syndrome risk and shifts HDL subclass cholesterol content (Lipids 2018)
- In dal-Outcomes, Lp(a) after acute coronary syndrome did not predict recurrent ischaemic events on background statin therapy (JAMA Cardiol 2018)
- Metabolite profiling identifies more than 80 breakdown products of dalcetrapib in human plasma, none of them major (J Pharm Biomed Anal 2018)
- Lipid-based formulations boost oral exposure of a poorly soluble CETP inhibitor up to 10-fold in preclinical species (J Pharm Sci 2018)
- An 8-week randomized trial finds Cuban policosanol lowers blood pressure and CETP activity by 20% while boosting HDL function in healthy women (Oxid Med Cell Longev 2018)
- CETP-deficient patients show markedly more large HDL particles but fewer small, more anti-atherogenic HDL particles, alongside more atherogenic very small LDL (PLoS One 2018)
- Aerobic exercise reshapes arterial and macrophage gene expression toward atheroprotection in CETP-transgenic mice, independent of changes in CETP activity (Front Physiol 2018)
- CETP variant rs1800777 is linked to greater fat mass, central obesity, and lower HDL cholesterol in obese adults (Endocrinol Diabetes Nutr 2018)
- Lower serum CETP levels found in the oldest members of Greek long-lived families (Open Cardiovasc Med J 2018)
- Mendelian randomisation links the CETP inhibitor target locus to lower abdominal aortic aneurysm risk (JAMA Cardiol 2018)
- Large Chinese biobank study finds genetically lower CETP activity raises HDL cholesterol but not vascular protection (JAMA Cardiol 2018)
- Statin-driven normalisation of HDL lipid composition lags behind LDL and apoB reduction, revealing role of CETP (J Clin Lipidol 2018)
- CETP variant rs1800777 A allele linked to milder liver damage in fatty liver disease (Ann Nutr Metab 2018)
- Curcumin does not significantly change serum CETP levels in metabolic syndrome, trial finds (Avicenna J Phytomed 2018)
- The CETP I405V polymorphism is an independent risk factor for Alzheimer's and vascular dementia in a Southern Italian cohort (J Alzheimers Dis 2018)
- A well-powered Mendelian randomization study finds CETP-driven HDL cholesterol is not associated with Alzheimer's disease risk (Alzheimers Dement 2018)
- Modeling shows adding a CETP inhibitor would push LDL-target attainment above 95 percent in familial hypercholesterolemia, versus just 54 percent with ezetimibe alone (J Clin Lipidol 2018)
- Meta-analysis identifies two CETP variants among the leading genetic risk factors for polypoidal choroidal vasculopathy in Asians (J Ophthalmol 2018)
2017 79
- Weight loss plus exercise normalizes the HDL lipidome, lowers CETP activity, and boosts cholesterol efflux capacity in metabolic syndrome (Arterioscler Thromb Vasc Biol 2018)
- The present therapeutic role of CETP inhibitors: REVEAL numbers, HDL-C +104%, LDL-C -18%, major coronary events RR 0.91, against three prior failures (Pharmacol Res 2018)
- Meta-analysis of 34,781 patients confirms the lipid benefits of anacetrapib carry no excess hepatic or muscular risk (Postgrad Med 2018)
- Prebeta-1 HDL, the particle CETP feeds on, is elevated across three dyslipidaemia phenotypes in 2,435 people (J Clin Lipidol 2018)
- Formulation science: a lipid-based delivery system boosts oral absorption of the CETP inhibitor CP-532,623, and supersaturation, not just solubility, predicts how well (Mol Pharm 2017)
- New benzyl benzamide compound inhibits CETP by 82.2% in vitro, with docking confirming it fits the drug pocket (Arch Pharm 2017)
- Mendelian randomization finds no overall causal link between genetically determined CETP and carotid intima-media thickness (J Clin Lipidol 2018)
- Exercise raises HDL in CETP-transgenic mice by lowering CETP activity 19%, and an anabolic steroid specifically blunts that effect (Lipids 2017)
- A new piperidine-based CETP inhibitor retains potency in hypertriglyceridemic plasma where other CETP inhibitors lose efficacy (J Med Chem 2017)
- Adding torcetrapib to atorvastatin lowers lipoprotein(a) by 11 percent while modestly raising PCSK9, an ILLUMINATE biomarker substudy finds (J Clin Lipidol 2018)
- Inhibiting CETP with des-fluoro-anacetrapib cuts in-stent intimal area by 43% via a scavenger receptor-B1-dependent pathway (ATVB 2017)
- Trials and tribulations of CETP inhibitors: the REVEAL benefit traces to lower non-HDL-C, not higher HDL-C, plus a small diabetes reduction (Circ Res 2018)
- Nat Rev Cardiol commentary: the REVEAL coronary benefit from CETP inhibition is probably down to lowering non-HDL-C, not raising HDL-C (Nat Rev Cardiol 2017)
- N,N-substituted amine derivatives yield a sub-micromolar CETP inhibitor lead compound (Molecules 2017)
- A proteomic risk score could have flagged harm from torcetrapib within 3 months of ILLUMINATE, revealing unexpected immune and inflammatory effects (Circulation 2018)
- Six-month high-fat feeding of CETP-humanised male mice reveals a biphasic lipid response with insulin resistance preceding dyslipidemia, mirroring human ageing (Physiol Rep 2017)
- Anacetrapib, the new CETP inhibitor: raises large HDL2 and pre-beta HDL, lowers Lp(a) via ApoA production, and shows a hint of glucose benefit (Diseases 2017)
- CETP TaqIB B2B2 genotype blunts cholesterol-lowering response to simvastatin in Thai patients (Cardiovasc Ther 2017)
- Pharmacogenetics of HDL-targeting and statin therapies: dal-OUTCOMES and dal-PLAQUE-2 gave concordant results for dalcetrapib in the favourable genotype (Curr Atheroscler Rep 2017)
- In 1,264 Lithuanians, two CETP variants raise exudative AMD risk up to 1.7-fold while a third, rs3764261, cuts it by 1.8-fold (Gene 2017)
- Landmark genetic study explains why CETP inhibitors lower LDL cholesterol without reducing cardiovascular events (JAMA 2017)
- Electron microscopy shows torcetrapib and anacetrapib block CETP by favoring binary complexes over ternary lipoprotein bridging (Biochim Biophys Acta 2017)
- Human CETP transgenic pigs created as a new model for dyslipidaemia and atherosclerosis research (Lipids Health Dis 2017)
- A hospital pharmacy bulletin sums up CETP inhibitors for practising pharmacists: three failures, then a REVEAL success for anacetrapib (Hosp Pharm 2017)
- A single dose of anacetrapib inhibits CETP equally well in young Japanese and white men, with a Japanese breakfast boosting exposure similarly (J Clin Pharmacol 2018)
- Saffron-derived crocin raises CETP levels within treated patients, but not significantly versus placebo (ARYA Atheroscler 2017)
- REVEAL: anacetrapib cuts major coronary events by 9% in 30,449 patients already on intensive statin therapy (N Engl J Med 2017)
- Molecular dynamics simulations show torcetrapib, anacetrapib, and evacetrapib all destabilize the hydrophobic tunnel of CETP (J Biomol Struct Dyn 2018)
- No benefit with evacetrapib despite raising HDL 130% and cutting LDL 37%: is this the end of the road for the cetrapibs? (Expert Opin Pharmacother 2017)
- Nat Rev Cardiol: most genetic variants that raise HDL-C don't lower cardiovascular risk, but CETP variants are a notable exception (Nat Rev Cardiol 2018)
- In Japanese patients, evacetrapib added to atorvastatin cuts LDL-C by 25.70% versus placebo and more than doubles HDL-C (Circ J 2017)
- Review maps CETP-mediated transfer as the indirect route of reverse cholesterol transport to the liver (Anatol J Cardiol 2017)
- CETP TaqIB variant is linked to diabetic retinopathy incidence over nine years, though HbA1c and triglycerides prove the stronger predictors (Diabetes Res Clin Pract 2017)
- CETP can carry triglycerides too, not just cholesteryl esters, and simulations show why the slower TG transfer happens (Sci Rep 2017)
- Anacetrapib lowers lipoprotein(a) by cutting its production rate 41%, not by speeding its clearance (ATVB 2017)
- Neovascular age-related macular degeneration is linked to more HDL and IDL particles, an association unaffected by the CETP D442G mutation (J Lipid Res 2017)
- Basal-bolus insulin lowers maternal triglycerides in gestational diabetes without changing CETP activity (J Obstet Gynaecol Res 2017)
- Evacetrapib monotherapy lowers LDL-C by 34.3% and raises HDL-C by 124% in Japanese patients with hypercholesterolemia (Circ J 2017)
- Meta-analysis confirms the CETP TaqIB B2 allele protects against ischemic stroke (J Stroke Cerebrovasc Dis 2017)
- Five of six CETP polymorphisms are linked to metabolic syndrome in Uyghur adults, with two protective haplotypes identified (Int J Environ Res Public Health 2017)
- Glucocorticoids downregulate CETP gene expression in macrophages, and doubling hydrocortisone dose lowers CETP activity and raises HDL size in patients (Eur J Clin Invest 2017)
- Only 42% of 96,944 CETP-inhibitor trial subjects ever appeared in a published report, a case study in biomarker-driven drug development finds (Circ Cardiovasc Qual Outcomes 2017)
- CETP inhibitors lower lipoprotein(a) by around 50 percent, review notes, in comparison with apheresis and other new drugs (Atheroscler Suppl 2017)
- CETP variant rs3764261 is one of four risk alleles linked to lower HDL cholesterol in pregnant Chinese women (Oncotarget 2017)
- Evacetrapib failed to reduce cardiovascular events despite large lipid changes in ACCELERATE (N Engl J Med 2017)
- A new dissolution test detects as little as 10% crystalline drug contamination in evacetrapib spray-dried dispersion tablets (J Pharm Biomed Anal 2017)
- Same drug, opposite effect: dalcetrapib raised HDL in rabbits but cut it 48% in monkeys, while anacetrapib behaved consistently across species (J Lipid Res 2017)
- Protein-truncating CETP variants lower coronary heart disease risk by 30 percent in a 58 469-participant sequencing study (Circ Res 2017)
- Human phase 1 data confirm anacetrapib keeps accumulating in fat for a year while plasma levels plateau, explaining its long residence time (Clin Pharmacol Ther 2017)
- Mendelian randomization finds HDL-raising CETP variants also raise the risk of age-related macular degeneration (Ophthalmology 2017)
- CETP knockout rabbits show less atherosclerosis, better cholesterol efflux, and HDL that suppresses endothelial adhesion molecules (Arterioscler Thromb Vasc Biol 2017)
- A protective CETP haplotype, but not individual TaqIB or D442G variants, lowers essential hypertension risk in Chinese Mongolians (Turk J Med Sci 2017)
- Phase 3 trial finds anacetrapib added to statins cuts LDL-C by 37% and more than doubles HDL-C, well tolerated over 24 weeks (Am J Cardiol 2017)
- ACCENTUATE: evacetrapib beat ezetimibe and higher-dose statin on LDL-C and Lp(a), but also raised hsCRP, a clue to why ACCELERATE later failed (Atherosclerosis 2017)
- The SGLT2 inhibitor dapagliflozin lowers HbA1c and body weight in type 2 diabetes but leaves HDL cholesterol, subfractions, and CETP activity unchanged (Cardiovasc Diabetol 2017)
- Rabbit developmental study finds the offspring-survival NOAEL for evacetrapib is a third of the maternal NOAEL (Birth Defects Res 2017)
- High-dose evacetrapib causes toxicity in parent rats but leaves fertility and fetal development unharmed in rats and rabbits (Birth Defects Res 2017)
- Torcetrapib raised HDL ApoC-III and LpA-I subclasses without altering ApoB particles in ILLUMINATE (Am J Cardiol 2017)
- Anacetrapib lowers VLDL triglyceride only on a statin background, by boosting the catabolic rate of VLDL-TG (J Lipid Res 2017)
- In Japanese patients, adding anacetrapib to statins nearly doubles HDL-C and sustains lipid benefits through a 28-week extension (Atherosclerosis 2017)
- CETP TaqIB genotype shapes how herbal tea affects HDL cholesterol and triglycerides in hypercholesterolemic patients (Asia Pac J Clin Nutr 2017)
- Policosanol supplementation reduced CETP activity by up to 32% and lowered blood pressure in healthy adults (Int J Mol Med 2017)
- Large-scale pleiotropy study identifies CETP as one of six newly discovered genome-wide-significant loci for coronary artery disease (J Am Coll Cardiol 2017)
- REVEAL trial design enrolled 30,449 patients to test whether anacetrapib lipid changes reduce cardiovascular events (Am Heart J 2017)
- A Mediterranean diet enriched with olive oil lowers CETP activity and improves multiple HDL functions in the year-long PREDIMED trial (Circulation 2017)
- CETP redistributes the vasoprotective lipid sphingosine-1-phosphate from HDL to apoB lipoproteins, changing which signals it triggers (Arterioscler Thromb Vasc Biol 2017)
- Pharmacogenomics review details how ADCY9 genotype determines the cardiovascular effect of dalcetrapib in dal-OUTCOMES (ATVB 2017)
- Anacetrapib impairs endothelial function in CETP-transgenic mice despite raising HDL-C fivefold, while evacetrapib does not (Atherosclerosis 2017)
- Meta-analysis links the CETP C-629A polymorphism to higher coronary heart disease risk and circulating CETP in Caucasians (Oncotarget 2017)
- A review traces the evolution of HDL-raising therapeutics from niacin and fibrates to CETP inhibitors, reconstituted HDL, and apoA-I mimetics (Curr Pharm Des 2017)
- Systematic review of 23 studies finds the CETP B1 risk allele responds better to dietary interventions than B2B2 (Nutr Metab 2017)
- CETP variant rs1800775 is associated with HDL cholesterol and total cholesterol, but not LDL, in pregnant Chinese women (J Clin Lipidol 2017)
- CETP activity is highest in cord and maternal blood of growth-restricted neonates, alongside multiple proatherogenic lipoprotein changes (J Clin Lipidol 2017)
- Fluorinated benzamide CETP inhibitors reach sub-micromolar potency, with fluorine position dictating activity (Med Chem 2017)
- CETP gene variants are associated with neuropsychiatric symptom severity in Alzheimer's disease (Braz J Psychiatry 2017)
- Review weighs whether anacetrapib can succeed as a cardioprotective CETP inhibitor where earlier drugs failed (Drug Des Devel Ther 2017)
- Review details how evacetrapib raised HDL-C by 128% and cut LDL-C by 35% yet produced no clinical benefit in ACCELERATE (Cardiol Rev 2017)
- CETP gene variants linked to memory loss risk in a rural and tribal Indian cohort study (J Alzheimers Dis 2017)
- CETP-overexpressing transgenic rabbits show more macrophage foam cells despite unchanged lesion area (Mediators Inflamm 2017)
2016 76
- Total fat intake modifies the CETP Taq1B link to HDL cholesterol only in type 2 diabetes patients without dyslipidemia (Clin Nutr 2018)
- A year of Mediterranean diet raises HDL cholesterol and lowers triglycerides specifically in carriers of the CETP rs3764261 T allele, CORDIOPREV trial finds (Clin Nutr 2018)
- Pharmacokinetic review details the long elimination half-life and faeces-dominant clearance of anacetrapib (Expert Opin Drug Metab Toxicol 2017)
- Kinetic tracer studies reveal CETP inhibition raises apoA-I and lowers apoB by shifting catabolism rates of HDL and LDL in opposite directions (Curr Opin Lipidol 2016)
- MF59-adjuvanted CETP vaccine protects rabbits from atherosclerosis without a strong antibody or CETP-activity effect (Iran J Basic Med Sci 2016)
- Review highlights ADCY9 pharmacogenomics as a model for rescuing dalcetrapib and future lipid trials (Curr Opin Lipidol 2016)
- Review surveys CETP inhibitor outcome trials from the harm of torcetrapib to the futility of later agents (Curr Opin Lipidol 2016)
- CETP rs708272 B2 allele is linked to a more antiatherogenic LDL subfraction profile in statin-treated coronary heart disease patients (Biochem Genet 2016)
- Rare CETP coding variants linked to age-related macular degeneration risk in a Japanese population study (Hum Mol Genet 2016)
- CETP variant rs820299 nominally associates with metabolic syndrome and interacts with lifestyle factors in a Taiwanese replication study (Sci Rep 2016)
- Both 25 mg and 100 mg doses of anacetrapib substantially cut LDL-C and raise HDL-C on top of statin therapy (Am J Cardiol 2017)
- CETP variants that raise HDL cholesterol also increase risk of intracerebral haemorrhage (Ann Neurol 2016)
- Yamashita argues CETP inhibition may backfire by generating small dense LDL and downregulating hepatic SR-BI (Curr Opin Lipidol 2016)
- Fragment-based design yields a novel pentacyclic triterpenoid CETP inhibitor with sub-micromolar potency (Eur J Med Chem 2017)
- Meta-regression of 312 175 patients shows CETP inhibitors deliver less cardiovascular benefit than their LDL-lowering predicts (JAMA 2016)
- Arsenic trioxide independently raises CETP protein levels in liver cells while suppressing LXR-beta and cholesterol efflux (Chem Biol Interact 2016)
- Meta-analysis of over 40,000 subjects confirms CETP TaqIB B1 allele raises ischemic cardiovascular disease risk and lowers HDL cholesterol (Int J Environ Res Public Health 2016)
- The CETP locus is the only genome-wide-significant genetic determinant of HDL-C response to statins, independent of baseline HDL-C, in a 27,720-person meta-analysis (J Med Genet 2016)
- CETP knockout sensitizes estrogen-receptor-positive breast cancer cells to cholesterol-depleting cytotoxic agents (Genes Cancer 2016)
- Structural study designs a self-binding CETP peptide stabilized by pi-pi stacking and halogen bonding (Bioorg Chem 2016)
- CETP Taq1B is linked to glycated hemoglobin levels in hyperlipidemic patients with diabetes, a link modulated by an LIPG variant (Can J Diabetes 2016)
- Review compares torcetrapib, evacetrapib, dalcetrapib and anacetrapib trial outcomes and the future of CETP inhibition (J Cardiovasc Pharmacol Ther 2017)
- Cryo-electron tomography reveals a polyhedral, not spherical, 3D structure for VLDL particles (J Lipid Res 2016)
- LC-MS/MS method measures anacetrapib pharmacokinetics and low protein binding in rats (Biomed Chromatogr 2017)
- Plasma CETP is higher in metabolic syndrome, but the Taq1B genotype itself shows no direct link to the syndrome in Iranian subjects (Biochem Genet 2016)
- Circulating PCSK9 levels and CETP plasma activity are independently correlated in patients with metabolic disease (Cardiovasc Diabetol 2016)
- Higher serum CETP independently predicted mild cognitive impairment in type 2 diabetic patients (J Alzheimers Dis 2016)
- A new cycloalkene-scaffold CETP inhibitor raises HDL cholesterol in hamsters (Eur J Med Chem 2016)
- CETP TaqIB and I405V variants strongly linked to centenarian status in Hainan, China (Asian Pac J Trop Med 2016)
- CETP I405V shows no link to age or cardiovascular disease despite raising HDL cholesterol (BMC Geriatr 2016)
- Molecular dynamics simulations support a tunnel mechanism for lipid transfer by CETP (J Biol Chem 2016)
- Genotype-dependent dalcetrapib effects on cholesterol efflux and inflammation confirm the ADCY9 pharmacogenomic signal (Circ Cardiovasc Genet 2016)
- Urban versus rural residence predicts opposite CETP and PLTP activity patterns in Polish men, independent of smoking and alcohol use (Arch Med Sci 2016)
- Raising gastric pH with omeprazole modestly increases evacetrapib exposure, but not enough to matter clinically (Pharmacotherapy 2016)
- In female mice, CETP enables an estrogen-SHP pathway raising VLDL triglyceride production and, independently, an ERalpha pathway boosting liver fat oxidation (J Lipid Res 2016)
- CETP TaqIB, but not apo AI 75G/A, significantly shapes HDL cholesterol levels in Polish men and women (Arch Med Sci 2016)
- Active rheumatoid arthritis is linked to higher CETP activity and impaired paraoxonase function, with apoA-I predicting arterial stiffness (Atherosclerosis 2016)
- Higher serum CETP levels and the -629A allele are linked to angiographically confirmed coronary atherosclerosis (Indian J Clin Biochem 2017)
- Pigs bred for high CETP activity show altered hepatic expression of inflammatory genes and microRNAs, with gender and breed effects (Mamm Genome 2016)
- CETP inhibitors, challenges and perspectives: off-target failure for torcetrapib, futility for dalcetrapib and evacetrapib, early promise for anacetrapib and TA-8995 (Expert Rev Cardiovasc Ther 2016)
- CETP binds factor Xa and boosts prothrombinase activity, and the VTE-linked Gln451 variant shows five-fold higher thrombin generation than wild-type (J Atheroscler Thromb 2016)
- Whole-body model finds high-activity CETP genotypes raise LDL-C more with ageing than low-activity genotypes (Biosystems 2016)
- Molecular dynamics studies show small-molecule CETP inhibitors act by physically blocking the lipid transfer tunnel (J Phys Chem B 2016)
- All-atom simulations show a complete cholesteryl ester can pass through the CETP tunnel at a physiologically realistic rate (J Biol Chem 2016)
- A review appraises whether newer CETP inhibitors can avoid the off-target effects that undid torcetrapib (Curr Cardiol Rep 2016)
- A high-dose tetanus toxoid-CETP vaccine lowers CETP activity and raises HDL-C in rabbits but fails to reduce atherosclerotic lesions (Biomed Pharmacother 2016)
- Review distinguishes humanized-mouse from rabbit models to find where CETP inhibition truly protects against atherosclerosis (Eur J Clin Invest 2016)
- In Japanese patients with familial hypercholesterolaemia, anacetrapib cuts LDL-C by nearly 30% versus placebo in 12 weeks (Atherosclerosis 2016)
- Baseline CETP level predicts how much pitavastatin lowers LDL-C, via LXR-dependent suppression of CETP transcription (Lipids Health Dis 2016)
- Anacetrapib raises HDL apoA-I and plasma CETP levels by slowing their clearance rather than boosting their production (ATVB 2016)
- CETP inhibitors raise blood pressure through a CETP-independent, redox- and STAT3-dependent vascular contraction pathway (J Pharmacol Exp Ther 2016)
- Two CETP variants have opposite effects on coronary artery disease risk in the first such study in Saudi Arabians (Hum Genomics 2016)
- Novel benzylaminopropionanilide CETP inhibitors raise HDL and lower LDL in hamsters (Bioorg Med Chem 2016)
- Active hepatitis C infection is associated with higher serum CETP and HDL triglyceride than after viral eradication (World J Hepatol 2016)
- A protective CETP variant buffers the memory-decline effect of APOE4 in older adults (Neurobiol Aging 2016)
- Structural study refutes the ternary tunnel complex model of how CETP transfers cholesteryl ester (J Struct Biol 2016)
- Policosanol combined with reconstituted HDL outperforms anacetrapib at inhibiting CETP in a hyperlipidemic zebrafish model (Rejuvenation Res 2016)
- Severe hepatic impairment, but not severe renal impairment, raises evacetrapib exposure and prolongs its half-life (Eur J Clin Pharmacol 2016)
- CETP inhibition is not yet dead, argues a pro perspective ahead of the REVEAL trial (Arterioscler Thromb Vasc Biol 2016)
- CETP and PLTP exemplify how BPI-like TULIP proteins form tubular channels to exchange lipids between lipoprotein particles (Biochim Biophys Acta 2016)
- Across 6,606 adults and multiple imaging-based fat measures, no association is found between body fat and serum CETP, challenging the adipose-tissue-as-CETP-source hypothesis (Atherosclerosis 2016)
- A genome-wide meta-analysis in Hispanic populations confirms CETP as a genome-wide-significant locus for HDL cholesterol (Sci Rep 2016)
- CETP I405V variant shows no association with premature coronary artery disease presence or severity in Iranian patients (Bosn J Basic Med Sci 2016)
- CETP expression does not alter glucose tolerance, insulin secretion, or tissue glucose uptake in transgenic mice across multiple conditions (Lipids Health Dis 2016)
- dal-PLAQUE substudy finds dalcetrapib did not affect progression of vascular calcification (J Am Coll Cardiol 2016)
- A structure-guided approach discovers a novel indoline series of CETP inhibitors (ACS Med Chem Lett 2016)
- Human CETP transgenic mice show higher survival and lower IL-6 after polymicrobial sepsis, linked to reduced macrophage TLR4 and NF-kB activation (Mediators Inflamm 2016)
- Six months of aerobic exercise raises oxidized-HDL levels in women without any change in CETP or adiponectin concentration (Free Radic Res 2016)
- Review highlights zebrafish, which retain a cetp ortholog, as an emerging model for dyslipidaemia research (Front Endocrinol (Lausanne) 2016)
- Review weighs past CETP inhibitor trial failures against hopes for newer, more favourable agents (Clin Med Insights Cardiol 2016)
- Plasma CETP causes pancreatic beta cell dysfunction via islet cholesterol accumulation in mice (Nutr Metab 2016)
- Phase 1 single ascending dose study of the CETP inhibitor CKD-519 shows potent target inhibition (Drug Des Devel Ther 2016)
- Meta-analysis finds evacetrapib raises HDL-C by 86% and cuts LDL-C by 21%, with no effect on triglycerides (Curr Pharm Des 2016)
- Commentary marks evacetrapib as another CETP inhibitor lost to the gap between lipid improvement and clinical benefit (Bratisl Lek Listy 2016)
- CETP c.*84G>A variant doubles coronary artery disease risk in South Indian patients (PLoS One 2016)
- TA-8995 (obicetrapib) raises ABCA1-specific cholesterol efflux capacity by 28% and preBeta-1 HDL by 36%, showing functional as well as HDL-C gains (J Clin Lipidol 2016)
2015 79
- LC-MS/MS method quantifies anacetrapib, a stable-isotope tracer, and four metabolites in human plasma (J Chromatogr B 2016)
- White adipose tissue accumulates anacetrapib up to 40-fold, explaining its long elimination half-life in mice (Drug Metab Dispos 2016)
- Review asks whether anacetrapib is the last surviving CETP inhibitor as REVEAL results loom (Expert Opin Pharmacother 2016)
- Evacetrapib cuts small LDL particles by up to 95% and lipoprotein(a) by up to 40%, alone or added to statins (J Clin Lipidol 2016)
- Extended-release niacin/laropiprant abolishes the postprandial rise in CETP activity and boosts HDL's fecal cholesterol removal capacity (Arterioscler Thromb Vasc Biol 2015)
- Eight CETP gene polymorphisms show distinct HDL, LDL, and triglyceride associations in Kazak and Uyghur adults from Western China (Int J Environ Res Public Health 2015)
- A new non-steady-state tracer method shows anacetrapib blocks 97% of postprandial triglyceride flux into HDL (J Lipid Res 2016)
- Optimised benzylaminopropanamide derivative HL16 emerges as a sub-micromolar CETP inhibitor active in hamsters (Bioorg Med Chem 2015)
- Stable-isotope tracer study measures evacetrapib absolute oral bioavailability at 44.8% (J Labelled Comp Radiopharm 2016)
- Review previews two pending phase 3 trials that will decide the future of CETP inhibition (Curr Opin Lipidol 2015)
- CETP is among the genes most strongly linked to lipid change over time and incident hyperlipidemia in a large Chinese cohort study (Circ Cardiovasc Genet 2016)
- BMS-795311 matches torcetrapib for raising HDL in hamsters without raising blood pressure or aldosterone synthase (J Med Chem 2015)
- Evacetrapib raises ABCA1-specific cholesterol efflux capacity and pre-beta-1 HDL, effects that statins alone do not share (JACC 2015)
- Policosanol-loaded reconstituted HDL inhibits CETP activity by up to 47 percent and promotes tissue regeneration (Rejuvenation Res 2015)
- Contrary to expectation, higher plasma TMAO from L-carnitine correlates with smaller aortic lesions in CETP-expressing ApoE-deficient mice (Atherosclerosis 2015)
- Review argues CETP inhibitors remain the most potent HDL-raising agents but their cardiovascular benefit is still unproven (Clin Ther 2015)
- Evacetrapib inhibits every major CYP enzyme in vitro, but clinical drug-drug interactions turn out weak (Br J Clin Pharmacol 2015)
- Meta-analysis links CETP rs3764261 variant to higher age-related macular degeneration risk across ethnicities (Sci Rep 2015)
- CYP3A handles about 90% of the metabolic clearance of evacetrapib, but even strong CYP3A inhibitors barely raise its exposure (Pharmacol Res Perspect 2015)
- Resequencing the entire CETP gene uncovers rare variants that independently affect HDL cholesterol in both whites and African blacks (Metabolism 2016)
- ACCELERATE trial design targets 12,092 high-risk patients to test the effect of evacetrapib on cardiovascular outcomes (Am Heart J 2015)
- Niacin/laropiprant lowers CETP activity alongside multiple inflammatory markers but modestly improves HDL efflux without changing HDL antioxidant capacity (J Am Heart Assoc 2015)
- CETP variant rs708272 nearly doubles metabolic syndrome risk in women from southwestern Mexico (Int J Mol Sci 2015)
- A chiral HPLC method resolves the methyl ester of evacetrapib from its stereoisomers and five impurities (J Chromatogr A 2015)
- Anacetrapib lowers VLDL/LDL cholesterol through both CETP inhibition and a separate PCSK9-lowering mechanism in mice (J Lipid Res 2015)
- CETP variant rs5882 shows no association with LDL cholesterol lowering from plant sterols, unlike CYP7A1 and APOE variants (Am J Clin Nutr 2015)
- QSAR models guide design of twelve new diphenylpyridylethanamine CETP inhibitors (Bioorg Med Chem Lett 2015)
- Eliminating liver Kupffer cells abolishes hepatic CETP expression and lowers plasma CETP, identifying their cellular origin for this protein (Hepatology 2015)
- CETP variant rs3764261 raises HDL cholesterol but does not affect diabetes risk or recurrent cardiovascular events in vascular disease patients (Atherosclerosis 2015)
- CETP I405V II genotype linked to gray matter diffusion abnormalities in healthy older adults (J Neural Transm 2015)
- A review argues the failure of niacin to reduce cardiovascular events, alongside CETP inhibitor trial results, exposes the flaws of the HDL cholesterol hypothesis (Curr Atheroscler Rep 2015)
- CETP variant rs5882 determines whether plant sterol consumption lowers triglycerides, crossover trial finds (Appl Physiol Nutr Metab 2015)
- Two linked upstream CETP variants have opposite effects on gene expression via disrupted transcription factor binding sites (Pharmacogenet Genomics 2015)
- Review argues patient stratification, and caution in sepsis, are needed before CETP can succeed as a drug target (Expert Opin Ther Targets 2015)
- Novel CETP microdeletion lowers enzyme activity and raises HDL-associated cholesterol in three carriers (Clin Genet 2016)
- CETP-deficient cells cannot efficiently convert diglyceride into stored triglyceride (J Lipid Res 2015)
- High-pressure crystallization confirms a predicted, more stable polymorph of dalcetrapib before late-stage development (Nat Commun 2015)
- CETP variant rs708272 is one of three protective polymorphisms shielding HIV patients on antiretroviral therapy from atherogenic dyslipidemia (AIDS Res Hum Retroviruses 2015)
- Inhibiting CETP with des-fluoro-anacetrapib doubles capillary density in ischemic rabbit hindlimbs via SR-B1 and PI3K/Akt signaling (Int J Cardiol 2015)
- Brief review previews CETP inhibitor trial results as REVEAL data for anacetrapib approaches (Eur Cardiol 2015)
- In vivo, anacetrapib promotes rather than blocks cholesteryl ester flux into large HDL, contradicting in vitro homotypic-transfer predictions (Eur J Pharmacol 2015)
- TULIP: the original TA-8995 (obicetrapib) trial cuts LDL-C by up to 45.3% and raises HDL-C by up to 179% with no serious adverse events (Lancet 2015)
- CETP TaqIB polymorphism shows no link to metabolic syndrome in Southern Thai subjects (Biochem Genet 2015)
- Novel CETP inhibitor K-312 lowers PCSK9 through a CETP-independent SREBP mechanism (Am J Physiol Endocrinol Metab 2015)
- A review proposes that HDL regulates the beta2-adrenergic receptor pathway through the same ADCY9 signaling axis linked to dalcetrapib response (Arch Med Res 2015)
- Meta-analysis finds LDL-C and non-HDL-C, not HDL-C, predict lesion reduction across CETP-expressing animal and human trials (Eur J Pharmacol 2015)
- Anacetrapib lowers LDL-ApoB by accelerating its clearance, not by slowing its production (J Clin Invest 2015)
- Meta-analysis finds adding a CETP inhibitor to statin therapy does not reduce cardiovascular events (Int J Cardiol 2015)
- Topoisomerase II inhibitors etoposide and teniposide activate hepatic CETP expression via LXR and boost reverse cholesterol transport in CETP transgenic mice (J Biol Chem 2015)
- Flaxseed oil lowers small dense LDL alongside CETP and apoB concentrations after twelve weeks in Japanese men (Nutr J 2015)
- Modeling shows the short half-life of the CETP inhibitor RG7232 drives oscillating on/off effects on lipoprotein metabolism (CPT Pharmacometrics Syst Pharmacol 2015)
- CETP deficiency protects against fatal liver damage from schistosomiasis by starving parasite eggs of HDL cholesteryl ester (J Biomed Res 2015)
- Meta-regression of 167 311 patients finds raising HDL cholesterol with CETP inhibitors does not predict clinical benefit (Heart 2015)
- New diterpenes isolated from Engleromyces goetzii fungus show CETP inhibitory activity (Nat Prod Bioprospect 2015)
- Review proposes historic hepatic schistosomiasis as a screening factor behind East Asia's unusually high rate of genetic CETP deficiency (Nutrients 2015)
- The CETP B2 allele is linked to lower LDL cholesterol specifically in black, not white, South African women (Atherosclerosis 2015)
- Electron microscopy shows CETP binds HDL through hydrophobic surface interactions, not protein contacts (Sci Rep 2015)
- A high-fat breakfast raises steady-state evacetrapib exposure by 44%, with correspondingly larger lipid and CETP-activity changes (J Cardiovasc Pharmacol Ther 2015)
- REALIZE phase 3 trial: anacetrapib cuts LDL-C by 39·7% versus placebo in familial hypercholesterolaemia over one year (Lancet 2015)
- Modeling predicts a 550-day half-life for the tissue depot of anacetrapib, but no comparable accumulation for evacetrapib (J Clin Pharmacol 2015)
- Combined CETP B1 and eNOS 4a alleles raise coronary artery disease risk up to 34-fold in Malay and Indian, but not Chinese, ethnic groups (Clin Appl Thromb Hemost 2016)
- Simvastatin blunts the boost that dalcetrapib gives to cholesterol efflux from macrophages in vitro (Cardiovasc Drugs Ther 2015)
- Inhibiting CETP with des-fluoro-anacetrapib nearly doubles re-endothelialization after balloon injury in rabbit aortas (ATVB 2015)
- The Morton lab introduces substrate-preference modification as a new paradigm for engineering CETP-targeting drugs (J Lipid Res 2015)
- CETP inhibitors trigger aldosterone-producing enzymes in adipocytes through Nox-driven reactive oxygen species and STAT3 (J Pharmacol Exp Ther 2015)
- Overexpressing full-length CETP in fat cells cuts triglyceride accumulation in half by boosting turnover and blocking synthesis (J Lipid Res 2015)
- Discovery study links the ADCY9 rs1967309 polymorphism to a 39% cardiovascular benefit from dalcetrapib (Circ Cardiovasc Genet 2015)
- CETP variant rs5882 G allele is linked to lower HDL cholesterol in obese and non-obese individuals alike (Gene 2015)
- Mendelian randomization meta-analysis of 40,000 subjects finds lower circulating CETP causally reduces coronary heart disease risk (Circ Cardiovasc Genet 2015)
- Transgenic CETP expression nearly doubles run distance in obese female mice via increased muscle mitochondrial oxidative capacity and PGC-1alpha (PLoS One 2015)
- A review argues cholesterol efflux capacity, not HDL cholesterol, is the more meaningful marker after CETP inhibitor and niacin trials failed to reduce cardiovascular outcomes (Prog Cardiovasc Dis 2015)
- Atorvastatin fails to protect against atrial fibrillation in patients with the CETP TaqIB B2B2 genotype (J Atr Fibrillation 2015)
- Pioglitazone does not change CETP or improve peripheral vessel function in nondiabetic patients over nine months (Cardiology 2015)
- The CETP locus is one of only three individually significant lipid-associated SNPs confirmed in a first Algerian population genetics study (Int J Clin Exp Pathol 2015)
- CETP concentration is elevated and inversely correlates with hemoglobin in women with iron deficiency anaemia (Clin Lab 2015)
- Review highlights that CETP inhibitors lower blood glucose alongside raising HDL cholesterol (Front Pharmacol 2015)
- Handbook chapter surveys emerging HDL-targeted drugs, from CETP inhibitors to PPAR and LXR agonists (Handb Exp Pharmacol 2015)
- Systematic review tracks CETP inhibitors from the toxicity of torcetrapib to the greater potency and safety of anacetrapib and evacetrapib (Am J Ther 2015)
- Fine-mapping of the CETP region identifies five novel variants, including a common intronic insertion, linked to HDL-C (NPJ Aging Mech Dis 2015)
2014 81
- CETP -629C/A genotype predicts HDL-C but the CC genotype benefits most from atorvastatin's LDL-C-lowering effect in Chinese CHD patients (Med Sci Monit 2014)
- CETP genotype predicts who benefits most from a low-carbohydrate diet for raising HDL and lowering triglycerides, replicated across two randomized trials (J Lipid Res 2015)
- Niacin plus laropiprant, but not fenofibrate, significantly lowers CETP and LCAT activity in type 2 diabetic patients with low HDL (Atherosclerosis 2015)
- Plant-produced chimeric protein targeting ApoB100 and CETP epitopes elicits antibody responses in mice (Mol Biotechnol 2014)
- Atomistic simulations reveal how CETP penetrates HDL via a tryptophan anchor and phenylalanine barrier (J Lipid Res 2015)
- Elevated CETP activity during acute STEMI independently predicts endothelial dysfunction and 12.8-fold higher 30-day mortality risk (Atherosclerosis 2014)
- The LDL-C and HDL-C effects of anacetrapib were smaller in Black than White DEFINE trial patients (J Clin Lipidol 2015)
- Meta-analysis of over 17,000 subjects confirms CETP TaqIB B2B2 genotype protects against myocardial infarction (Medicine 2014)
- Review from the discoverer of CETP deficiency in Japan surveys anacetrapib and evacetrapib as candidate cures for atherogenic dyslipidemia (Mol Cells 2014)
- Atomistic simulations show anacetrapib lodges in the N-terminal tunnel of CETP to block cholesteryl ester diffusion (PLoS Comput Biol 2014)
- Review updates the pipeline of emerging hyperlipidaemia drugs, focused mainly on anacetrapib and evacetrapib (Expert Opin Emerg Drugs 2014)
- Less lipophilic hexahydrofuroquinoline CETP inhibitor clears fat tissue quickly and avoids off-target hypertension signals (J Med Chem 2014)
- Mendelian randomization using the CETP TaqIB polymorphism finds genetically raised HDL cholesterol does not translate into lower coronary disease risk (BMC Med Genet 2014)
- Cholesteryl ester diffusion and self-association within the HDL phospholipid bilayer set the pace of CETP-mediated lipid transfer (Arch Biochem Biophys 2014)
- Anacetrapib reshapes LDL particle subfractions differently than atorvastatin, and neither drug reduces the smallest LDL particles (J Clin Lipidol 2015)
- Dalcetrapib, but not anacetrapib, raises plasma and liver levels of the dietary antioxidants lutein and zeaxanthin (Lipids 2014)
- Dalcetrapib raises plasma campesterol only in patients with intact ABCA1 and ApoA1, a crossover trial finds (Lipids 2014)
- A review shows PON1 activation and its flux across HDL particle sizes during maturation are blocked by CETP and LCAT inhibitors (Clin Chim Acta 2015)
- Meta-analysis of 69,515 patients finds niacin and CETP inhibitors do not reduce cardiovascular mortality (Nutr Metab Cardiovasc Dis 2015)
- CETP variants A373P and Taq1 have opposite effects on low HDL cholesterol risk in Iranian children and teenagers (Atherosclerosis 2014)
- CETP TaqIB B2 homozygotes get the strongest heart-protective benefit from moderate alcohol intake, replicating a prior finding in men (Alcohol 2014)
- Computational mapping of CETP missense mutations identifies cholesterol-binding regions relevant to drug design (Arch Biochem Biophys 2014)
- Review argues HDL-raising therapy remains an unmet cardiovascular need after torcetrapib and dalcetrapib failures (Transl Med UniSa 2015)
- First-in-human data: TA-8995 (obicetrapib) blocks 92-99% of CETP activity and is well tolerated across 1 to 150mg doses (Br J Clin Pharmacol 2014)
- Cache County Study links CETP I405V valine allele to slower cognitive decline in 4,486 older adults (Neurobiol Aging 2015)
- Lipid-based drug delivery greatly improves oral exposure to two CETP inhibitors, torcetrapib and CP-532,623, in beagle dogs (Eur J Pharm Biopharm 2014)
- Increased fruit and vegetable intake lowers serum amyloid A and CETP activity in HDL subfractions across two randomized trials (Br J Nutr 2014)
- Ten CETP locus SNPs are among the strongest genetic determinants of HDL cholesterol variability in a Latvian population (Meta Gene 2014)
- Anacetrapib dose-dependently shrinks atherosclerotic lesions by up to 92% and adds to the benefit of atorvastatin (Eur Heart J 2015)
- Meta-analysis links the CETP rs5882 A allele to increased Alzheimer's disease risk in Caucasians (DNA Cell Biol 2014)
- New synthesis route scales a polycyclic CETP inhibitor to multikilogram quantities (Org Lett 2014)
- Review of hypertriglyceridemia drugs places CETP and ANGPTL3/4 inhibitors among agents enhancing triglyceride-rich lipoprotein clearance (Prog Lipid Res 2014)
- Review previews upcoming dyslipidaemia drugs, from CETP inhibitors to PCSK9 inhibitors and MTP inhibitors (J Cardiovasc Pharmacol Ther 2015)
- CETP G allele carriers show distinct waist circumference and metabolic profiles, independent of glucose and lipid changes (Diabetes Res Clin Pract 2014)
- CETP TaqIB B2 allele carriers have higher HDL cholesterol and antioxidant enzyme activity in both healthy and diabetic Argentinians (J Diabetes Investig 2015)
- BMJ meta-analysis of 117,411 patients finds niacin, fibrates, and CETP inhibitors do not reduce mortality on top of statins (BMJ 2014)
- CETP is one of five gene loci with pleiotropic effects across metabolic syndrome components in over 15,000 African Americans (Circ Cardiovasc Genet 2014)
- At matched CETP inhibition, only anacetrapib boosts macrophage-to-feces cholesterol excretion in dyslipidemic hamsters (Eur J Pharmacol 2014)
- CETP TaqIB B2B2 genotype is linked to more favorable HDL cholesterol levels in West Siberian Caucasians (Bull Exp Biol Med 2014)
- At the highest dose, evacetrapib inhibits CETP by 91% and raises HDL-C by 87% without moving 24-hour blood pressure (J Pharm Pharmacol 2014)
- Dalcetrapib is rapidly hydrolyzed to its active thiol and excreted largely unchanged in rats and monkeys (Xenobiotica 2014)
- Neither moderate hepatic nor severe renal impairment meaningfully alters anacetrapib pharmacokinetics (J Clin Pharmacol 2014)
- CETP inhibitors reduce hepatic LDL receptor and PCSK9 via an off-target SREBP2 mechanism (Atherosclerosis 2014)
- The CETP rs5882 variant predicts white matter microstructure, with opposite effects in young versus older adults (Neurobiol Aging 2014)
- CETP I405V Val/Val genotype significantly determines HDL cholesterol levels in myocardial infarction patients (J Clin Diagn Res 2014)
- Review questions where CETP inhibitors will fit clinically outside patients with very low HDL cholesterol (Expert Opin Investig Drugs 2014)
- Bone marrow-derived hepatic lipase mitigates the HDL-lowering effect of bone marrow-derived CETP in double-knockout mice (J Lipid Res 2014)
- Torcetrapib raises HDL cholesterol in primates without touching non-HDL cholesterol, distinguishing it from an FXR antagonist tested alongside it (Life Sci 2014)
- In rhesus macaques, anacetrapib reproduces the human lipid response and significantly lowers plasma PCSK9 (Eur J Pharmacol 2014)
- CETP and APOE variants interact to raise hypertriglyceridemia risk in oldest-old Chinese women (Exp Gerontol 2014)
- Two more years of anacetrapib in the DEFINE extension sustain a 39.9% LDL-C drop and 153.3% HDL-C rise with no new safety signals (J Cardiovasc Pharmacol Ther 2014)
- A review names failed CETP-inhibitor and niacin trials as key evidence complicating the HDL-cholesterol paradigm for cardiovascular prevention (Clin Pharmacol Ther 2014)
- Dose-ranging phase 2 trial in Japanese patients shows evacetrapib 500 mg raises HDL-C by 136% and cuts CETP activity by 95% (Am J Cardiol 2014)
- A brush-type Whelk-O 1 chiral column resolves evacetrapib from its enantiomer, two diastereomers, and six impurities (J Chromatogr A 2014)
- CETP activity is 30 percent higher in South Asians than Europeans and tracks the full pattern of atherogenic dyslipidemia (Eur J Prev Cardiol 2014)
- The dal-ACUTE trial finds dalcetrapib raises HDL cholesterol by a third after acute coronary syndrome but boosts cholesterol efflux by only a tenth (Eur Heart J 2014)
- Fibrates and fish oil, but not corn oil, activate PPAR-alpha to raise hepatic CETP expression and plasma activity in transgenic mice (J Nutr Biochem 2014)
- HDL from patients with CETP- or hepatic-lipase-deficiency hyperalphalipoproteinemia is not dysfunctional and shows enhanced cholesterol efflux from macrophages (Atherosclerosis 2014)
- Even at 8 times the therapeutic dose, anacetrapib does not clinically prolong the QTcF interval (J Clin Pharmacol 2014)
- Glycation destroys apolipoprotein C1's natural ability to inhibit CETP in patients with diabetes (Diabetes Care 2014)
- Very low plasma CETP is linked to impaired HDL cholesterol efflux in the LURIC cohort (Eur J Clin Invest 2014)
- CETP C-terminal peptides drive lipid particles from large aggregates into small micelle-like structures via disorder-to-order transitions, a proposed lipid-transfer mechanism (J Struct Biol 2014)
- CETP variant rs3764261 is linked to reduced risk of advanced age-related macular degeneration in a Chinese population (Ophthalmic Genet 2015)
- Torcetrapib cuts insulin levels by 49 percent and improves glucose uptake across tissues in insulin-resistant hamsters (Atherosclerosis 2014)
- Population PK/PD model finds evacetrapib exposure predicts up to a 177% HDL-C increase and 44.1% LDL-C decrease (CPT Pharmacometrics Syst Pharmacol 2014)
- Diphenylpyridylethanamine-based aminoheterocycles optimised as CETP inhibitors with better metabolic stability (Bioorg Med Chem Lett 2014)
- A single CETP gene variant, rs5883, is identified as the main driver of the exon-9-skipping splice form (Biochem Biophys Res Commun 2014)
- Review surveys HDL-targeted therapies as CETP inhibitor trials split between discontinuation and ongoing phase III testing (Circ Res 2014)
- Meta-analysis finds CETP TaqIB genotype raises Alzheimer's risk only in APOE4-positive Asians, with no overall population association (Neurobiol Aging 2014)
- A review names CETP mutations as a specific genetic cause of high HDL cholesterol, distinct from the mutations that cause low HDL (Curr Med Chem 2014)
- Meta-analysis of seven CETP variants finds rs708272 and rs1800775 are promising biomarkers for myocardial infarction risk (PLoS One 2014)
- CETP TaqIB B2B2 genotype raises atrial fibrillation risk, especially in postmenopausal women with higher triglycerides (J Atr Fibrillation 2014)
- CETP TaqIB mutation carriers with low HDL cholesterol have a fivefold higher risk of premature coronary artery disease in Egyptians (J Clin Lipidol 2014)
- Amino-acid-modified fungal pigment derivatives yield micromolar, non-competitive CETP inhibitors (Nat Prod Res 2014)
- HDL from genetically CETP-deficient carriers is worse at activating eNOS, despite normal cholesterol-efflux capacity (PLoS One 2014)
- Provocative 2014 opinion piece argues the evidence had turned against CETP inhibition and calls for an urgent trial review (F1000Res 2014)
- CETP deficiency linked to cardiovascular disease and stroke within a high-HDL syndrome, especially in women (Mol Genet Metab Rep 2014)
- A review argues the torcetrapib setback shifted focus from HDL cholesterol quantity to HDL particle functionality (Am J Ther 2014)
- Unlike torcetrapib, anacetrapib raises HDL-C by 138% without elevating blood pressure or disturbing electrolytes (Cardiol Rev 2014)
- Review asks whether anacetrapib and evacetrapib can succeed where torcetrapib and dalcetrapib failed to reduce cardiovascular risk (Annu Rev Med 2014)
- Anti-CETP vaccine reduces atherosclerosis and fatty liver disease in cholesterol-fed rabbits (PLoS One 2014)
2013 64
- Novel non-THQ torcetrapib analog PF-04445597 avoids the aldosterone-inducing effect linked to torcetrapib toxicity (Xenobiotica 2014)
- The original discovery that hamster CETP uniquely drives one-way lipid flow from VLDL to HDL reveals CETP orthologs are not functionally equivalent across species (J Lipid Res 2014)
- Review argues CETP inhibitor failures show over-reliance on HDL cholesterol as an efficacy marker (Clin Lipidol 2013)
- Review names CETP inhibition among the most promising pharmacological approaches to raising HDL despite recent trial failures (Curr Opin Lipidol 2013)
- CETP variant rs708272 lowers coronary atherosclerosis risk while a linked variant shapes HDL cholesterol in Chinese healthy controls (Lipids Health Dis 2013)
- A thorough QT study finds evacetrapib safe on cardiac rhythm even at 5-fold the exposure planned for phase 3 (J Cardiovasc Pharmacol Ther 2014)
- CETP gene promoter variants show no association with longevity in two Han Chinese samples (Mol Biol Rep 2013)
- A review names CETP inhibition among three specific pharmacological strategies to boost reverse cholesterol transport (Indian J Exp Biol 2013)
- The CETP rs1532624 AA genotype has lower CETP activity, higher HDL-C, but a weaker LDL-C response to statins in Jordanian patients (Curr Mol Pharmacol 2013)
- CETP Taq1B B1/B1 genotype predicts a favorable triglyceride/HDL-C response to kiwifruit in hypercholesterolaemic men (Br J Nutr 2013)
- LCAT and CETP activity track with disturbed HDL and triglyceride-rich lipoprotein composition after kidney transplant (Cell Biochem Biophys 2013)
- Inhibiting secretory phospholipase A2 raises CETP activity via VLDL-apoE content, offsetting its antiatherosclerotic benefit in triple-transgenic mice (Arterioscler Thromb Vasc Biol 2013)
- 10-Dehydrogingerdione raises HDL cholesterol by suppressing CETP and curbs oxidative and inflammatory markers in rabbits (Atherosclerosis 2013)
- CETP B1B1 genotype tracks with lower HDL cholesterol from birth through age 5-6 in children at cardiovascular risk (Med Sci Monit 2013)
- Anacetrapib lipid effects and detectable plasma drug persist for years after stopping treatment (Am J Cardiol 2014)
- CETP enhancer variant rs3764261 boosts statin-associated HDL-C rise but reduces statin protection against myocardial infarction (Clin Pharmacol Ther 2013)
- Perspective reviews the discovery and development of CETP inhibitors for reducing residual cardiovascular risk (J Med Chem 2014)
- A Filipino GWAS finds suggestive CETP and TOM1 associations with HDL cholesterol and allelic heterogeneity at the CETP locus (J Lipid Res 2013)
- CETP variant rs3764261 raises the risk of polypoidal choroidal vasculopathy in a Japanese population (Invest Ophthalmol Vis Sci 2013)
- Review asks why targeting HDL for cardiovascular protection has not delivered clinical benefit (J Cardiovasc Pharmacol 2013)
- CETP variant rs708272 associates with HDL-C and LDL-C levels in 365 Turkish children (OMICS 2013)
- Validated comparative QSAR modelling of 104 CETP inhibitors identifies key structural drivers of potency (Comput Biol Med 2013)
- Perspective argues HDL functionality, not HDL-C concentration, should guide the future evaluation of CETP inhibitors (Clin Pharmacokinet 2013)
- In hamsters, anacetrapib raises preβ HDL and reverse cholesterol transport without affecting cholesterol absorption, unlike dalcetrapib (J Lipid Res 2013)
- CETP genetic variants do not predict recurrent heart attacks in secondary prevention patients, but may raise mortality after bypass surgery (Am J Cardiol 2013)
- Cysteine 13 of CETP is the key residue that lets dalcetrapib decouple cholesteryl ester transfer from HDL remodeling (Biochim Biophys Acta 2013)
- Isotope-labeled anacetrapib and its metabolites are synthesized to support bioavailability and drug-metabolism studies (J Labelled Comp Radiopharm 2013)
- CETP I405V polymorphism is an independent risk factor for endometriosis in a case-control study of women (Gynecol Endocrinol 2013)
- Review narrates the CETP inhibitor class from the mortality excess of torcetrapib to the still-pending REVEAL and ACCELERATE trials (Curr Opin Cardiol 2013)
- Antisense CETP inhibition, unlike anacetrapib, boosts macrophage reverse cholesterol transport in CETP-transgenic mice (J Lipid Res 2013)
- A stroke-prevention review flags CETP inhibitor trial success as a potential turning point for dyslipidemia treatment (Maturitas 2013)
- Absence of the CETP B2 allele doubles coronary artery disease risk, but only in ethnic Chinese Singaporeans (Lipids Health Dis 2013)
- Ten-arm dose-ranging trial in Japanese patients shows anacetrapib raises HDL-C up to 159% and adds to the LDL-lowering of atorvastatin (Atherosclerosis 2013)
- Schaefer argues CETP inhibitors fail to cut coronary risk because they disrupt normal HDL metabolism (Curr Opin Lipidol 2013)
- CETP inhibition boosts postprandial insulin secretion via enhanced cholesterol efflux from beta cells (Circ Res 2013)
- CETP activity and mass are lower in rheumatoid arthritis patients taking glucocorticoids (J Rheumatol 2013)
- Chronic rifampin dosing slashes anacetrapib exposure by 65% through CYP3A induction, while a single dose barely moves it (J Clin Pharmacol 2013)
- Two CETP variants are among only eight significant HDL predictors identified across 65 SNPs and 23 candidate genes (Lipids Health Dis 2013)
- Review collates the bioanalytical methods developed to quantify anacetrapib, dalcetrapib, and torcetrapib in biological samples (Biomed Chromatogr 2013)
- Dietary cholesterol dose-dependently drives osteoarthritis in CETP-humanised mice, and atorvastatin but not ezetimibe suppresses it despite similar cholesterol lowering (Ann Rheum Dis 2013)
- Bile-acid-activated farnesoid X receptor identified as a novel driver of CETP expression, explaining low HDL-C in cholestasis (J Lipid Res 2013)
- HIV infection is associated with elevated plasma CETP and LCAT alongside low HDL, without one-year progression of subclinical atherosclerosis (Atherosclerosis 2013)
- CETP gene promoter methylation correlates with LDL-C, HDL-C, and HDL particle size in familial hypercholesterolaemia patients (Atherosclerosis 2013)
- Low-normal thyroid function raises plasma cholesteryl ester transfer in type 2 diabetes (Atherosclerosis 2013)
- Hepatic and renal impairment increase dalcetrapib active-thiol exposure by up to 81% (Clin Pharmacokinet 2013)
- Specific lysophospholipid micelles reverse the beta-sheet, amyloid-fibril-forming conformation of a CETP C-terminus D470N mutant peptide back to alpha-helix (Biochem Biophys Res Commun 2013)
- HDL3 reduces macrophage ER stress and partially restores apoE and CETP secretion suppressed by tunicamycin (Biochem Biophys Res Commun 2013)
- HIV/HAART patients show a blunted triglyceride-HDL cholesterol relationship driven by higher CETP mass but lower CETP-specific activity, not altered total CETP activity (Metabolism 2013)
- A CETP variant is among four SNPs significantly linked to plasma cholesterol, though only APOB and NPC1L1 show novel diet-gene interactions (J Lipid Res 2013)
- Probenecid raises exposure to the active thiol form of dalcetrapib by up to 21 percent (Int J Clin Pharmacol Ther 2013)
- In the Framingham Heart Study, low CETP or high PLTP activity predicts more than double the cardiovascular risk in men but not women (Atherosclerosis 2013)
- CETP genotype frequencies do not differ between centenarians, nonagenarians, and average-lifespan controls (Angiology 2013)
- CETP variant rs17231506 is one of five genes shaping sex-specific cholesterol efflux capacity independent of HDL-C (Arterioscler Thromb Vasc Biol 2013)
- Endogenous CETP activity above 34% marks high cardiovascular risk in a cohort of 1,403 patients (Atherosclerosis 2013)
- Fenofibrate and extended-release niacin raise HDL cholesterol equally but reshape HDL particle size differently, without improving cholesterol efflux (J Clin Lipidol 2013)
- CETP is the single most common genetic factor influencing HDL cholesterol in the Latvian population, ten-SNP association study finds (PLoS One 2013)
- Review notes CETP inhibitors raise HDL-C by 31-138 percent, but whether this lowers coronary risk remains unresolved (Circ J 2013)
- CETP transgene protects obese female mice from insulin resistance via bile acid signalling (Mol Metab 2013)
- CETP I405V reverses direction: protective for longevity in Ashkenazi Jews but a risk allele in Chinese (PLoS One 2013)
- Broad review on residual cardiovascular risk after statins notes anacetrapib and evacetrapib survive where two other CETP compounds failed (Vasc Health Risk Manag 2013)
- Vitamin E tocotrienol supplementation lowered CETP activity and improved lipids in chronic hemodialysis patients (Vasc Health Risk Manag 2013)
- Review tallies the HDL-C and LDL-C effects of each CETP inhibitor ahead of anacetrapib and evacetrapib outcomes in 2017 (Curr Pharm Des 2013)
- Meta-analysis of 12 trials finds CETP inhibitors raise HDL-c by 20.5 mg/dL and lower LDL-c by 17.1 mg/dL, with a blood-pressure signal from torcetrapib (PLoS One 2013)
- CETP rs3764261 T allele is the top single-locus HDL-C predictor among 13 SNPs in a 3,050-person Japanese cohort (PLoS One 2013)
2012 88
- Anacetrapib-raised HDL retains its anti-inflammatory effect on endothelial cells (Biochim Biophys Acta 2013)
- Baseline CETP activity nearly doubles in carriers of the eNOS T-786C polymorphism, atorvastatin crossover study finds (Arq Bras Cardiol 2013)
- Network pharmacology points to PDGFR, HGFR, and IL-2 receptor as possible off-target drivers of the cardiovascular harm from torcetrapib (BMC Syst Biol 2012)
- Novel CETP promoter variants found in hyperalphalipoproteinemia patients sharply cut gene transcriptional activity (Clin Chim Acta 2013)
- Unlike torcetrapib, dalcetrapib, evacetrapib, and anacetrapib do not raise blood pressure or aldosterone (Curr Opin Lipidol 2012)
- CETP TaqIB genotype raises HDL cholesterol but does not predict Alzheimer's disease risk in a Han Chinese cohort (Lipids Health Dis 2012)
- The Friedewald formula underestimates LDL-C by 12 mg/dl after anacetrapib treatment, likely from VLDL-C overestimation (J Lipid Res 2013)
- Molecular dynamics simulation reveals CETP forms a more flexible structure in solution than in the crystal, supporting a continuous internal tunnel (Proteins 2012)
- CETP inhibition alone fails to boost reverse cholesterol transport in hamsters unless paired with the LDL-lowering drug berberine (Arterioscler Thromb Vasc Biol 2013)
- Meta-analysis of over 15,000 subjects finds the CETP TaqIB B1 allele raises coronary artery disease risk specifically in Han Chinese (Mol Biol Rep 2013)
- Dalcetrapib raised HDL-C by up to 40% but did not reduce cardiovascular events in dal-OUTCOMES (N Engl J Med 2012)
- The CETP locus reaches genome-wide significance for baseline Lp-PLA2 mass in a JUPITER-trial GWAS of 6,851 statin-treated participants (Circ Cardiovasc Genet 2012)
- Review surveys torcetrapib, dalcetrapib, anacetrapib, and evacetrapib as HDL-raising targets after the mortality signal in ILLUMINATE (Curr Vasc Pharmacol 2012)
- A 34-year genetic study finds CETP-lowering variants cut ischemic heart disease risk by 24 percent with no adverse effects seen with torcetrapib (J Am Coll Cardiol 2012)
- CETP I405V and Taq1B polymorphisms show inconsistent links to subclinical carotid atherosclerosis in Brazilians (Lipids Health Dis 2012)
- Higher CETP mass independently predicts a lower leukocyte count, and switching atorvastatin to pitavastatin raises CETP mass by 8.8 percent (Am J Cardiovasc Drugs 2012)
- The weight-loss drug orlistat cuts exposure to active dalcetrapib by more than half by blocking its ester hydrolysis (J Cardiovasc Pharmacol 2012)
- CETP I405V is linked to lower small dense LDL levels, unrelated to coronary artery disease risk, in Indian subjects (Indian J Clin Biochem 2012)
- CETP B1 allele combined with an eNOS variant raises coronary artery disease risk 18-fold in Western Iranians (Hum Genomics 2012)
- Crystal structures show torcetrapib and a second inhibitor block the lipid-transfer tunnel of CETP at its narrow neck (J Biol Chem 2012)
- The excess mortality and cardiovascular harm of torcetrapib were confined to the low-dose atorvastatin subgroup in ILLUMINATE (J Lipid Res 2012)
- Two linked CETP SNPs more than double the odds of fatty liver in adolescent girls, independent of adiposity (J Gastroenterol Hepatol 2012)
- CETP R451Q raises coronary stenosis risk while Taq1B B2 lowers it in a Tunisian angiography cohort (J Cardiovasc Med (Hagerstown) 2012)
- Higher endogenous CETP activity boosts cholesterol efflux capacity via pre-beta1-HDL in women (Arterioscler Thromb Vasc Biol 2012)
- Fluorinated diphenylpyridylethanamine derivatives balance metabolic stability and CETP potency (Bioorg Med Chem Lett 2012)
- Dalcetrapib is hydrolyzed within 20 seconds in human intestinal fluid, but is stable in gastric fluid at low pH (Int J Pharm 2012)
- Baseline plasma CETP activity is elevated in dyslipidaemic patients and correlates with triglycerides (Int J Clin Pharmacol Ther 2012)
- Review tallies CETP inhibitor trial results from the 2006 failure of torcetrapib to the early promise of evacetrapib (Curr Opin Lipidol 2012)
- Review weighs whether CETP inhibition can rescue the HDL-raising hypothesis after AIM-HIGH, HERS, ILLUMINATE, and dal-OUTCOMES (Curr Treat Options Cardiovasc Med 2012)
- DEFINE trial found anacetrapib safe through 76 weeks with no signal for the 25% event excess seen with a prior CETP inhibitor (Expert Rev Cardiovasc Ther 2012)
- CETP variant rs5882 is one of only four significant SNP predictors of plasma homocysteine among 64 tested in healthy adults (J Nutr 2012)
- A 12-week lycopene trial lowers serum CETP activity and boosts LCAT and paraoxonase-1 activity in overweight middle-aged adults (J Nutr Biochem 2013)
- A distinct HDL-like particle seen in complete genetic CETP deficiency is absent in dalcetrapib-treated volunteers (Curr Vasc Pharmacol 2012)
- Anacetrapib has no clinically meaningful interaction with warfarin, sparing patients a dosage adjustment (Br J Clin Pharmacol 2012)
- Update captures dal-OUTCOMES futility and the decision by Roche to end the dalcetrapib program in May 2012 (Future Cardiol 2012)
- Niacin lowers plasma CETP mass 30% by reducing liver macrophage content, not by directly suppressing macrophage CETP expression (Biochem Pharmacol 2012)
- Review details the mode of action and clinical profile of dalcetrapib as dal-OUTCOMES interim results end its development (Expert Opin Investig Drugs 2012)
- CETP -629 AA genotype is enriched in metabolic syndrome patients and linked to lower CETP but higher LDL-C and total cholesterol (Mol Biol Rep 2012)
- Optimised DPPE-derivative CETP inhibitor shows robust efficacy without raising blood pressure in telemetered rats (J Med Chem 2012)
- A landmark review proposes the first comprehensive step-by-step molecular model of CETP action: sensing, penetration, docking, ternary complex, transfer, dissociation (J Lipid Res 2012)
- Review profiles the early safety advantage of evacetrapib over torcetrapib as cardiovascular outcomes remain unknown (Curr Cardiol Rep 2012)
- Common CETP genetic variants do not alter how well the apoB/apoA-I ratio predicts first major cardiovascular events compared with TC/HDL-C (J Clin Lipidol 2012)
- Barter and Rye review the CETP inhibition hypothesis after the harm caused by torcetrapib and the futility of dalcetrapib (J Lipid Res 2012)
- CETP and ABCA1 genotype together determine whether atorvastatin or simvastatin gives a better lipid response (Angiology 2012)
- Quinoline-3-carboxamide derivatives reach 80.1 percent CETP inhibitory activity in newly designed series (Molecules 2012)
- Annual exercise-genomics review highlights physical activity modifying how CETP and two other genes affect HDL cholesterol (Med Sci Sports Exerc 2012)
- Meta-analysis confirms CETP TaqIB polymorphism is linked to coronary artery disease in Chinese patients (J Zhejiang Univ Sci B 2012)
- Review distills lessons from the torcetrapib failure for the CETP inhibitors that followed it into clinical development (Curr Clin Pharmacol 2012)
- New tetrazolyl tetrahydroquinoline CETP inhibitors raise HDL cholesterol in a transgenic mouse model (Bioorg Med Chem Lett 2012)
- LC-MS/MS method quantifies dalcetrapib-thiol and its S-methyl and S-glucuronide metabolites down to 5 ng/mL (J Pharm Biomed Anal 2012)
- ApoC1's natural inhibition of plasma CETP is blunted in dyslipidaemic coronary artery disease patients (J Lipid Res 2012)
- Torcetrapib cuts apoB-48 production by nearly half, but the effect vanishes in patients already on atorvastatin (J Lipid Res 2012)
- Torcetrapib raises blood pressure across four independent cardiovascular models, validating them as predictive lead-optimization tools (J Cardiovasc Pharmacol 2012)
- Dalcetrapib does not affect the pharmacokinetics of a combined oral contraceptive in a crossover trial (Int J Clin Pharmacol Ther 2012)
- Resequencing finds rare CETP mutations and a common variant far more often in Thai patients with very high HDL cholesterol (Am J Cardiol 2012)
- CETP I405V valine homozygosity is linked to better cognitive function after age 65 (Neurobiol Aging 2012)
- Tetrahydronaphthyridine CETP inhibitors reach nanomolar potency and raise HDL-C in transgenic mice (Bioorg Med Chem Lett 2012)
- Knocking down hepatic SR-BI raises CETP-mediated cholesteryl ester transfer from HDL to apoB lipoproteins and halves atherosclerotic lesion area in rabbits (Atherosclerosis 2012)
- Xanthohumol from hops shows the strongest CETP-inhibitory activity among screened plant chalcones (Food Chem 2012)
- Review argues the off-target harm of torcetrapib is not a class effect shared by dalcetrapib, anacetrapib, and evacetrapib (Drugs 2012)
- CETP polymorphisms are linked to brain structure and Alzheimer's risk in an APOE-dependent manner (Brain Imaging Behav 2012)
- Adding dalcetrapib to pravastatin reshapes HDL composition and boosts two cholesterol efflux pathways in a phase IIb dose-ranging study (Am Heart J 2012)
- Structural study proposes a tunnel-bridging mechanism for how CETP transfers cholesteryl ester between HDL and LDL (Nat Chem Biol 2012)
- Non-HDL-C and insulin resistance predict high CETP activity in patients at risk for type 2 diabetes (Clin Biochem 2012)
- Dal-VESSEL trial finds dalcetrapib cut CETP activity 56% without harming endothelial function or blood pressure (Eur Heart J 2012)
- CETP TaqIB genotype tracks with HDL-C differently in long-lived versus younger Chinese Bama Zhuang adults (Lipids Health Dis 2012)
- LDL apheresis transiently reduces CETP-mediated cholesteryl ester transfer and cholesterol efflux capacity in familial hypercholesterolemia (J Lipid Res 2012)
- Modeling predicts an effective human dose for the CETP inhibitor BAY 60-5521, later confirmed in a first-in-man study (Br J Clin Pharmacol 2012)
- First-in-human single dose study of the CETP inhibitor BAY 60-5521 shows dose-dependent CETP inhibition and HDL rise (Br J Clin Pharmacol 2012)
- Schwartz reviews conflicting CETP genetic and animal evidence ahead of the anacetrapib and dalcetrapib outcomes trials (Curr Atheroscler Rep 2012)
- Low CETP activity more than doubles coronary artery disease risk in an Asian Indian diabetic cohort (Pharmacogenet Genomics 2012)
- CETP-driven cholesteryl ester enrichment of apoB particles is exaggerated in type 1 diabetes (Eur J Clin Invest 2012)
- Liver tumors seen in a 2-year mouse study of dalcetrapib trace to a rodent-specific pathway not relevant to humans (Toxicol Appl Pharmacol 2012)
- A Nature Reviews Endocrinology paper argues HDL actively regulates glucose metabolism, positioning CETP inhibitors for rapid clinical translation to diabetes (Nat Rev Endocrinol 2012)
- CETP variant rs9923854 enriched in the oldest-old across Danish and German cohorts (Age (Dordr) 2012)
- CETP inhibition boosts the cholesterol-removing power of large HDL2b particles after a meal, but not their delivery to the liver (Atherosclerosis 2012)
- Molecular dynamics simulations reveal helix X of CETP as a lid gating lipid exchange with HDL (PLoS Comput Biol 2012)
- CETP is the least frequently mutated of three genes (LIPG, CETP, GALNT2) found in Caucasian families with extremely high HDL cholesterol (PLoS One 2012)
- Two CETP splice-affecting variants raise mortality and heart attack risk specifically in men, mechanism traced to liver mRNA splicing (PLoS One 2012)
- Ezetimibe lowers CETP mass by 20 percent in most type 2 diabetes patients, tracking with HDL subclass shifts (Endocr J 2012)
- Heterozygous CETP-deficient HDL is remodeled toward more cholesteryl ester and less triglyceride but keeps normal antioxidative capacity (PLoS One 2012)
- Hop-derived xanthohumol prevents atherosclerosis in CETP-transgenic mice by inhibiting CETP and enriching HDL with apoE (PLoS One 2012)
- A review of biomarker and imaging trials shows the favorable lipid effects of torcetrapib failed to predict a 58 percent rise in mortality (Can J Cardiol 2012)
- GWAS replication confirms CETP rs3764261 association with HDL-C in a 3,781-person Asian Indian cohort (PLoS One 2012)
- Chinese medicine preparation SUB885C cuts CETP activity 74% and raises HDL-C in ApoE*3Leiden.CETP mice (PLoS One 2012)
- Review compiles dal-VESSEL, dal-PLAQUE, and DEFINE lipid results ahead of dal-OUTCOMES and REVEAL in 2013 and 2017 (Vasc Health Risk Manag 2012)
- Review focuses on anacetrapib as the CETP inhibitor without the mortality signal of torcetrapib (Vasc Health Risk Manag 2012)
- Review recounts the termination of dalcetrapib and the broader questions it raises for CETP inhibition and the HDL hypothesis (Drug Des Devel Ther 2012)
2011 81
- Women with angina pectoris show enhanced CETP activity in both HDL and LDL alongside impaired HDL antioxidant enzymes (Int J Mol Med 2011)
- Contradicting earlier reports, the CETP I405V polymorphism is linked to faster cognitive decline and higher Alzheimer's risk in a large US cohort (Aging Cell 2012)
- Review positions anacetrapib as free of the off-target toxicity of torcetrapib, with phase III trial results still awaited (Expert Opin Investig Drugs 2012)
- Anacetrapib shrinks medium and small LDL while paradoxically raising the smallest, densest LDL4b subfraction (J Lipid Res 2012)
- NMR fine-mapping finds CETP among only four loci linked to bulk serum lipids, versus eight linked to lipoprotein subfractions (Hum Mol Genet 2012)
- A review questions whether CETP inhibition can reduce cardiovascular events given the complex link between CETP loss-of-function and coronary risk (Curr Cardiol Rep 2011)
- Torcetrapib boosts reverse cholesterol transport by 118 percent in obese, insulin-resistant transgenic mice (Clin Transl Sci 2011)
- Anacetrapib does not meaningfully inhibit P-glycoprotein, leaving digoxin exposure essentially unchanged (Biopharm Drug Dispos 2011)
- Review by the developers of anacetrapib frames CETP inhibition as a new approach to cutting cardiovascular risk (Clin Pharmacol Ther 2012)
- Dalcetrapib cut CETP activity up to 58% and raised HDL-C up to 34% regardless of diabetes or metabolic syndrome status (Diabetes Obes Metab 2012)
- Three novel CETP gene mutations identified in Japanese patients with hyperalphalipoproteinemia (Clin Chim Acta 2012)
- Evacetrapib raised HDL-C up to 129% and lowered LDL-C up to 36% alone or with statins in a 398-patient dose-ranging trial (JAMA 2011)
- SAR study on the central phenyl ring of biphenyl oxazolidinone CETP inhibitors finds analogs matching anacetrapib in potency (Bioorg Med Chem Lett 2012)
- Barter and Rye ask where CETP inhibition stands after the off-target failure of torcetrapib (Trends Pharmacol Sci 2011)
- Review calls anacetrapib a new weapon against dyslipidemia, pending long-term mortality data (Curr Clin Pharmacol 2011)
- ApoA-I stimulates CETP and apoE secretion from lipid-loaded macrophages via NF-kB inhibition and PKA activation (Biochem Biophys Res Commun 2011)
- CETP is one of only two loci genome-wide-significantly associated with Lp-PLA2 mass in a five-study CHARGE Consortium meta-analysis (Eur Heart J 2011)
- A 16-week very-low-calorie diet in obese type 2 diabetics cuts plasma CETP by 18% and raises apoA-I by 16%, without improving HDL cholesterol efflux (Diabetes Care 2011)
- A new reverse-phase-array lipoprotein-profiling method shows dalcetrapib, unlike torcetrapib and anacetrapib, spares pre-beta HDL formation (J Lipid Res 2011)
- Sirtori weighs the cancer and sepsis signals of torcetrapib against the dramatic 139% HDL rise seen with anacetrapib (Expert Opin Investig Drugs 2011)
- Review explains why CETP inhibition raises HDL2 cholesterol without necessarily improving reverse cholesterol transport (Biochim Biophys Acta 2011)
- Discovery paper introduces evacetrapib, a potent CETP inhibitor that raises HDL cholesterol without inducing aldosterone or raising blood pressure (J Lipid Res 2011)
- Chemical remodeling of LDL, not release from its inactive complex, drives LTIP activation, requiring either LCAT or CETP activity (J Lipid Res 2011)
- Unlike torcetrapib, dalcetrapib shifts cholesterol homeostasis toward absorption markers rather than synthesis markers (Atherosclerosis 2011)
- Torcetrapib impairs endothelial function and raises vascular oxidative stress in hypertensive rats, reversed by endothelin blockade (Eur Heart J 2012)
- The dal-PLAQUE imaging trial finds no evidence dalcetrapib harms the arterial wall after the failure of torcetrapib (Lancet 2011)
- CETP TaqIB polymorphism flags high coronary risk but cannot distinguish left main from more peripheral disease (Lipids Health Dis 2011)
- Unlike LCAT or ABCA1 mutations, heterozygous CETP mutations leave plasma sphingosine-1-phosphate and apoM levels unaffected (Atherosclerosis 2011)
- Eight weeks after stopping anacetrapib, HDL-C remains up to 43.4% higher, tracking residual drug levels and CETP inhibition (Am Heart J 2011)
- Anacetrapib inhibited CETP 94% and boosted macrophage-to-feces cholesterol excretion in hamsters (J Lipid Res 2011)
- Saccharin-fed zebrafish show elevated CETP activity while aspartame-fed zebrafish suffer acute deaths under high-cholesterol diet (Food Chem Toxicol 2011)
- PPAR-delta agonist GW501516 lowers CETP activity alongside broad apoB and apoC-III kinetic changes in obese dyslipidemic men (J Clin Endocrinol Metab 2011)
- CETP actually boosts the ability of HDL to block LDL oxidation, a finding that may help explain why torcetrapib failed to slow vascular disease (IUBMB Life 2011)
- High CETP is an independent negative determinant of LDL size and tracks with CAD prevalence in haemodialysis patients (Nephrology (Carlton) 2011)
- CETP concentration is higher in coronary heart disease patients but is not itself an independent predictor of LDL particle size (Bosn J Basic Med Sci 2011)
- Review synthesises structural and biophysical evidence for how CETP moves lipids between HDL and LDL (Biochem Soc Trans 2011)
- The dal-PLAQUE study is designed to track dalcetrapib effects on carotid plaque burden and inflammation with MRI and PET/CT (Am Heart J 2011)
- Review distinguishes CETP inhibitors from the CETP modulator dalcetrapib by their opposite effects on HDL2-to-HDL3 transfer (Curr Opin Lipidol 2011)
- CETP enhances insulin-stimulated glucose uptake in human adipocyte cells (Life Sci 2011)
- Leoligin, a lignan from Edelweiss, is identified as a novel CETP activator (Atherosclerosis 2011)
- Torcetrapib improved glycemic control in 6,661 diabetic ILLUMINATE participants despite the overall harm of the trial (Circulation 2011)
- Systematic review confirms the CETP Taq-1B minor allele is protective against metabolic syndrome, among only eight genetic associations that hold up (Obes Rev 2011)
- CETP B1 allele raises coronary artery disease and diabetes risk independent of HDL-C in western Iran (Genet Test Mol Biomarkers 2011)
- Medicinal chemistry paper describes the structure-activity work that led to the discovery of anacetrapib (J Med Chem 2011)
- Large AMD meta-analysis discovers two new genetic loci and confirms CETP among ten previously known susceptibility genes (Hum Mol Genet 2011)
- The PAGE study fails to replicate CETP rs1864163's HDL-C association across roughly 38,000 diverse-ancestry adults despite adequate power (PLoS Genet 2011)
- A high-fat meal raises exposure to dalcetrapib by up to 44 percent across three phase I crossover studies (Clin Ther 2011)
- CETP deficiency, not high CETP activity, impairs postprandial lipemia clearance and correlates with carotid atherosclerosis in women (Lipids Health Dis 2011)
- CETP protects against the rise in VLDL caused by reconstituted HDL infusion, resolving a mouse-versus-human discrepancy (J Lipid Res 2011)
- Review names CETP as one of only two candidate genes for lipid response to exercise training, despite roughly 100 inconsistent studies (J Appl Physiol 2011)
- Natural compound isolated from ginger rhizome inhibits CETP with an IC50 of 35 micromolar (Arch Pharm Res 2011)
- Framingham study finds plasma CETP activity has only minimal association with blood pressure change over time (J Hypertens 2011)
- Familial hypercholesterolemia patients show elevated CETP-mediated cholesteryl ester transfer and defective reverse cholesterol transport (Arterioscler Thromb Vasc Biol 2011)
- Aerobic exercise boosts macrophage-to-feces reverse cholesterol transport in CETP-transgenic mice without changing CETP activity (Lipids 2011)
- Tree shrew CETP structure-function mapping identifies Asn110 as essential for secretion and residues 344/452 as essential for cholesteryl ester transfer (Lipids 2011)
- Combining CETP B2B2 with an ABCA1 variant produces the largest HDL cholesterol gap seen in a Chinese cohort of nearly 1 mmol/L (Acta Cardiol 2011)
- Review surveys the controversial CETP-atherosclerosis relationship and emerging roles in Alzheimer's disease, inflammation and obesity (IUBMB Life 2011)
- Plasma cholesteryl ester transfer activity, not CETP mass, predicts incident cardiovascular disease in a nested case-control study (Atherosclerosis 2011)
- New biphenyl oxazolidinone CETP inhibitor scaffold reaches sub-100 nanomolar potency (ACS Med Chem Lett 2011)
- CETP expression partly rescues abnormal HDL distribution but not atherosclerosis in SR-BI-deficient mice (J Biol Chem 2011)
- CETP and hepatic lipase gene variants interact to raise carotid atherosclerosis risk in 1,549-person SAPHIR cohort (Atherosclerosis 2011)
- A novel CETP promoter deletion causing CETP deficiency does not impair HDL function in reverse cholesterol transport (Atherosclerosis 2011)
- Intestinal and hepatic first-pass metabolism strips more than 90 percent of active dalcetrapib-thiol in monkeys (Xenobiotica 2011)
- Oxazolidinone-substituted benzoxazole CETP inhibitors raise HDL cholesterol up to 33 mg/dl in mice while avoiding hERG channel binding (Bioorg Med Chem Lett 2011)
- Population PK/PD modeling picks the 100 mg tablet dose for anacetrapib phase III without a dedicated phase IIb trial to test it (AAPS J 2011)
- Dense candidate-gene genotyping confirms CETP among established HDL-C loci in a 7,857-person meta-analysis and reveals multiple independent signals at several loci (Circ Cardiovasc Genet 2011)
- A hidden solvent impurity turns out to enable a scalable, chromatography-free synthesis of the anacetrapib biaryl core (J Org Chem 2011)
- AHA 2010 trials update reports DEFINE found no adverse safety signal for anacetrapib (Cardiovasc Drugs Ther 2011)
- Three CETP variants are among only six SNPs linked to HDL cholesterol in European adolescents, first shown in this age group (Atherosclerosis 2011)
- CETP variant rs1532624 reduces heart attack risk in women regardless of physical activity level, unlike an LPL variant with an activity-dependent effect (Circ Cardiovasc Genet 2011)
- A review classifies novel HDL-raising drugs into four strategies, including CETP inhibition, to address residual cardiovascular risk (Nat Rev Cardiol 2011)
- A four-week rimonabant intervention in CETP-humanised mice cuts body weight 9.4% and plasma cholesterol 24%, with systems-lipidomics revealing distinct plasma and liver lipid signatures (PLoS One 2011)
- A decade-spanning review narrows thirty cholesterol-lowering drug targets to six for detailed chemical and mechanistic analysis, including CETP inhibitors (Curr Med Chem 2011)
- Higher CETP levels in follicular fluid correlate with more mature oocytes and higher IVF/ICSI fertilization rates (Iran J Reprod Med 2011)
- CETP Taq1B B1B1 genotype independently raises type 2 diabetes risk, and a hepatic lipase variant amplifies it further (PLoS One 2011)
- CETP activity is higher in obese adolescent boys and correlates with more TV watching and higher milk intake (Arch Med Res 2011)
- A well-powered study of CETP sequence variation finds no meaningful association with cognitive decline or dementia risk (Int J Mol Epidemiol Genet 2011)
- A disease-associated CETP mutation drives amyloid formation and cytotoxicity in vitro (Int J Mol Sci 2011)
- Doses of dalcetrapib up to 4500 mg, far above the therapeutic dose, are well tolerated in a phase I ascending-dose study (Clin Drug Investig 2011)
- Review argues lipid therapy must look beyond LDL, citing CETP inhibition as promising but still unproven in outcome trials (Curr Pharm Des 2011)
- Review finds anacetrapib and dalcetrapib safely raise HDL-C without the off-target effects that doomed torcetrapib (Ann Pharmacother 2011)
2010 81
- CETP Taq1B B1B1 genotype is more common in Egyptian metabolic syndrome patients and tracks with lower HDL cholesterol (Diabetes Metab Syndr 2011)
- An orally delivered trefoil-factor-CETP chimeric vaccine raises intestinal and serum anti-CETP antibodies and inhibits atherosclerosis in rabbits (Peptides 2010)
- CETP promoter variant -629C>A is strongly linked to cardiovascular disease specifically in Asian Indian patients with type 2 diabetes (J Diabetes Complications 2011)
- Review notes CETP transgene expression normalizes hepatic HDL cholesteryl ester delivery in humanized SR-BI knockout mice (World J Gastroenterol 2010)
- The dal-VESSEL study is designed as the largest trial of brachial flow-mediated dilatation to test dalcetrapib effects on endothelial function (Curr Med Res Opin 2011)
- Ezetimibe does not blunt the HDL-raising effect of dalcetrapib, and each drug leaves the other pharmacokinetics largely unchanged (Br J Clin Pharmacol 2010)
- CETP and LPL polymorphisms jointly predict cardiovascular risk in women with high HDL cholesterol and CRP (Atherosclerosis 2011)
- The original benzoxazole scaffold-redesign paper discovers CETP inhibitor 11v, raising HDL cholesterol by 24 mg/dl in mice (Bioorg Med Chem Lett 2011)
- Landmark NEJM safety trial shows anacetrapib avoids the cardiovascular harm of torcetrapib while doubling HDL cholesterol (N Engl J Med 2010)
- Molecular docking maps the hydrophobic P1/P2 binding pockets used by trifluoro-aminopropanol CETP inhibitors (J Mol Model 2011)
- CETP mutations raise HDL 27-hydroxycholesterol, and CETP mass correlates more strongly with 27OHC-ester than cholesteryl ester transfer (Atherosclerosis 2010)
- Chromanol derivatives emerge as a novel class of orally active CETP inhibitors suitable for clinical development (Bioorg Med Chem Lett 2011)
- 2-Arylbenzoxazole CETP inhibitors raise HDL cholesterol in cynoCETP transgenic mice (Bioorg Med Chem Lett 2011)
- Lead biphenyl CETP inhibitor 12d significantly raises HDL in a transgenic mouse model (Bioorg Med Chem Lett 2010)
- Naturally low CETP and PLTP activity may explain atherosclerosis resistance in tree shrews and Beijing ducks (Lipids Health Dis 2010)
- Up-titrated rosuvastatin and atorvastatin both significantly reduce CETP mass and activity in low-HDL-C cardiovascular patients (Curr Med Res Opin 2010)
- CETP TaqI and -629C/A variants predict a bigger HDL-C rise on atorvastatin, while CETP 405I/V predicts higher MI risk in CAD patients (DNA Cell Biol 2010)
- Atorvastatin reduces exposure to dalcetrapib without diminishing its cardiovascular benefit, two crossover studies find (Expert Opin Investig Drugs 2010)
- A structural-and-metabolic-network computational model predicts off-target causes of the hypertensive side effect of torcetrapib in kidney tissue (PLoS Comput Biol 2010)
- Only dalcetrapib preserves pre-beta HDL formation and boosts fecal sterol excretion, unlike torcetrapib and anacetrapib (J Lipid Res 2010)
- CETP variant rs5882 is the second-strongest of nine genetic hits for low HDL cholesterol and heart disease risk in a 60-gene screen (J Lipid Res 2010)
- CETP Taq1B B2B2 genotype is linked to the highest HDL cholesterol and lowest oxidative stress marker levels in Tehran adults (Lipids Health Dis 2010)
- CETP Taq1B polymorphism shows no effect on HDL cholesterol or coronary artery disease risk in a Turkish angiography cohort (Genet Test Mol Biomarkers 2010)
- Lead benzylamino-methanone compound achieves 30 percent CETP inhibition at 10 micromolar (Molecules 2010)
- Postprandial lipemia boosts HDL2's cholesterol efflux capacity but raises CETP-mediated transfer and impairs hepatic HDL delivery in type IIB hyperlipidemia (J Lipid Res 2010)
- Higher on-statin CETP mass predicts fewer recurrent coronary events in the PROVE IT-TIMI 22 trial (Am J Cardiol 2010)
- Gastric bypass weight loss in obese women improves HDL remodeling, with CETP mass changes tracking glucose improvement but not fat-mass loss (J Lipid Res 2010)
- CETP activity stays unchanged despite severely disrupted lipoproteins in Hantaan virus renal failure (BMB Rep 2010)
- A review finds niacin remains the most potent HDL-raising therapy while CETP inhibitors stand closest to clinic despite the mortality signal seen with torcetrapib (Curr Treat Options Cardiovasc Med 2010)
- L-type calcium channels explain how torcetrapib raises aldosterone and blood pressure, an effect dalcetrapib does not share (J Hypertens 2010)
- Two CETP inhibitors reach systemic circulation mainly via lymphatic transport, 22 to 28% of dose (Pharm Res 2010)
- Review traces the ILLUMINATE mortality signal of torcetrapib to adrenal aldosterone secretion, not receptor blockade (Hypertens Res 2010)
- Review argues CETP may be atheroprotective and aid host defense, complicating the case for inhibiting it (Cardiovasc Ther 2011)
- A workaround measures two acyl-glucuronide metabolites of torcetrapib in monkey urine without ever having reference standards for them (Biomed Chromatogr 2010)
- Noninvasive high-definition oscillometry matches implanted telemetry for tracking torcetrapib-induced blood pressure rises in dogs (J Am Assoc Lab Anim Sci 2010)
- CETP variants raise HDL cholesterol by up to 14 percent regardless of diet, alcohol, or diabetes status in a high-risk Mediterranean population (J Lipid Res 2010)
- A review of CETP molecular mechanisms notes the negative phase III torcetrapib trials challenged the future of the drug class (Cell Mol Life Sci 2010)
- Octodon degus develop human-like atherosclerosis on a cholesterol diet, with baseline CETP activity comparable to humans (Atherosclerosis 2010)
- Acute Epstein-Barr virus infection transiently elevates CETP activity alongside other atherogenic lipid changes that resolve within four months (Atherosclerosis 2010)
- Even at more than 6 times the therapeutic dose, dalcetrapib does not prolong the QT interval in healthy subjects (Eur J Clin Pharmacol 2010)
- Low CETP activity and enhanced HDL2 paraoxonase found together in a patient with unusually low LDL-to-cholesterol ratio (Int J Mol Med 2010)
- People with genetically reduced CETP levels have lower, not higher, blood pressure, arguing against a CETP class effect behind the hypertension seen with torcetrapib (Mayo Clin Proc 2010)
- Review of phase II dalcetrapib data flags its unique CETP-binding mechanism ahead of dal-OUTCOMES (Expert Opin Investig Drugs 2010)
- CETP variant rs708272 improves diagnostic accuracy for identifying patients with active atherosclerosis (Swiss Med Wkly 2010)
- Low plasma CETP predicts higher mortality in nondiabetic coronary disease patients in the KAROLA cohort (Eur J Clin Invest 2010)
- Rosuvastatin raises its own peak concentration by 26 percent when combined with dalcetrapib, but the LDL benefit of the combination still exceeds statin alone (J Clin Pharmacol 2010)
- CETP TaqIB B2 allele more than doubles recurrent event risk in postinfarction patients with high HDL-C and CRP (Arterioscler Thromb Vasc Biol 2010)
- Anacetrapib binds CETP reversibly while dalcetrapib binds covalently, explaining their different inhibitory kinetics (J Lipid Res 2010)
- A review argues CETP inhibitor trial failures show HDL-C elevation alone is insufficient, motivating apoA-I-targeted therapies instead (Drugs 2010)
- Anacetrapib doubles HDL cholesterol and, unlike niacin, boosts cholesterol efflux per particle at high HDL levels (ATVB 2010)
- Torcetrapib impairs blood vessel dilation through a mechanism unrelated to CETP inhibition or HDL elevation, unlike a structurally different CETP inhibitor (J Cardiovasc Pharmacol 2010)
- CETP restores HDL cholesterol in SR-BI-deficient mice but fails to prevent atherosclerosis (Arterioscler Thromb Vasc Biol 2010)
- LXRalpha, not LXRbeta, drives human CETP transcription, confirmed in monkeys, human-CETP-transgenic mice, and HepG2 cells (Atherosclerosis 2010)
- CETP is one of only four genes confirmed to affect HDL cholesterol, with no evidence its effect depends on alcohol intake (Atherosclerosis 2010)
- Review asks whether anacetrapib offers the greatest HDL-raising, LDL-lowering promise among CETP inhibitors (Cardiovasc Ther 2011)
- A review identifies CETP as a key enzyme liberating serum amyloid A during acute-phase HDL remodeling (Curr Opin Endocrinol Diabetes Obes 2010)
- Review links apoB signal-peptide and CETP B1B1 combination to lower VLDL apoB secretion in obese men (Curr Opin Lipidol 2010)
- Falling CETP levels during hospitalization predict mortality in patients with severe sepsis (Eur J Clin Invest 2010)
- CETP TaqIB fails to protect against coronary heart disease over 10 years despite raising HDL cholesterol, and even raises risk in drinkers (Atherosclerosis 2010)
- CETP Taq1B B2 allele linked to lower coronary artery disease risk in Asian Indians (J Community Genet 2010)
- A humanized transgenic mouse model shows torcetrapib raises HDL cholesterol by 53 percent, less than a potent PPAR-alpha agonist (J Cardiovasc Pharmacol Ther 2010)
- Thirty-five days of bed rest raises plasma CETP by 27% independently of fat mass in healthy men (J Clin Endocrinol Metab 2010)
- A review explains why CETP-expressing hamsters, not mice, are the preferred preclinical model for testing reverse-cholesterol-transport drugs (Curr Opin Investig Drugs 2010)
- A review argues that after the torcetrapib failure, HDL functionality biomarkers are needed since HDL cholesterol alone is not a functional measure (Expert Rev Cardiovasc Ther 2010)
- Pioglitazone lowers plasma CETP mass and hepatic triglyceride content while raising HDL cholesterol in type 2 diabetes, confirming prior mouse findings (Diabetes Care 2010)
- CETP TaqIB B1B1 men are most responsive to a high-carbohydrate low-fat diet's HDL-raising effect in young Chinese adults (J Nutr Biochem 2010)
- CETP TaqIB genotype distinguishes a longevity syndrome of simultaneously high HDL and LDL cholesterol (Open Cardiovasc Med J 2010)
- A 48-week trial finds dalcetrapib raises HDL cholesterol by a third with no measurable effect on lymph node size (Eur Heart J 2010)
- Novel tetrahydrochinoline derivatives yield a potent CETP inhibitor with favourable pharmacokinetics for clinical development (Bioorg Med Chem Lett 2010)
- Pharmacophore and QSAR modelling identifies new CETP inhibitor leads including NSC 40331 at 6.5 micromolar (Eur J Med Chem 2010)
- A JAMA study links CETP valine-405 homozygosity to slower memory decline and lower dementia incidence (JAMA 2010)
- The rodent-specific scavenger receptor MARCO drives the off-target lipid uptake seen with dalcetrapib in mouse macrophages (Toxicol In Vitro 2010)
- LURIC study of 3,256 angiography patients finds low, not high, CETP levels predict mortality (Circulation 2010)
- A new benzoxazine class of CETP inhibitors raises HDL cholesterol in transgenic mice and hamsters (Bioorg Med Chem Lett 2010)
- CETP TaqIB genotype determines whether atorvastatin raises or lowers HDL cholesterol (Open Cardiovasc Med J 2010)
- Olive-oil-enriched skim milk raises HDL cholesterol most in children with the CETP B1B1 genotype (Ann Nutr Metab 2010)
- CETP raises HDL triglyceride but leaves triglyceride production and clearance unchanged in APOE*3-Leiden mice (J Lipid Res 2010)
- Metabolic syndrome raises serum CETP activity 38% alongside dysfunctional, antioxidant-depleted HDL (Int J Mol Med 2010)
- A review argues that the harms of torcetrapib trace to its own tight CETP binding and an aldosterone-like effect, not to CETP inhibition itself (Rom J Intern Med 2010)
- Drug profile tracks the path of anacetrapib from Merck development into a 76-week international phase III trial (Am J Cardiovasc Drugs 2010)
- Davidson explains how triglycerides turn CETP into a generator of small, dense, atherogenic LDL and HDL particles (J Clin Lipidol 2010)
2009 93
- Mendelian randomization shows the hypertensive effect of torcetrapib is not caused by CETP inhibition (Circulation 2010)
- High fasting CETP levels predict a larger postprandial HDL cholesterol drop after fat-rich meals, independent of triglyceride rise, in the Hoorn prandial study (Metabolism 2010)
- Modifying the alpha-alkoxyamide moiety of arylbenzoxazole CETP inhibitors yields an orally bioavailable lead (Bioorg Med Chem Lett 2010)
- Anacetrapib shows moderate oral bioavailability in rats and monkeys, with most of the dose excreted unchanged in feces (Drug Metab Dispos 2010)
- Nearly 87% of an oral anacetrapib dose is eliminated unchanged in feces, with only trace CYP3A4-generated metabolites (Drug Metab Dispos 2010)
- Higher circulating CETP activity predicts fewer cardiovascular events over 15 years in the Framingham Heart Study (Circulation 2009)
- A dietary lysine-to-arginine ratio trial finds no effect on CETP or LCAT activity, though it modestly shifts postprandial VLDL, triglycerides, and inflammation markers (Atherosclerosis 2010)
- Combined LIPC and CETP I405V variants double coronary artery disease risk, but the effect fades in women with high HDL cholesterol (Genet Test Mol Biomarkers 2009)
- Torcetrapib raises blood pressure in dogs through systemic and pulmonary vasoconstriction that also strains the heart (J Cardiovasc Pharmacol 2009)
- Torcetrapib raises blood pressure and RAAS gene expression in rats, but dalcetrapib does neither (Br J Pharmacol 2009)
- Dal-OUTCOMES trial design targets 15,600 recent-ACS patients to test whether dalcetrapib reduces cardiovascular events (Am Heart J 2009)
- Ciprofibrate boosts CETP gene expression and speeds cholesterol delivery to the liver in CETP-transgenic mice (Lipids Health Dis 2009)
- CETP -629C>A promoter variant predicts HDL-C response to growth hormone only in glucocorticoid-treated patients (Eur J Endocrinol 2010)
- CETP TaqIB B2 allele partly protects against the atherogenic HDL profile of type 2 diabetes, but only in women with milder insulin resistance (Atherosclerosis 2010)
- A review argues the mortality signal from torcetrapib traces to off-target toxicity, not to CETP inhibition itself (Am J Cardiol 2009)
- HDL from patients on high-dose torcetrapib removes more cholesterol from macrophages, correlating with the atheroma regression seen on the drug (Am J Cardiol 2009)
- Barter reflects on ILLUMINATE: the harm caused by torcetrapib likely reflects off-target effects, not CETP inhibition itself (Am J Cardiol 2009)
- Lead 2-arylbenzoxazole compound inhibits CETP with an IC50 of 28 nanomolar (Bioorg Med Chem Lett 2009)
- Torcetrapib does not block CETP or LPS-binding-protein interactions, ruling out a direct sepsis-mortality mechanism (J Lipid Res 2010)
- CETP Taq1B B1B1 genotype is linked to higher insulin and HOMA levels, suggesting a role in glucose regulation (Nutr Metab Cardiovasc Dis 2011)
- Chapman and colleagues place CETP at the center of how statins, fibrates, niacin, and CETP inhibitors modulate HDL (Eur Heart J 2010)
- The novel SR-BI inhibitor ITX5061 raises HDL cholesterol by 20% in humans and reduces atherosclerosis in mice regardless of CETP expression (Arterioscler Thromb Vasc Biol 2009)
- CETP TaqIB polymorphism does not predict coronary restenosis after angioplasty and stenting (Angiology 2010)
- CETP -629C>A polymorphism is not among the genetic determinants of coronary artery disease in Turks despite its HDL cholesterol effect (Cell Biochem Funct 2009)
- DEFINE trial design paper describes screening 2,757 patients and randomizing 1,623 across 153 centers in 20 countries (Am Heart J 2009)
- A high-fat meal can raise anacetrapib exposure up to eight-fold, but age, sex, and obesity barely move it (Br J Clin Pharmacol 2009)
- Review finds the lipoprotein effects of anacetrapib surpass both torcetrapib and dalcetrapib, though long-term safety remains unproven (Curr Opin Investig Drugs 2009)
- Patent landscape review tracks CETP inhibitor development from 2000 through the termination of torcetrapib (Expert Opin Ther Pat 2009)
- Inflammatory macrophages selectively lose the LXR-driven induction of CETP seen in noninflammatory cells, even as ABCA1 and ABCG1 induction persist (Arterioscler Thromb Vasc Biol 2009)
- Nevirapine raises HDL cholesterol in HIV patients by boosting apoA-I production, with a modest CETP activity increase (Arterioscler Thromb Vasc Biol 2009)
- Review highlights a paradox, CETP protects against bacterial infection but promotes atherosclerosis (Atherosclerosis 2009)
- Berry anthocyanins raise HDL and lower LDL cholesterol via natural CETP inhibition in a placebo-controlled trial (Am J Clin Nutr 2009)
- Rare CETP-deficient case reveals independent control of remnant triglyceride and cholesterol after a fat load (Ann Clin Biochem 2009)
- Higher CETP quartiles predict more coronary calcium and thicker carotid intima-media in Japanese men, independent of D442G genotype (Am J Cardiol 2009)
- Multiple-dose study of the CETP inhibitor CP-800,569 shows dose-dependent HDL rise and LDL fall (Clin Pharmacol Ther 2009)
- Improved asymmetric synthesis route delivers a potent tetrahydroquinoline CETP inhibitor without a hazardous aryltin reagent (Org Lett 2009)
- Statin-induced LDL and non-HDL cholesterol reductions track with falling CETP mass in type 2 diabetes (Expert Opin Ther Targets 2009)
- Pooled phase II data show dalcetrapib raises HDL cholesterol up to 36 percent without the blood pressure or aldosterone effects seen with torcetrapib (Am J Cardiol 2009)
- Hegele argues the pressor effect of torcetrapib, not CETP inhibition itself, doomed the drug and asks if the class deserves another chance (Curr Opin Cardiol 2009)
- LCAT overexpression raises HDL cholesterol but does not boost macrophage reverse cholesterol transport, even alongside SR-BI or CETP coexpression (Circulation 2009)
- CETP TaqIB and I405V polymorphisms show sex-specific effects on postprandial triglycerides in familial hypercholesterolaemia (Lipids Health Dis 2009)
- Two new CETP and LIPC gene mutations identified as causes of extremely high HDL cholesterol in Thai patients (Metabolism 2009)
- Brucella infection raises CETP activity and leaves an unresolved atherogenic lipid profile four months after treatment (J Lipid Res 2009)
- A review catalogs the chiral and achiral bioanalytical methods developed to measure torcetrapib across six species (Bioanalysis 2009)
- Torcetrapib and CP-532,623 raise blood pressure via a chemotype-specific mechanism dissociated from CETP inhibition timing (J Cardiovasc Pharmacol 2009)
- CETP TaqIB significantly shapes baseline HDL subpopulation profile in postmenopausal women, though hormone therapy response is largely unaffected (Clin Endocrinol 2010)
- JTT-705, the dalcetrapib precursor compound, blocks LPS-triggered TNF-alpha production in mice by targeting a cysteine on MD-2 (J Biol Chem 2009)
- CETP gene mutations shape LDL and HDL cholesterol from birth through the first year of life (Clin Chim Acta 2009)
- CETP variant D442G raises HDL cholesterol nearly three times more in obese than normal-weight Chinese individuals (Obesity 2009)
- The CETP SNP rs1800775 explains more variance in HDL cholesterol than any other single lipid gene variant studied in older adults (Eur Heart J 2009)
- Apolipoprotein CI regulates CETP activity in human plasma but not in rabbit plasma, a species-specific mechanism (J Lipid Res 2009)
- CETP delays clearance of dietary fat by slowing triglyceride clearance and suppressing lipoprotein lipase (Biochem J 2009)
- Reducing proteinuria lowers LDL cholesterol together with plasma CETP mass, but also lowers HDL cholesterol (Expert Opin Ther Targets 2009)
- Genome-wide protein-ligand network analysis maps the off-target pathways behind the hypertensive side effect of torcetrapib (PLoS Comput Biol 2009)
- CETP TaqIB B2 allele linked to higher HDL cholesterol in Greek children (Nutr Metab Cardiovasc Dis 2010)
- CETP locus generalizes as a blood-lipid determinant across black, Mexican American, and white US populations (Circ Cardiovasc Genet 2009)
- CETP TAQIB and I405V rare alleles are modestly associated with reduced obesity risk in Chinese adults, largely via HDL levels (Acta Diabetol 2009)
- CETP genotype tracks with HDL cholesterol and triglycerides but not with coronary artery disease risk in Turkish angiography patients (Eurasian J Med 2009)
- CETP -629C/A AA genotype raises HDL cholesterol but may still carry higher coronary artery disease risk in Iranian Azeris (Iran Biomed J 2009)
- Dalcetrapib inhibits CYP enzymes in vitro but has no clinically relevant drug interaction with a five-probe drug cocktail (Curr Med Res Opin 2009)
- A conformationally constrained CETP inhibitor matches the HDL-raising efficacy of torcetrapib across hamsters, transgenic mice, and monkeys (J Med Chem 2009)
- A translational-medicine commentary argues the failure of 4 large torcetrapib trials calls for biomarker-driven drug development, not abandonment of CETP as a target (Biochem Pharmacol 2009)
- High-dose atorvastatin reduces pre-beta-HDL formation and CETP activity in type 2 diabetes, mediated by falling PLTP activity and triglycerides, not CETP (Biochim Biophys Acta 2009)
- CETP drives atherosclerosis mainly by raising VLDL-cholesterol, not by lowering HDL-cholesterol, in APOE*3-Leiden mice (Atherosclerosis 2009)
- CETP-HDL association is one of only four gene-lipid-trait pairs replicated using a new cardiovascular gene chip in a multiethnic cohort (J Lipid Res 2009)
- Tetrahydroquinoline platform yields a 39nM CETP inhibitor for raising HDL-C (Bioorg Med Chem Lett 2009)
- Plasma CETP and PLTP levels are unchanged in end-stage renal disease despite HDL abnormalities (Nephrol Dial Transplant 2009)
- A mathematical model shows torcetrapib and JTT-705 inhibit CETP more potently than classic competitive inhibition would predict (J Lipid Res 2009)
- CETP I405V VV genotype is linked to higher HDL cholesterol in Turks, an effect modified by sex and triglycerides (Cell Biochem Funct 2009)
- CETP variant A373P is independently linked to lower HDL cholesterol and ApoA-I-containing lipoproteins, largely independent of other tested genes (Metabolism 2009)
- CETP activity is markedly elevated in Iranian patients with primary combined hyperlipidaemia, modulated by Taq1B genotype (Indian J Med Res 2009)
- Ketoconazole unexpectedly lowers exposure to dalcetrapib rather than raising it, contrary to typical CYP3A4-inhibitor interactions (Clin Ther 2009)
- CETP I405V V-allele carriers lose more ApoA-I and HDL cholesterol when switched from a high to low polyunsaturated fat diet (Horm Metab Res 2009)
- Tesaglitazar lowers CETP mass and activity and halts progression of existing atherosclerosis in CETP-transgenic mice (Br J Pharmacol 2009)
- Anacetrapib leaves simvastatin pharmacokinetics unchanged while adding incremental LDL-C lowering when combined (Br J Clin Pharmacol 2009)
- Torcetrapib raises apolipoprotein A-II levels by slowing its clearance and shifting it into a different HDL subpopulation (J Lipid Res 2009)
- A PADRE T-cell epitope CETP vaccine paired with CpG adjuvant elicits stronger anti-CETP antibody responses than the CETi-1 vaccine in mice and rabbits (Hum Vaccin 2009)
- A review draws lessons from ILLUMINATE on the hypertension risk of CETP inhibitors despite raising HDL cholesterol by up to 100 percent (Curr Hypertens Rep 2009)
- CETP-mediated cholesterol transfer cannot substitute for SR-BI in adrenal steroid production (J Lipid Res 2009)
- A CETP variant raises vascular dementia risk and lowers white matter lesion load, but only in APOE4 non-carriers (J Neural Transm 2009)
- Genome-wide analysis of 18,245 women finds CETP is the only HDL-raising locus that also lowers heart attack risk, supporting a causal role (Circ Cardiovasc Genet 2009)
- Torcetrapib induces adrenal aldosterone and cortisol via intracellular calcium signaling, unrelated to CETP inhibition (Endocrinology 2009)
- A novel CETP R37X mutation causes complete CETP deficiency and extreme HDL elevation without atherosclerosis in a Swedish man (Atherosclerosis 2009)
- Rising VLDL-triglyceride from bexarotene drives CETP activity up and HDL cholesterol down (Endocrinology 2009)
- CETP B1B1 genotype nearly triples coronary heart disease risk in a South Indian population (Clin Chim Acta 2009)
- CETP variants without known cardioprotective effects still raise large HDL particle concentrations by up to 40 percent, questioning what HDL particle size means (Clin Chem 2009)
- CETP TaqIB B2B2 genotype more than doubles cardiovascular death risk after acute coronary syndrome, unless the patient takes a statin (Clin Chem Lab Med 2009)
- Review surveys CETP's role in lipid metabolism and the state of small-molecule inhibitor development for raising HDL-C (Curr Top Med Chem 2009)
- A review of nonstatin add-on therapies finds torcetrapib raised mortality in coronary patients despite a marked rise in HDL cholesterol (Curr Atheroscler Rep 2009)
- A review weighs four possible explanations for why torcetrapib raised cardiovascular risk despite raising HDL cholesterol (Ann Med 2009)
- Adding a bile correction factor sharpens allometric prediction of human pharmacokinetic parameters for orally dosed torcetrapib (Eur J Drug Metab Pharmacokinet 2009)
- A review links the B1B1 CETP genotype to higher CETP activity, lower HDL cholesterol, and more pronounced postprandial lipemia (Curr Med Chem 2009)
- Clinician's overview names CETP inhibitors the most potent HDL-raising drugs, but torcetrapib fell to excess cardiovascular harm (Angiology 2009)
2008 80
- CETP expression reverses the direction of PXR agonism effect on HDL cholesterol, turning an increase in mice into a dose-dependent decrease (Biochim Biophys Acta 2009)
- Thyromimetic T-0681 cuts atherosclerosis 80% in rabbits by raising hepatic LDL receptors, not by changing CETP (J Lipid Res 2008)
- Phase 2 dose-ranging trial finds anacetrapib plus atorvastatin cuts LDL-C by 70% and more than doubles HDL-C (Am Heart J 2009)
- Serum cholesterol efflux capacity is preserved or enhanced in genetically CETP-deficient patients (Clin Chim Acta 2008)
- Long-term danazol use lowers CETP mass without significantly affecting HDL cholesterol or atherosclerosis markers (Clin Ther 2008)
- CETP gene variants that raise HDL cholesterol actually lower diastolic blood pressure, arguing the hypertension seen with torcetrapib is compound specific (Pharmacogenet Genomics 2008)
- Torcetrapib partly restores healthy HDL2 and HDL3 function in type IIB hyperlipidemia, boosting cholesterol efflux by up to 38 percent (Arterioscler Thromb Vasc Biol 2009)
- The ILLUSTRATE trial finds coronary atheroma regression on torcetrapib only in patients reaching the highest quartile of HDL-C rise (Circulation 2008)
- Pooled RADIANCE trial data link the carotid-thickening harm of torcetrapib to a mineralocorticoid effect, not to its HDL-raising action (Circulation 2008)
- A review notes a meta-analysis linking CETP-lowering alleles to reduced coronary heart disease, distinct from the off-target failure of torcetrapib (J Lipid Res 2009)
- A perspective argues the torcetrapib failure should redirect HDL drug development away from raw cholesterol concentration and toward specific antiatherosclerotic components (Ann Clin Biochem 2009)
- Diet-induced hypercholesterolemia raises plasma LTIP mass 2.5-fold while suppressing its hepatic mRNA, diverging from CETP's response in hamsters and rabbits (J Lipid Res 2008)
- The combined action of SAA, secretory phospholipase A2, and CETP remodels HDL during the acute phase response while preserving cholesterol efflux capacity (Arterioscler Thromb Vasc Biol 2009)
- Anacetrapib neither inhibits nor induces CYP3A, but ketoconazole raises its own exposure more than fourfold (J Clin Pharmacol 2009)
- CETP discovered to protect mice against lethal bacterial endotoxin by dampening the inflammatory response (Shock 2008)
- A CETP gene variant favors healthy survival past age 90 in long-lived Japanese-American men (J Gerontol A Biol Sci Med Sci 2008)
- Natural variation in plasma CETP levels does not affect RAAS responsiveness or blood pressure reactivity in healthy men (Expert Opin Ther Targets 2008)
- A review argues the off-target effects of torcetrapib, not the CETP-inhibition mechanism itself, likely overrode any cardiovascular benefit (Cardiol Clin 2008)
- Genetically low CETP predicts higher 10-year mortality in statin-treated men with coronary artery disease (Eur Heart J 2008)
- CETP B1 allele raises metabolic syndrome risk specifically in Turkish women, large cross-sectional study finds (Anadolu Kardiyol Derg 2008)
- CETP Taq1B B2 allele cuts coronary stenosis risk by 18 percent overall, and 38 percent in male nonsmokers, in Tunisians (Arch Cardiovasc Dis 2008)
- Only triglyceride-rich apoB lipoprotein subclasses accept cholesteryl esters transferred by CETP (Eur J Clin Invest 2008)
- Review asks whether JTT-705 (dalcetrapib) or anacetrapib can still succeed after the collapse of torcetrapib (Expert Opin Investig Drugs 2008)
- JTT-705 (dalcetrapib) raised HDL-C 26% and improved endothelial function only in low-baseline-HDL patients (Thromb Res 2009)
- Acute coronary syndrome reduces leucocyte CETP expression up to 6-fold, with recovery tracking reduced inflammation, confirmed in CETP transgenic mice (J Intern Med 2008)
- First CETP gene mutations identified in Italian patients with extremely high HDL cholesterol, including two premature-stop-codon variants (Atherosclerosis 2009)
- ANGPTL3 abnormalities outnumber CETP abnormalities in Japanese hyperalphalipoproteinemic subjects (Clin Chim Acta 2008)
- A review argues the torcetrapib failure highlights HDL functionality, not raw HDL cholesterol level, as the real therapeutic target (Curr Opin Investig Drugs 2008)
- 3D-QSAR modelling of 61 dibenzodioxepinone and dibenzodioxocinone compounds maps the structural features driving CETP inhibitory potency (Molecules 2008)
- Torcetrapib is extensively metabolized in humans with terminal half-lives of 211 to 373 hours (Drug Metab Dispos 2008)
- CETP TaqIB predicts HDL cholesterol in one Chinese ethnic minority but not in neighboring Han Chinese (J Investig Med 2008)
- Apple polyphenols improve cholesterol distribution in hamsters by directly inhibiting CETP activity (Mol Nutr Food Res 2008)
- Review weighs conflicting evidence for CETP as a pro- versus antiatherogenic therapeutic target (Expert Opin Ther Targets 2008)
- Niacin raises HDL cholesterol by suppressing hepatic CETP expression, not by any CETP-independent route (Arterioscler Thromb Vasc Biol 2008)
- CETP genetic variants are linked to plasma vitamin E levels, extending CETP genetics beyond cholesterol transport (Br J Nutr 2009)
- Two CETP variants are among only seven SNPs confirmed to affect HDL cholesterol in a 384-SNP, 251-gene screen (J Lipid Res 2008)
- Torcetrapib forms more than 28 species-dependent metabolites in rats, monkeys, and mice (Drug Metab Dispos 2008)
- Biosensor mapping places the torcetrapib binding site at Cys-13 in the CETP lipid-binding pocket (Bioconjug Chem 2008)
- CETP variants shape cerebral and peripheral cholesterol metabolism but not Alzheimer's disease risk (Brain Res 2008)
- CETP haplotype G raises early-onset heart-attack risk up to 6-fold in men, independent of HDL-C (Ann Hum Genet 2008)
- Landmark JAMA meta-analysis of over 190,000 people finds CETP genotypes that inhibit CETP activity only weakly reduce coronary risk (JAMA 2008)
- FXRalpha suppresses CETP gene expression by competing with LXRalpha at a shared promoter element (Mol Cells 2008)
- Review attributes statins' modest HDL-raising effect to reduced CETP-mediated cholesterol flow (Cardiovasc Drugs Ther 2008)
- Serum CETP is lowest at birth and rises sharply to peak levels in infancy, reference data from healthy Chinese children (Clin Biochem 2008)
- Adrenalectomy prevents the torcetrapib blood pressure rise, proving CETP inhibition itself is not the culprit (Br J Pharmacol 2008)
- Updated pooled analysis finds the CETP B2 allele may raise, not lower, cardiovascular risk in the general population despite higher HDL cholesterol (Pharmacogenomics 2008)
- Both wild-type CETP and its poorly secreted splice variants trigger the same endoplasmic reticulum stress response (J Lipid Res 2008)
- Neither high CETP activity nor low HDL cholesterol predicts cardiovascular events in stage V chronic kidney disease (Nephrol Dial Transplant 2008)
- Six weeks of endurance training lowers CETP activity regardless of egg intake in unfit adults (J Nutr Biochem 2008)
- Review reconsiders the protective reputation of HDL after the abrupt ILLUMINATE failure of torcetrapib (Biochem Pharmacol 2008)
- Torcetrapib produces smaller but more inflamed, less stable plaques than atorvastatin in humanized transgenic mice (Circulation 2008)
- CETP TaqIB variant, unlike APOE4, shows no link to obesity or blood pressure in North Indian subjects (Mol Cell Biochem 2008)
- A review argues ABCA1 and ABCG1 transporters, not raw HDL cholesterol level, drive HDL's atheroprotective effect after the torcetrapib failure (Cell Metab 2008)
- A review concludes the mineralocorticoid-driven hypertension seen with torcetrapib is not a CETP-inhibitor class effect, since JTT-705 and MK-825 do not raise blood pressure (Nat Clin Pract Cardiovasc Med 2008)
- A review proposes injecting synthetic HDL directly as an alternative after torcetrapib, the furthest-developed HDL-raising pill, was halted for excess mortality (Nutr Metab Cardiovasc Dis 2008)
- A fat load raises CETP mass and cholesteryl ester transfer while lowering HDL cholesterol in obese metabolic syndrome men, unaffected by statin or statin-ezetimibe treatment (Clin Endocrinol 2008)
- A diabetes-dyslipidemia review predicts the disappointing torcetrapib results will renew interest in niacin therapy (Curr Opin Endocrinol Diabetes Obes 2008)
- A review attributes the excess deaths seen with torcetrapib to an off-target effect, not to CETP inhibition, while low HDL remains an important risk marker (Curr Opin Endocrinol Diabetes Obes 2008)
- A review argues the torcetrapib failure shifted laboratory focus from HDL cholesterol concentration to HDL particle heterogeneity and function (Clin Chem 2008)
- Cyclosporine and Rapamycin, but not Tacrolimus or Mycophenolate, raise in vitro CETP activity while all four immunosuppressants suppress lipoprotein lipase (Int J Pharm 2008)
- LTIP loses its CETP-inhibiting activity when sequestered into a 470 kDa apolipoprotein complex (J Lipid Res 2008)
- Two novel CETP protein variants identified through resequencing in individuals of Asian ancestry, both partly functional (Atherosclerosis 2009)
- Array synthesis optimizes a high-throughput screening hit into a novel 2-arylbenzoxazole CETP inhibitor series (Bioorg Med Chem Lett 2008)
- CETP B1B1 genotype combined with APOE or APOC3 risk variants quadruples coronary artery disease risk when all three are present (Atherosclerosis 2008)
- A new LC-MS/MS assay quantifies torcetrapib in hamster and dog plasma down to 1 nanogram per mL (Biomed Chromatogr 2008)
- CETP levels track with bile acid concentration in children with Alagille syndrome cholestasis (Atherosclerosis 2008)
- CETP coding variants R451Q and A373P predict coronary calcium independent of HDL cholesterol in a multi-ethnic cohort (Atherosclerosis 2008)
- Probucol lowers ANGPTL3 and large-HDL phospholipids while raising prebeta1-HDL in hypercholesterolemic patients (Atherosclerosis 2008)
- CETP gene is the only lipid-metabolism gene whose HDL-C association shifts with menopause in the ARIC Study (Atherosclerosis 2008)
- A Nature Reviews Drug Discovery analysis asks whether the torcetrapib failure means functional quality of HDL matters more than its circulating quantity (Nat Rev Drug Discov 2008)
- CETP Taq1B B2 variant cuts metabolic syndrome risk by up to 57% in a large Austrian cohort (Obesity (Silver Spring) 2008)
- Glucocorticoid replacement erases the CETP promoter variant's link to HDL cholesterol in hypopituitary patients (Clin Endocrinol (Oxf) 2008)
- Genome-wide meta-analysis of 20,000-plus people confirms CETP among eleven established lipid loci and finds new ones (Nat Genet 2008)
- A review revisiting a 40-year-old study names the CETP, VLDL-triglyceride, and hepatic lipase cluster as drivers of atherogenic HDL and LDL remodeling (Rom J Intern Med 2008)
- CETP B1B1 genotype is nearly twice as common in Taiwanese people with a parental history of cardiovascular disease (Med Princ Pract 2008)
- Review surveys a CETP-inhibiting vaccine among emerging anti-atherosclerotic vaccine strategies (Cardiol Rev 2008)
- Review questions whether CETP inhibitors remain a viable therapeutic approach after a major trial failure (Cardiovasc Ther 2008)
- A review argues four disappointing torcetrapib trials require refining the HDL hypothesis, since HDL may be more carrier protein than cholesterol transporter (Ann Med 2008)
- Review recounts how ILLUMINATE, RADIANCE, and ERASE ended the promise of torcetrapib for isolated low HDL syndrome (Am J Ther 2008)
- Review traces CETP inhibition from a Japanese deficiency discovery to the ILLUMINATE termination of torcetrapib and early anacetrapib data (Cardiol Rev 2008)
2007 85
- Combined CETP- and hepatic-lipase-lowering gene variants raise HDL cholesterol but still increase coronary disease risk in the REGRESS trial (Atherosclerosis 2008)
- Metabolic syndrome patients show hypoadiponectinemia, elevated adhesion molecules, and higher CETP-mediated cholesteryl ester-triglyceride exchange (Atherosclerosis 2008)
- CETP promoter variant linked to lower CETP levels also impairs the ability of plasma to remove cholesterol from cells, a possible clue to its cardiovascular risk (Biochim Biophys Acta 2008)
- First-in-class phase I trials show anacetrapib raises HDL-C by 129% and lowers LDL-C by 38% without raising blood pressure (Lancet 2007)
- Alcohol only reduces heart disease risk in CETP TaqIB B2 carriers, especially among women, two large US cohort studies find (Eur Heart J 2008)
- HIV infection raises CETP mass and activity and redirects cholesterol away from HDL (Atherosclerosis 2007)
- Both raising and lowering CETP activity can enhance reverse cholesterol transport, depending on the species and pathway studied (Cardiovasc Res 2008)
- A review proposes that the now-known crystal structure of CETP could guide the design of inhibitors that avoid the nonproductive HDL complex formed by torcetrapib (Am J Cardiol 2007)
- A review questions whether CETP inhibitors can ultimately reduce cardiovascular events after torcetrapib raised blood pressure without slowing coronary atherosclerosis (Am J Cardiol 2007)
- CETP plasma levels are positively correlated with blood clotting speed, and recombinant CETP enhances prothrombinase activity, revealing a previously unknown procoagulant role (Thromb Haemost 2007)
- CETP activity is significantly elevated in Iranian patients with primary hypertriglyceridemia, and modulated by Taq1B genotype (Pak J Biol Sci 2007)
- The CETP D442G variant shows a preliminary protective association against Alzheimer's disease in Chinese APOE4 carriers (Brain Res 2008)
- CETP I405V fails to replicate as a longevity gene in a large American Caucasian cohort (Biogerontology 2007)
- Torcetrapib reduces VLDL apolipoprotein E levels alone, but on background atorvastatin instead boosts its content and speeds VLDL clearance (J Lipid Res 2008)
- A post hoc review of the safety monitoring board for the torcetrapib trial warns against over-relying on formal statistical stopping rules (Eur J Clin Pharmacol 2008)
- Complexing with spherical HDL protects CETP from mast cell chymase degradation, while CETP reciprocally protects discoidal HDL (J Lipid Res 2008)
- The ILLUMINATE trial halts torcetrapib development after finding a 58 percent rise in death from any cause despite a 72 percent HDL cholesterol increase (N Engl J Med 2007)
- Chiral LC-MS/MS assay separates torcetrapib enantiomers in hamster plasma down to 5 ng/mL (J Chromatogr B 2007)
- Vitamin E supplementation modestly lowers HDL cholesterol in statin-treated patients without affecting CETP or CYP3A activity (Am J Health Syst Pharm 2007)
- CETP Taq1 B2 allele nearly halves ischemic stroke risk in Sardinian women, but not men (J Intern Med 2007)
- CETP activity correlates with insulin resistance and leptin in obese subjects, but not independently of other factors (Metabolism 2007)
- Patients with the highest CETP-driven cholesteryl ester transfer rate had their first heart attack 18 years earlier (J Am Coll Cardiol 2007)
- Torcetrapib cuts postprandial VLDL-1 by 40 percent and reduces its atherogenic cholesteryl-ester content in type IIB hyperlipidemia (Arterioscler Thromb Vasc Biol 2008)
- CETP I405V I-allele carriers respond better to simvastatin, with greater triglyceride and HDL cholesterol improvement (Expert Opin Pharmacother 2007)
- Smoking advances first heart attack by up to 9 years in CETP TaqIB B1 carriers, but not in B2B2 homozygotes (Ann Noninvasive Electrocardiol 2007)
- Self-emulsifying formulation cuts the food effect of torcetrapib from 5-fold to 3-fold in dogs (Int J Pharm 2008)
- Atorvastatin's HDL-raising effect in mice requires CETP expression, proving statins work partly by suppressing CETP (Atherosclerosis 2007)
- A regulatory perspective argues the termination of torcetrapib means future HDL therapies will need preapproval proof of effects on actual disease progression (Am J Cardiol 2007)
- CETP expression boosts macrophage reverse cholesterol transport in mice via the LDL receptor pathway (Circulation 2007)
- Rosuvastatin lowered CETP activity and mass while raising HDL-C in metabolic syndrome patients (Atherosclerosis 2008)
- A chiral HPLC method separates the two torcetrapib enantiomers in hamster plasma down to 0.1 microgram per mL (J Chromatogr B 2007)
- Three newly discovered rat gene loci determine whether human CETP causes severe hypercholesterolemia when expressed as a transgene (J Hypertens 2007)
- A review of CETP inhibition in dyslipidemia finds that the benefit of raising HDL depends heavily on triglyceride-rich lipoprotein levels (Curr Atheroscler Rep 2007)
- CETP TaqIB B1B1 genotype predicts sudden death in type 2 diabetes, an effect independent of its HDL cholesterol impact (Diabetes Care 2007)
- Fenofibrate shifts HDL from large HDL2 to small HDL3 particles over 5 years in type 2 diabetes without changing CETP, PLTP, or LCAT activity (Diabetologia 2007)
- ALPS study finds CETP mass changes track LDL cholesterol, not HDL, with the probucol derivative AGI-1067 (J Clin Lipidol 2007)
- The favorable CETP-VV genotype is found to buffer the deleterious effect of the lipoprotein(a) gene in exceptionally long-lived Ashkenazi Jews (PLoS Comput Biol 2007)
- The RADIANCE 2 trial finds torcetrapib raises blood pressure and HDL but does not slow carotid thickening in mixed dyslipidaemia (Lancet 2007)
- CETP -629C>A genotype effect on HDL cholesterol is only partly explained by its impact on cholesteryl ester transfer activity (Scand J Clin Lab Invest 2008)
- Pioglitazone and rosiglitazone move CETP activity in opposite directions despite similar glucose control (Diabetes Metab Res Rev 2007)
- A review says the CETP crystal structure could enable inhibitors that avoid the nonproductive HDL-binding complex formed by torcetrapib (Curr Opin Cardiol 2007)
- CETP overexpression in transgenic mice does not impair macrophage reverse cholesterol transport or HDL's LDL-antioxidant activity (Atherosclerosis 2007)
- 2D and hologram QSAR models of 85 trifluoro-aminopropanol CETP inhibitors identify key structural drivers of potency (Bioorg Med Chem 2007)
- CETP variants replicate their known HDL cholesterol association in renal transplant patients, but do not predict fluvastatin response (J Lipid Res 2007)
- Elevated CETP levels track with oxidized LDL in dyslipidemic patients (Clin Biochem 2007)
- New fluorescence quencher triples the signal window of a CETP activity assay for large-scale drug screening (Anal Biochem 2007)
- CETP I405V VV genotype cuts myocardial infarction risk in men by 43 percent in the Rotterdam Study (Eur J Cardiovasc Prev Rehabil 2007)
- Review dissects how CETP and PLTP jointly drive low HDL in type 2 diabetes via specific apolipoprotein modulators (Curr Opin Lipidol 2007)
- CETP B1B1 genotype triples coronary artery disease risk in Taiwanese patients with type 2 diabetes (Metabolism 2007)
- Fenofibrate raises HDL cholesterol by up to 91% only in the presence of CETP, via a 72% reduction in hepatic CETP expression, in transgenic mice (J Lipid Res 2007)
- White women with a CETP -629 A/A genotype gain the most HDL cholesterol from 20 weeks of endurance training (Physiol Genomics 2007)
- Chronic CETP deficiency disrupts adipocyte lipid storage, revealing a novel intracellular role for CETP (J Biol Chem 2007)
- The Rotterdam Study links CETP I405V VV genotype to increased Alzheimer's disease risk in APOE4 non-carriers (Neurogenetics 2007)
- The first molecular characterization of avian CETP finds chicken CETP activity rises with dietary cholesterol and falls with egg-laying maturity, likely regulated by estrogen (Comp Biochem Physiol B 2007)
- CETP genotype shows no association with cognitive function or lifetime cognitive change in the Scottish Mental Survey cohort (Neurosci Lett 2007)
- Rare CETP variants, not the common TaqIB marker, best explain the link of the gene to coronary artery disease in 4,811 patients (J Am Coll Cardiol 2007)
- Low serum albumin is the main driver of elevated CETP in children with active nephrotic syndrome (Clin Biochem 2007)
- Psyllium plus plant sterols lowers CETP activity by 11% and raises LDL receptor abundance by 26%, explaining part of its LDL-lowering mechanism (J Nutr 2007)
- CETP expression reverses the obesity caused by apolipoprotein CIII overexpression in transgenic mice (Int J Obes 2007)
- A review argues the torcetrapib failure highlighted the gap between HDL cholesterol levels and HDL anti-inflammatory function (J Clin Lipidol 2007)
- Hepatic lipase and CETP gene variants interact to raise HDL-C, but the combined genotype does not lower cardiovascular risk (J Clin Endocrinol Metab 2007)
- Higher plasma CETP predicts lower cardiovascular event risk specifically in men with low triglycerides, in the PREVEND study (Eur Heart J 2007)
- Review concludes the link between CETP and atherosclerosis risk depends on gene-environment interaction, unlike the direct effects of APOA1 and ABCA1 (Curr Opin Lipidol 2007)
- RADIANCE 1 and 2 are designed to compare torcetrapib plus atorvastatin against atorvastatin alone in over 1,650 patients using carotid ultrasound (Curr Med Res Opin 2007)
- CETP deficiency sharply blunts the post-meal triglyceride spike and remnant lipoprotein formation (Atherosclerosis 2008)
- The ILLUSTRATE trial finds no significant slowing of coronary atheroma progression from torcetrapib despite reaching an LDL-to-HDL ratio below 1.0 (N Engl J Med 2007)
- The RADIANCE 1 trial finds torcetrapib worsens common carotid thickening in familial hypercholesterolemia despite raising HDL to 81.5 mg per dL (N Engl J Med 2007)
- Torcetrapib can raise HDL cholesterol by up to 106 percent alone or combined with atorvastatin, a review of emerging HDL-raising therapies notes (Curr Drug Targets 2007)
- Torcetrapib cuts aortic atherosclerosis by 60 percent in rabbits fed an atherogenic diet, tracking the ratio of total cholesterol to HDL (J Lipid Res 2007)
- Doubling the dose of torcetrapib from 60 to 120 mg turns a modest boost in macrophage cholesterol efflux into a dramatic one (Arterioscler Thromb Vasc Biol 2007)
- A meta-analysis of 23 trials finds HDL-raising tracks with reduced atherosclerosis progression for every drug class except the torcetrapib-atorvastatin combination (J Clin Lipidol 2007)
- Bone marrow-derived CETP alone drives a proatherogenic lipid profile and 1.8-fold more atherosclerosis, and Kupffer cells supply half of hepatic CETP, in LDL receptor knockout mice (Circ Res 2007)
- Tetrazole and ester substituted tetrahydroquinoxalines emerge as a potent new class of CETP inhibitors (Bioorg Med Chem Lett 2007)
- CETP haplotype linked to higher HDL-C across three populations shows no association with coronary heart disease risk (Hum Genet 2007)
- In the Hoorn Study, high CETP concentration more than triples cardiovascular disease risk in women with Type 2 diabetes, with no such association in men (Diabet Med 2007)
- CETP expression protects SR-BI-deficient mice from diet-induced atherosclerosis by remodeling buoyant HDL toward normal density (Arterioscler Thromb Vasc Biol 2007)
- A critical appraisal argues high CETP may actually lower cardiovascular risk when triglycerides are low, complicating the case for CETP inhibition (Eur J Clin Invest 2007)
- First crystal structure of CETP reveals a 60-angstrom tunnel holding four lipid molecules (Nat Struct Mol Biol 2007)
- A review classifies CETP among the HDL-elevating drug targets, distinct from ApoA1-mimetic fast-acting approaches, for treating atherosclerosis (Cardiovasc Hematol Agents Med Chem 2007)
- Serum CETP correlates positively with total cholesterol, beta-lipoprotein, apoB, and apoE, and is lower overall but higher in women, in type 2 diabetes (Med Princ Pract 2007)
- CETP B2B2 genotype protects against acute coronary syndrome only in normal-weight Greeks, not the overweight or obese (Hum Hered 2007)
- CETP TaqIB B2 allele blunts the post-meal fat spike in patients with familial hypercholesterolemia (Clin Chem Lab Med 2007)
- Mini-review places CETP-mediated cholesteryl ester transfer within the broader reverse cholesterol transport pathway (Rom J Intern Med 2007)
- Review asks whether torcetrapib will become the next big advance in coronary heart disease prevention (Curr Atheroscler Rep 2007)
- Hypothesis paper proposes that the ILLUMINATE deaths from torcetrapib trace to eNOS inhibition via HDL-SR-BI signaling loss (Med Hypotheses 2007)
2006 57
- A rare long CETP allele raises coronary artery disease risk nearly 7-fold in Corsican patients (Exp Mol Pathol 2006)
- CETP gene variants predict how much fat monozygotic twins gain during 100 days of deliberate overfeeding (Atherosclerosis 2008)
- A novel CETP splice-site mutation causes isolated high HDL cholesterol in Caucasians, distinct from ordinary hyperalphalipoproteinemia (J Lipid Res 2007)
- A longevity-associated CETP genotype preserves cognitive function in two independent cohorts (Neurology 2006)
- Unlike hepatic lipase and LPL variants, the CETP-HDL cholesterol link is not modified by dietary fat intake in a large biracial cohort (Atherosclerosis 2007)
- Plasma CETP activity tracks hepatic cholesterol synthesis machinery in humanized transgenic mice (Clin Exp Pharmacol Physiol 2006)
- Review of thirteen clinical CETP-inhibition studies finds pharmacological inhibitors raise HDL-C more consistently than vaccines (Curr Med Res Opin 2006)
- A review makes the case for CETP inhibition as a novel strategy to reduce residual atherosclerotic risk beyond statin therapy (Eur Heart J 2007)
- Plasma CETP mass and PLTP activity, but not adiponectin or resistin, are independently linked to leptin levels in type 2 diabetes (Biochim Biophys Acta 2007)
- Dense genotyping of the CETP gene in over 2,000 people pinpoints a promoter SNP at position -4,502 as likely functional for HDL cholesterol (J Lipid Res 2007)
- Torcetrapib alone raises HDL cholesterol by up to 54.5 percent, with less LDL benefit in patients with high triglycerides (J Am Coll Cardiol 2006)
- Adding torcetrapib to atorvastatin raises HDL cholesterol by up to 40 percent with no dose-related rise in adverse events (J Am Coll Cardiol 2006)
- CETP promoter -1337 CC genotype doubles coronary atherosclerosis risk in Japanese familial hypercholesterolaemia patients (Clin Sci 2006)
- Chimeric fusions of CETP with the bacterial-binding protein BPI retain function from both parent proteins up to a threshold (Biochemistry 2006)
- A rapid 6-hour HDL subfractionation method reveals HDL has a dual role in oxidation: CETP-dependent prooxidant during VLDL oxidation, antioxidant during LDL oxidation (J Lipid Res 2007)
- CETP expression amplifies hepatic cholesteryl ester and triglyceride accumulation from apoC-I deficiency by up to 302% in mice (J Lipid Res 2007)
- CETP directly delivers HDL cholesteryl ester to the liver independent of SR-BI and LDL receptor pathways (Biochim Biophys Acta 2006)
- Fenofibrate lowers CETP activity while raising PLTP activity, reshaping apoB-100 kinetics in metabolic syndrome (Clin Sci (Lond) 2006)
- CETP expression multiplies atherosclerotic lesion area 7-fold in the new E3L.CETP mouse model (Arterioscler Thromb Vasc Biol 2006)
- A review describes proof-of-principle preclinical and clinical results for a semi-annual CETP vaccine to raise HDL and address unmet cardiovascular need (Vascul Pharmacol 2006)
- Partial, not complete, CETP inhibition preferentially blocks lipid transfer to LDL while sparing HDL flux (Atherosclerosis 2006)
- Higher plasma CETP concentration, but not CETP genotype, predicts fewer cardiovascular events in pravastatin-treated coronary disease patients (J Intern Med 2006)
- A review previews a large-scale CETP-inhibitor imaging and outcomes program as the next frontier after statin-driven atherosclerosis regression (Can J Cardiol 2006)
- Torcetrapib raises large alpha-1 HDL particles by more than 50 percent in humans, mainly by slowing ApoA-I breakdown (Curr Opin Lipidol 2006)
- Two novel CETP nonsense mutations produce complete deficiency without coronary disease in a Greek pedigree (J Mol Med 2006)
- Mapping the CETP gene reveals seven distinct linkage blocks and yields an optimal set of eleven tagging SNPs for future association studies (Ann Hum Genet 2006)
- Combining three CETP polymorphisms predicts lipid profile better than any single variant in South Indians (Clin Chim Acta 2007)
- CETP expression speeds hepatic uptake of HDL cholesteryl ester but leaves VLDL secretion and biliary cholesterol excretion unchanged in mice (Atherosclerosis 2007)
- CETP is shown to directly drive formation of cholesterol-rich remnant lipoprotein particles, and JTT-705 blocks the effect (Clin Chim Acta 2007)
- Atorvastatin lowers CETP activity and raises paraoxonase without changing HDL cholesterol (Clin Biochem 2006)
- CETP is one of only four genes with consistent lipid effects across sex and race in the CARDIA cohort (Arterioscler Thromb Vasc Biol 2006)
- Adipose-specific CETP expression alone lowers HDL cholesterol and shrinks adipocytes in mice (J Lipid Res 2006)
- Simvastatin lowers cholesterol in cholesterol-fed rabbits without changing CETP activity (Drug Dev Ind Pharm 2006)
- CETP Taq1B B1 allele linked to worse lipid profile and higher blood pressure in kidney transplant patients (Transplant Proc 2006)
- Review surveys recent findings on plasma lipid transfer proteins including CETP's role in HDL delivery and coronary risk (Curr Opin Lipidol 2006)
- A CETP variant that raises HDL cholesterol paradoxically raises coronary risk once HDL-cholesterol is accounted for, large PREVEND study finds (J Clin Endocrinol Metab 2006)
- CETP TaqIB genotype link to HDL-C is stronger in alcohol drinkers than non-drinkers (Atherosclerosis 2007)
- HDL from CETP-deficient people shows 2- to 3-fold greater cholesterol efflux from macrophages via an ABCG1-dependent pathway enriched in LCAT and apoE (J Clin Invest 2006)
- CETP mass is elevated in men, but not women, with metabolic syndrome, and tracks inversely with LDL particle size in both sexes (Obesity 2006)
- Torcetrapib shifts almost entirely into triglyceride-rich lipoproteins in hyperlipidemic human plasma (Pharm Res 2006)
- CETP TaqIB is the only tested genetic system linked to atrial fibrillation, especially when combined with kidney or inflammation markers (BMC Med Genet 2006)
- A DNA vaccine displaying a CETP epitope on hepatitis B core protein cuts aortic lesion area by 80.6% in a rabbit atherosclerosis model (Vaccine 2006)
- CETP expression cuts atherosclerotic lesion size 44% in testosterone-deficient mice (J Lipid Res 2006)
- Torcetrapib alone clears apoB100 faster, but added to atorvastatin it instead cuts LDL and IDL production (Arterioscler Thromb Vasc Biol 2006)
- A review of HDL-raising therapy notes that both JTT-705 and torcetrapib attenuate aortic atherosclerosis in cholesterol-fed rabbits (Pharmacol Ther 2006)
- Torcetrapib can double HDL cholesterol while lowering LDL cholesterol by up to 42 percent, a review of CETP inhibitors reports (Curr Opin Pharmacol 2006)
- ApoE-containing HDL activates LCAT less efficiently than apoA-I-HDL and is remodeled by CETP into large fusion products instead of small lipid-poor particles (J Lipid Res 2006)
- CETP I405V homozygotes for the I allele have significantly less severe coronary artery narrowing (Clin Invest Med 2006)
- Review attributes chronic renal failure's HDL disorders partly to elevated CETP activity (Am J Physiol Renal Physiol 2006)
- Doubling torcetrapib to its maximum tolerated dose more than doubles HDL cholesterol when combined with atorvastatin (Drugs Today 2006)
- A review outlines early evidence that CETP inhibitors JTT-705 and torcetrapib raise HDL and lower LDL cholesterol in mildly dyslipidaemic patients (Expert Opin Investig Drugs 2006)
- Review dissects biochemical pathways beyond HDL-C by which CETP inhibition might protect against atherosclerosis (Arterioscler Thromb Vasc Biol 2006)
- CETP TaqIB rare allele is linked to lower internal carotid artery thickness in men, in the Framingham Heart Study (Atherosclerosis 2006)
- A review traces the CETP-inhibitor rationale from CETP-deficient Japanese populations with high HDL to early human trials of torcetrapib and JTT-705 (J Am Coll Cardiol 2006)
- Review traces how statins raise HDL cholesterol partly via a secondary reduction in CETP activity (Curr Atheroscler Rep 2006)
- Displaying CETP B cell epitopes on asparaginase induces high-titer anti-CETP antibodies lasting over eighteen weeks in mice (Protein Pept Lett 2006)
- A review argues raising HDL with torcetrapib is a promising new approach to atherosclerosis, pending trials with hard clinical endpoints (Recent Pat Cardiovasc Drug Discov 2006)
2005 63
- CETP I405V VV genotype is twice as common in people over 89 as in young adults, and linked to fewer vascular events (Arch Gerontol Geriatr 2006)
- CETP inhibition in rabbits blocks one HDL cholesteryl ester removal pathway but does not compromise overall clearance from plasma (Arterioscler Thromb Vasc Biol 2005)
- Review states the once-promising CETP Taq-I to statin-response link has now been disproved (Vascul Pharmacol 2006)
- Torcetrapib binds CETP roughly 5-fold tighter to HDL, locking it into a nonproductive complex that blocks all major lipid transfer (J Lipid Res 2006)
- CETP D442G mutation raises HDL cholesterol in Vietnamese schoolgirls regardless of nutritional status (Pediatr Res 2005)
- Plasma cholesteryl ester transfer, driven by CETP and triglycerides, predicts carotid intima-media thickness in type 2 diabetes (Diabetes 2005)
- A review finds genetic and plasma CETP-level studies give no clear answer on whether CETP inhibition will reduce atherosclerosis risk (Curr Drug Targets Cardiovasc Haematol Disord 2005)
- Human apoA-I overexpression strips apoC-I from HDL and removes most of HDL's natural CETP-inhibitory capacity in transgenic rats (J Lipid Res 2005)
- A review proposes that CETP is one of four enzymes that remodel spherical HDL into the lipid-poor apoA-I needed for reverse cholesterol transport (Arterioscler Thromb Vasc Biol 2006)
- CETP genotype fails to predict LDL cholesterol response to dietary fat, contradicting earlier studies (Nutr Metab Cardiovasc Dis 2005)
- A chimeric anti-CETP vaccine shrinks aortic plaques by over 40 percent in cholesterol-fed rabbits (Life Sci 2005)
- Omega-3 fatty acid intake correlates with lower CETP activity in Tunisian women with type 2 diabetes (Nutr Metab Cardiovasc Dis 2006)
- Two novel CETP gene variants are found in humans, and torcetrapib inhibits both variant and normal CETP equally (Biochim Biophys Acta 2005)
- Alcohol abuse alters CETP glycosylation, lowering its surface charge and likely its activity (Alcohol Alcohol 2006)
- ApoCI blocks CETP by disrupting CETP-HDL binding through its electrostatic C-terminal helix (J Biol Chem 2005)
- Full gene screening finds 12 novel CETP variants, three of which raise coronary heart disease risk in Chinese patients (Int J Cardiol 2005)
- A review of torcetrapib/atorvastatin combination therapy covers the chemistry, mechanism, and pharmacokinetics behind their complementary lipid effects (Expert Rev Cardiovasc Ther 2005)
- CETP directly delivers HDL cholesteryl ester to the liver through a receptor-independent pathway that torcetrapib only partly blocks (Arterioscler Thromb Vasc Biol 2005)
- The CETP C-629A promoter variant modifies the Alzheimer's disease risk conferred by APOE epsilon4 (J Neurol 2006)
- A high-fat monounsaturated diet blocks cholesterol from stimulating CETP by suppressing LXR-alpha expression, unlike a low-fat diet (J Lipid Res 2005)
- CETP TaqI B1/B2 genotype differs significantly in men with venous thrombosis, tracking their low-HDL/high-LDL profile (Circulation 2005)
- SR-BI processing of HDL2 segregates apoA-I and apoA-II catabolism into distinct particles, independent of CETP, LCAT, or PLTP (J Lipid Res 2005)
- Optimized dibenzodioxocinone derivatives yield low-nanomolar CETP inhibitors stable in rat plasma (Bioorg Med Chem Lett 2005)
- CETP TaqIB and LPL Ser447Ter polymorphisms show no association with ischaemic stroke in Greek patients (Neurosci Lett 2005)
- REGRESS Study identifies three interacting CETP promoter variants that jointly determine plasma CETP concentration (Hum Mol Genet 2005)
- Novel LCAT mutation in a Polish family leaves CETP activity at the low end of normal (Atherosclerosis 2006)
- CETP B2B2 homozygotes gain over ten times more HDL cholesterol from simvastatin than B1 carriers, unlike APOE or LIPC genotypes (Clin Chim Acta 2005)
- LXR agonists raise LDL cholesterol in CETP-expressing hamsters and monkeys, an effect invisible in CETP-lacking mice (J Lipid Res 2005)
- CETP TaqIB genotype shows no link to plaque composition or neointima after carotid endarterectomy, unlike hepatic lipase variant (Atherosclerosis 2005)
- CETP haplotype independently predicts triglyceride response to fluvastatin in familial hypercholesterolemia (Atherosclerosis 2005)
- Review highlights two small-molecule CETP inhibitors substantially raising HDL cholesterol in clinical trials (Curr Opin Cardiol 2005)
- CETP Taq1B B2B2 genotype predicts higher cardiovascular risk despite equal statin response in familial hypercholesterolemia (Eur J Hum Genet 2005)
- CETP TaqI B1B2 genotype triples hypertension risk in North Indian diabetics despite no direct T2DM link (BMC Endocr Disord 2005)
- A CETP-epitope vaccine carried by heat shock protein-65 reduces aortic lesions by up to 30.8% in rabbits (J Cardiovasc Pharmacol 2005)
- ABCG1's discovery as a large-HDL cholesterol exporter suggests CETP inhibition may enhance, not reduce, cholesterol efflux (Curr Opin Lipidol 2005)
- Familial low HDL patients have markedly reduced prebeta-HDL alongside elevated CETP and hepatic lipase activity, unrelated to prebeta-HDL levels (J Lipid Res 2005)
- Type 1 diabetics show enhanced cellular cholesterol efflux and higher CETP activity, and simvastatin lowers HDL cholesterol-linked CETP transfer without boosting efflux further (Diabetologia 2005)
- Adding JTT-705 to pravastatin raises HDL cholesterol by 28 percent after just 4 weeks in a placebo-controlled trial (Am J Cardiol 2005)
- Case report finds significant coronary stenosis in a woman with CETP deficiency and HDL-C of 209 mg/dL (Circ J 2005)
- High triglycerides nearly halve the HDL-raising benefit of a protective CETP promoter variant, large PREVEND study finds (J Clin Endocrinol Metab 2005)
- Clinician update reviews how CETP inhibition raises HDL by 50 to 100 percent in humans but flags mixed results across metabolic contexts (Circulation 2005)
- JTT-705 blocks vascular smooth muscle cell proliferation and angiogenesis through a mechanism independent of CETP inhibition (Atherosclerosis 2005)
- CETP activity rises with the number of diseased coronary vessels in Tunisian type 2 diabetics (Clin Biochem 2005)
- Carotid imaging shows CETP loss-of-function carriers, unlike apoA-I or ABCA1 mutation carriers, have unaltered atherosclerosis progression (Curr Opin Lipidol 2005)
- CETP Taq1B genotype predicts who benefits from cardiac rehabilitation's lipid effects (Atherosclerosis 2005)
- Torcetrapib raises apolipoprotein A-I in alpha1-migrating HDL by up to 382 percent at twice-daily dosing, without changing fecal sterol excretion (Arterioscler Thromb Vasc Biol 2005)
- Review names CETP inhibition as an emerging strategy for HDL-targeted cardiovascular drug development (Nat Rev Drug Discov 2005)
- Lymphocyte gene expression profiling finds CETP expression unaltered in Alzheimer's disease patients (Psychiatr Genet 2005)
- Two independent cohorts find no genetic association between CETP polymorphisms and late-onset Alzheimer's disease (Neurosci Lett 2005)
- CETP variants linked to HDL cholesterol are not the same ones linked to heart attack history, resolving a literature contradiction (Atherosclerosis 2005)
- The CETP 405-valine allele is identified as the first genotype linked to inherited exceptional human longevity (Mech Ageing Dev 2005)
- A review of four lipid transfer proteins highlights the early human results of torcetrapib as opening a new era in coronary heart disease prevention (Atherosclerosis 2005)
- CETP transgenic rats show dramatic lipid shifts on a sucrose diet but not on a high-fat/high-cholesterol diet (Atherosclerosis 2005)
- Torcetrapib inhibits every common CETP genetic variant equally, even the two that are naturally more stable in the body (J Biol Chem 2005)
- 13,677-subject meta-analysis confirms CETP TaqIB drives HDL and CAD risk but does not affect pravastatin response (Circulation 2005)
- Type 2 diabetes eliminates the CETP elevation normally seen in obesity by suppressing hepatic CETP expression (J Clin Endocrinol Metab 2005)
- CETP expression halves atherosclerotic lesion area in non-diabetic LDL-receptor-deficient mice, but this protection disappears with diabetes, another context-dependence finding for the CETP paradox (APMIS 2005)
- CETP B2B2 genotype is more common in diabetics but less common after a heart attack, suggesting a role in identifying diabetic risk (Atherosclerosis 2005)
- High-dose simvastatin lowers CETP activity dose-dependently and normalizes chylomicron remnant clearance in premature CAD (Atherosclerosis 2005)
- ApoCI overexpression backfires as a CETP-blocking strategy by triggering compensatory CETP gene induction (Biochem J 2005)
- A low-fat, low-cholesterol diet lowers CETP activity in type 1 diabetics without harming cholesterol efflux (Scand J Clin Lab Invest 2005)
- Review makes the case for pharmacological CETP inhibition as a therapeutic strategy pending clinical trial confirmation (Curr Top Med Chem 2005)
- CETP I405V and healthy aging link does not replicate in Italian centenarians (Mech Ageing Dev 2005)
2004 50
- CETP Taq1B genotype interacts with obesity in women and predicts small dense LDL in men in a 1029-person Austrian cohort (Biomed Pharmacother 2004)
- Prospective cohort data link elevated CETP concentration to higher cardiovascular risk only when triglycerides are also high (Curr Opin Lipidol 2004)
- Postprandial triglyceride-rich lipoproteins boost CETP-mediated cholesteryl ester transfer from LDL and HDL regardless of dietary fat type (Am J Clin Nutr 2004)
- Review names CETP inhibition as one of the two most important new targets for raising HDL cholesterol (Neth Heart J 2004)
- A moderate-expresser human-CETP transgenic rat model recapitulates female athero-resistance seen in humans (Atherosclerosis 2004)
- CETP activity correlates with HDL triglyceride enrichment and reduced antioxidant capacity in postmenopausal women (Atherosclerosis 2004)
- Torcetrapib 120 mg per day raises HDL cholesterol by 46 percent and lowers LDL cholesterol by 8 percent in subjects with low HDL, a review reports (Expert Opin Investig Drugs 2004)
- A newly characterized CETP promoter variant raises HDL cholesterol specifically in African Americans by weakening a transcription-factor binding site (Clin Genet 2004)
- CETP TaqB1B1 genotype linked to higher LDL cholesterol in Chinese coronary heart disease patients (Chin Med J (Engl) 2004)
- Review weighs CETP inhibition's physiology and animal-to-human evidence as a candidate route to raising HDL cholesterol (Curr Atheroscler Rep 2004)
- Review surveys CETP as a pivotal HDL-raising drug target as human CETP inhibitor data become available (J Lipid Res 2004)
- The EPIC-Norfolk study finds elevated CETP predicts higher future coronary artery disease risk, but only in people with high triglycerides (Circulation 2004)
- A highly variable repeat in the CETP promoter forms unusual DNA structures and predicts HDL-C levels (Biochim Biophys Acta 2004)
- Genome scan finds an LDL-particle-size linkage locus near CETP in familial combined hyperlipidemia families (Arterioscler Thromb Vasc Biol 2004)
- JTT-705 reshapes HDL toward larger, apolipoprotein E-rich particles with more antioxidant enzyme activity in rabbits (Arterioscler Thromb Vasc Biol 2004)
- Adjuvant-free Hsp65-CETP fusion vaccine induces antibodies lasting over 12 weeks and partially normalizes CETP activity in mice (Vaccine 2004)
- The CETP-to-LCAT activity ratio, not either enzyme individually, predicts small HDL3 particle enrichment in healthy Mexican adults (Endocr Res 2004)
- Review confirms CETP promoter variant -629 C to A, not TaqIB, drives CETP activity, and finds no TaqIB-pravastatin pharmacogenetic interaction (Curr Opin Lipidol 2004)
- CETP moves HDL lipids into adipocytes without receptors or endocytosis, overturning the prevailing uptake model (J Lipid Res 2004)
- CETP localizes to germinal centre B cells and their neoplastic lymphoma counterparts (Histopathology 2004)
- Large pharmacogenetic screen finds CETP-HDL response to pravastatin too weak to qualify, unlike the dominant HMG-CoA reductase signal (JAMA 2004)
- Egg-induced cholesterol hyperresponders show higher CETP and LCAT activity than hyporesponders (Metabolism 2004)
- CETP Taq1B B2B2 genotype linked to low HDL cholesterol in Turkish type 2 diabetic patients (Int J Mol Med 2004)
- Electron-withdrawing substituents boost potency in a new propanethioate class of CETP inhibitors, reaching 50 percent inhibition at 2 micromolar (Bioorg Med Chem Lett 2004)
- Daily exercise raises HDL cholesterol most in men with the CETP B1B1 genotype (Clin Genet 2004)
- Review names CETP inhibitors among emerging HDL-targeted therapies for insulin resistance syndrome (Semin Vasc Med 2004)
- Postprandial chylomicrons are up to 40 times more potent than VLDL at accepting cholesterol from LDL and HDL via LCAT and CETP (J Lipid Res 2004)
- Twice-daily torcetrapib doubles HDL cholesterol in the first published proof-of-concept trial of a CETP inhibitor (N Engl J Med 2004)
- SR-BI corrects the atherogenic, cholesteryl-ester-rich HDL seen in CETP deficiency (Atherosclerosis 2004)
- High baseline CETP predicts worse atherosclerosis progression on statins in familial hypercholesterolemia (Atherosclerosis 2004)
- Chemically induced P-407 mouse model of hyperlipidemia indirectly raises CETP activity while directly inhibiting lipoprotein and hepatic lipase (J Cardiovasc Pharmacol 2004)
- Elevated CETP mass helps explain smaller, denser LDL particles in familial hypercholesterolemia (J Lipid Res 2004)
- CETP TaqI B genotype shows no association with late-onset Alzheimer's disease or interaction with APOE4 or lipoprotein lipase (Neurosci Lett 2004)
- CETP TaqIB genotype fails to predict cardiovascular events or pravastatin benefit in the CARE trial cohort (J Am Coll Cardiol 2004)
- CETi-1, AVANT Immunotherapeutics CETP-targeting vaccine, entered Phase II trials for hypercholesterolemia and atherosclerosis by 2001 (Curr Opin Investig Drugs 2004)
- CETP -629A is one of only two individual gene variants, out of 58 tested, that protect against myocardial infarction (Eur Heart J 2004)
- First CETP-specific antibody fragments enable a new quantification assay and link plasma CETP to body fat mass (Clin Chem Lab Med 2004)
- Elderly men carrying a CETP mutation trend toward the lowest heart disease rates in a 7-year Honolulu Heart Program follow-up (J Lipid Res 2004)
- Omega-3 fatty acid concentrate selectively raises HDL2 cholesterol by 40% and paraoxonase by 10% without affecting CETP or LCAT in familial combined hyperlipidemia (Metabolism 2004)
- JTT-705 raises HDL cholesterol in rabbits by speeding up apolipoprotein A-I synthesis, not by slowing its breakdown (Atherosclerosis 2004)
- Combined CETP and ApoA-I genotypes span a 0.54 mmol/L range in HDL-C among Japanese women (Nutr Metab Cardiovasc Dis 2004)
- The first human trial of torcetrapib raises HDL cholesterol by up to 91 percent while producing a lipid profile resembling partial CETP deficiency (Arterioscler Thromb Vasc Biol 2004)
- CETP TaqIB genotype shows no link to preeclampsia or pregnancy lipid profile, unlike apoE (Eur J Obstet Gynecol Reprod Biol 2004)
- Type 2 diabetes lowers CETP specific activity while total CETP mass and activity remain unchanged, unlike PLTP which rises with triglycerides and obesity (Scand J Clin Lab Invest 2004)
- Review reports CETP autoimmunization vaccine has reached human trials alongside apolipoprotein mimetics (Curr Atheroscler Rep 2004)
- Novel CETP L296Q mutation discovered and linked to coronary heart disease and higher LDL cholesterol (Acta Biochim Biophys Sin (Shanghai) 2004)
- Plasma CETP concentration, not TaqIB genotype, predicts atherosclerosis progression and pravastatin benefit in REGRESS (Eur J Clin Invest 2004)
- Review catalogs ten CETP mutations behind hyperalphalipoproteinemia in Japanese CETP-deficient subjects (J Atheroscler Thromb 2004)
- Review positions CETP as a new therapeutic target, noting statins and fibrates already attenuate its activity indirectly (Pharmacol Ther 2004)
- Review examines conflicting evidence on CETP genetic variation and longevity in centenarians (J Atheroscler Thromb 2004)
2003 68
- CETP transgene expression reverses the cholesterol-raising effect of LXR agonists and instead lowers hepatic cholesterol while boosting biliary excretion in mice (J Lipid Res 2004)
- First evidence that CETP Taq1B genotype can guide statin therapy: B2 carriers benefit strongly, B1B1 homozygotes do not (Am Heart J 2003)
- CETP deficiency produces giant HDL particles carrying nearly every major apolipoprotein except apoA-IV (J Lipid Res 2004)
- Rosuvastatin cuts CETP mass 33-37% and, in hypertriglyceridemic patients, transfer activity by 59% (Atherosclerosis 2003)
- CETP activity rises 50% in one ABCA1-heterozygote kindred but not three others, alongside severe HDL abnormalities (Atherosclerosis 2003)
- Review proposes CETP-driven cholesteryl ester transfer as the metabolic link between high triglycerides and low HDL cholesterol in insulin resistance (Eur J Clin Invest 2003)
- Japan CETP Study Group finds CETP activity is the strongest determinant of both HDL-C and LDL-C in 591 subjects (Metabolism 2003)
- Hepatic lipase TT genotype protects against vascular disease only in hemodialysis patients with high CETP levels (Kidney Int 2003)
- Probucol still lowers HDL cholesterol in humans with complete CETP deficiency, disproving its CETP-dependent mechanism (Atherosclerosis 2003)
- A review names CETP among three plasma factors that release lipid-poor apoA-I from HDL during remodeling, the key acceptor for ABCA1-mediated cholesterol efflux (Arterioscler Thromb Vasc Biol 2004)
- Landmark study links large HDL and LDL particle size and the CETP 405 valine allele to exceptional human longevity (JAMA 2003)
- CETP TaqI B polymorphism only modestly raises HDL cholesterol in Saudis, too small an effect to explain their low HDL levels (Clin Sci 2003)
- CETP TaqIB genotype cuts cardiovascular risk 30% in non-smokers but not smokers in WOSCOPS (Eur Heart J 2003)
- Streptozotocin-induced diabetes raises CETP mass and activity in transgenic mice, partly reversed by insulin (Can J Physiol Pharmacol 2003)
- Treating periodontitis raises HDL cholesterol by 10.7% and CETP activity by 19.4%, improving cholesterol efflux especially in patients whose CRP fell (J Lipid Res 2004)
- Oleate-induced negative surface charge on LDL blocks LTIP activity at ten micromolar while only fully suppressing CETP above twenty micromolar (J Lipid Res 2003)
- Review names CETP-driven triglyceride enrichment of HDL as a key mechanism of low HDL in insulin resistance (Clin Biochem 2003)
- CETP expression completely abolishes LXR-agonist-induced HDL enlargement in mice (J Biol Chem 2003)
- LTIP steers CETP's lipid-transfer preference toward HDL3 while keeping HDL2 activity low and constant (J Biol Chem 2003)
- Cholesterol feeding boosts CETP mRNA up to 5-fold via LXRalpha in rabbits before FXR activation catches up (J Lipid Res 2003)
- Intravenous apoA-I/phosphatidylcholine discs raise plasma CETP concentration by 29.7% and cholesterol esterification rate by 69.5% within 12 hours in healthy men (Arterioscler Thromb Vasc Biol 2003)
- Insulin down-regulates CETP gene expression, reversing the elevation seen with insulin deficiency in transgenic mice (J Lipid Res 2003)
- The effect of CETP genotype on HDL cholesterol is unaffected by physical activity level in a population-based Swiss cohort (Med Sci Sports Exerc 2003)
- Phase 1 trial finds a CETP vaccine induces anti-CETP antibodies and is well tolerated in healthy adults (Atherosclerosis 2003)
- Human CETP expression completely prevents diet-induced atherosclerotic lesions in diabetic obese db/db mice (Arterioscler Thromb Vasc Biol 2003)
- CETP -629A allele cuts cardiovascular mortality risk in half in coronary artery disease patients, independent of HDL cholesterol or CETP activity (J Am Coll Cardiol 2003)
- The largest study of its kind finds CETP gene variants are not useful markers for predicting restenosis after angioplasty (J Thromb Haemost 2003)
- Red pepper supplementation lowers CETP activity and improves the lipid profile in cholesterol-fed rabbits (Clin Chim Acta 2003)
- CETP I405V genotype determines whether dietary plant sterols lower cholesterol and CETP concentration (J Nutr 2003)
- Mice and rats lack functional CETP due to a shared ancestral nonsense mutation, not altered regulation (Comp Biochem Physiol B 2003)
- Chiral optimization yields the most potent acyclic CETP inhibitor reported, with an IC50 of 0.77 nanomolar in buffer (J Med Chem 2003)
- Bezafibrate lowers CETP activity by 12% and cholesteryl ester transfer by 37% alongside reduced insulin resistance in hypertriglyceridemia (J Lipid Res 2003)
- Garlic supplementation lowers CETP activity and shrinks atherosclerotic lesions in cholesterol-fed rabbits (Life Sci 2003)
- Single endotoxin dose triggers rapid LDL decline and slower CETP activity loss in healthy volunteers (J Lipid Res 2003)
- A new liposome-based assay shows CETP transfer rate depends jointly on donor AND acceptor surface cholesteryl-ester content, with LDLs varying 1.8-fold in CE-presenting capacity (J Lipid Res 2003)
- A review of HDL structure names CETP among four proteins, alongside LCAT, SR-BI, and ABCA1, that remodel HDL particles in vivo (Front Biosci 2003)
- Short-term hypothyroidism significantly lowers serum CETP concentration but not activity, decoupled from HDL2:HDL3 and LDL-cholesterol correlations seen in controls (Clin Endocrinol 2003)
- Sp1 and Sp3 transcription factors regulate the human CETP gene promoter through three binding sites, with the Sp1/Sp3 ratio determining their relative activity (J Lipid Res 2003)
- JTT-705 (dalcetrapib) inhibits CETP and raises HDL-C across five animal species, mimicking CETP-deficient humans in marmosets (Eur J Pharmacol 2003)
- CETP activity rises 47% in impaired glucose tolerance and correlates with triglycerides, HDL composition, and apoA-I catabolic rate (Croat Med J 2003)
- Patients with atherogenic CETP genotypes get more HDL and triglyceride benefit from high-dose atorvastatin, DALI trial finds (Diabetes Care 2003)
- Full resequencing pinpoints the specific CETP promoter and repeat variants most strongly linked to CETP mass and HDL cholesterol (Atherosclerosis 2003)
- Review surveys CETP as both an unresolved genetic risk marker and a newly validated drug target (Curr Opin Lipidol 2003)
- CETP -629A allele linked to larger LDL particle size in 377 healthy middle-aged men (Atherosclerosis 2003)
- Plant stanol ester spread lowers CETP mass alongside LDL cholesterol and oxidized LDL in a Japanese trial (Nutrition 2003)
- Men who respond strongly to dietary cholesterol also show higher CETP activity during high-egg feeding, suggesting boosted reverse cholesterol transport (J Nutr 2003)
- Haplotype analysis reveals that the famous CETP TaqIB polymorphism is not actually a driver of CETP or HDL cholesterol levels (J Mol Med 2003)
- Meta-analysis of over 10,000 people confirms both CETP TaqIB and I405V variants significantly raise HDL cholesterol (J Lipid Res 2003)
- ApoA-I-free HDL-LpE particles are more than twofold more abundant in CETP-deficient subjects and efflux cholesterol as effectively as apoA-I (J Lipid Res 2003)
- New statistical method for analyzing gene haplotypes is validated using CETP variants and HDL cholesterol data from the REGRESS trial (Ann Hum Genet 2003)
- A newly discovered CETP splice variant in rabbit intestine, and its human counterpart, lacks the lipid-transfer-critical carboxy-end (Mol Cell Biochem 2003)
- Higher CETP activity in Hispanic postmenopausal women tracks with abdominal fat, not ethnicity itself (Metabolism 2003)
- Early phase I and II data show CETP inhibitors raise HDL-C by up to 70 percent, though effects on triglycerides remain unclear (Curr Opin Investig Drugs 2003)
- Only atorvastatin, not fenofibrate, lowers CETP activity in metabolic syndrome patients despite both lowering triglycerides (Diabetes 2003)
- Antisense knockdown of CETP in HepG2 cells raises cholesterol efflux to apoA-I but impairs SR-BI-mediated HDL cholesteryl ester uptake by the liver (Am J Physiol Endocrinol Metab 2003)
- An Alu repeat represses and a CPF binding site activates the human CETP gene's distal promoter (J Lipid Res 2003)
- CETP activity rises 32% after a fatty meal, but neither CETP nor PLTP activity correlates with the postprandial rise in plasma cholesterol efflux capacity (Nutr Metab Cardiovasc Dis 2003)
- Review argues the time is right to test CETP inhibition in randomized human atherosclerosis trials (Arterioscler Thromb Vasc Biol 2003)
- CETP deficiency raises HDL cholesterol in Japanese centenarians but does not affect longevity (J Mol Med (Berl) 2003)
- The inability of rat serum to transfer dietary oxidized cholesterol to LDL/HDL points to CETP as the mediator (J Lipid Res 2003)
- REGRESS study haplotype analysis shows -629C/A, not TaqIB, drives CETP concentration and HDL-C (Hum Mol Genet 2003)
- Tibolone lowers HDL cholesterol by 14% via increased hepatic lipase activity, but preserves cholesterol efflux capacity without affecting CETP activity (Clin Endocrinol 2003)
- CETP expression halves aortic lesion area in ovariectomized mice, an atheroprotective effect blunted by estrogen therapy (J Lipid Res 2003)
- CETP mutations explain most, but not all, cases of extremely high HDL cholesterol in 624 Japanese patients (Atherosclerosis 2003)
- CETP variants cannot explain why Asian Indians have both the highest heart disease rates and lowest HDL cholesterol in Singapore (Clin Genet 2003)
- CETP Taq1B B1B1 genotype independently predicts coronary artery disease in Koreans (Clin Genet 2003)
- CETP gene haplotypes, not individual SNPs, are the first shown to predict lipid response to statin therapy (Pharmacogenomics J 2003)
- Review explains how CETP-mediated cholesteryl ester transfer links low HDL-C to high triglycerides in insulin resistance and type 2 diabetes (Clin Lab 2003)
2002 54
- Review proposes CETP has a novel biological function transporting water-insoluble drugs between lipoproteins (Biochem Pharmacol 2002)
- The Hugh Sinclair Lecture synthesizes how ABCA1, LCAT, CETP, hepatic lipase, and PLTP together remodel HDL, naming CETP inhibition as a resulting therapeutic strategy (Atheroscler Suppl 2002)
- Expressing simian CETP in Fisher rats cuts HDL cholesterol by 48%, selectively depleting large apoE-containing HDL1 particles by 74% (J Lipid Res 2002)
- CETP TaqIB and apoE genotypes interact to shape cholesterol levels in 7-year-old children (Nutr Metab Cardiovasc Dis 2002)
- JTT-705 raises HDL cholesterol but fails to reduce aortic atherosclerosis in rabbits with severe hypercholesterolaemia (Clin Sci 2002)
- In type 1 diabetic children, arachidonic acid content of LDL cholesteryl ester correlates with CETP activity independent of CETP concentration, suggesting a route to excess LTB4 (Med Hypotheses 2002)
- Estradiol fatty-acid esters transfer from HDL to LDL via a CETP-associated process, a review finds, while their broader physiologic roles remain under study (Cardiovasc Res 2002)
- Overexpressing phospholipid transfer protein raises VLDL secretion 1.5-fold while lowering HDL cholesterol and CETP activity in CETP-transgenic mice (J Lipid Res 2002)
- Atorvastatin cuts postprandial CETP-mediated cholesteryl ester transfer from HDL to chylomicrons by up to 26% (J Clin Endocrinol Metab 2002)
- Meal-induced CETP activity redirects HDL cholesterol esters toward atherogenic VLDL-1 particles, rising 32-fold in type IIB hyperlipidemia versus healthy controls (J Lipid Res 2002)
- Antioxidant vitamins blunt the protective HDL2 rise from simvastatin-niacin therapy, possibly by stimulating CETP activity, a review concludes (Arterioscler Thromb Vasc Biol 2002)
- Bariatric-surgery weight loss of 28.7 kg lowers CETP mass 27% and activity 25% in morbidly obese women, alongside an increase in LDL particle size (Arterioscler Thromb Vasc Biol 2002)
- A review reports that apolipoprotein A-II modulates HDL atherogenicity in opposing directions, inhibiting CETP activity as one of several intermediate effects on reverse cholesterol transport (Atherosclerosis 2002)
- Review names CETP inhibitors among five emerging drug targets for lipid disorders beyond statins (Curr Atheroscler Rep 2002)
- High plasma CETP does not speed reverse cholesterol transport in vivo despite raising liver cholesteryl ester uptake (Atherosclerosis 2002)
- Chiral resolution of a trifluoro-3-amino-2-propanol lead reveals a 40-fold potency boost, reaching IC50 0.02 micromolar against CETP (J Med Chem 2002)
- A newly mapped major gene, not CETP or five other known HDL genes, controls large HDL particle levels in baboons (Atherosclerosis 2002)
- Genetic CETP deficiency nearly doubles plasma PLTP concentration by accumulating its inactive form (J Lipid Res 2002)
- Higher-dose atorvastatin cuts CETP-mediated cholesteryl ester transfer 30% while boosting cholesterol efflux in type IIB hyperlipidemia (Atherosclerosis 2002)
- CETP D442G mutation enlarges LDL particle size in coronary heart disease patients, suggesting an antiatherogenic role (Clin Chim Acta 2002)
- LCAT deficiency posttranscriptionally suppresses plasma CETP levels, likely via loss of HDL (Arterioscler Thromb Vasc Biol 2002)
- CETP B2B2 genotype raises HDL cholesterol and particle size specifically in women in the Columbia BioMarkers Study (Nutr Metab Cardiovasc Dis 2002)
- Two newly discovered CETP mutations block protein secretion, explaining more than 60 percent of severe high-HDL cases in Japan (J Lipid Res 2002)
- CETP TaqIB B2B2 genotype replicates its HDL cholesterol and coronary benefit in men with low HDL, VA-HIT trial finds (Arterioscler Thromb Vasc Biol 2002)
- CETP TaqIB B2 allele is less common in African Americans than Caucasians, ruling it out as an explanation for higher HDL-C (Atherosclerosis 2002)
- CETP inhibitory peptide P28 selectively blocks HDL-to-LDL but not HDL-to-HDL cholesteryl ester transfer (Lipids 2002)
- ApoCI deficiency doubles CETP-driven HDL cholesteryl ester depletion in transgenic mice (J Biol Chem 2002)
- D442G CETP mutation raises HDL cholesterol in Korean postmenopausal women but does not alter the HDL response to hormone therapy (Korean J Intern Med 2002)
- CETP Taq1B genotype only predicts HDL cholesterol in obese women with low fasting insulin (Atherosclerosis 2002)
- Review focuses on CETP inhibitors and ABC1-inducing nuclear receptor agonists as new HDL-raising drug approaches (Mini Rev Med Chem 2002)
- Adding CETP shifts lipoproteins toward VLDL and IDL/LDL, and appears to blunt diabetes-driven hyperlipidemia in LPL-deficient mice (J Lipid Res 2002)
- CETP genotype shapes which HDL subfractions rise with endurance exercise training (Metabolism 2002)
- Serum CETP is roughly double in obese children and falls with weight-loss therapy (Obes Res 2002)
- Egg-diet hyperresponder premenopausal women show higher CETP alongside apoB and apoC-III (J Am Coll Nutr 2002)
- The first human trial of JTT-705 finds 900 mg raises HDL cholesterol by 34 percent while cutting CETP activity by 37 percent (Circulation 2002)
- CETP mass varies widely in healthy Japanese people with very high HDL cholesterol (Intern Med 2002)
- HDL from rabbits treated with JTT-705 removes cholesterol from macrophages just as efficiently as normal HDL, despite higher CETP-inhibited levels (Atherosclerosis 2002)
- CETP activity is an independent predictor of LDL particle size in familial combined hyperlipidemia, alongside triglycerides and hepatic lipase (J Lipid Res 2002)
- CETP TaqIB B2 carriers have higher HDL cholesterol but no lower heart attack risk in a large Physicians Health Study cohort (Atherosclerosis 2002)
- Review explains why hypothyroidism keeps HDL normal or high via thyroid-hormone-regulated CETP suppression (Thyroid 2002)
- CETP activity does not predict LDL buoyancy in women, but CETP TaqIB genotype does predict CETP mass and HDL3 cholesterol (Arterioscler Thromb Vasc Biol 2002)
- CETP genotype, like four other candidate genes, fails to predict cholesterol response to plant stanol esters (Eur J Clin Invest 2002)
- Novel CETP promoter variant -971G/A found to be a non-functional marker linked to HDL-C via other polymorphisms (Atherosclerosis 2002)
- CETP I405V, not Taq1B, predicts smaller LDL particle size in Japanese patients (Atherosclerosis 2002)
- CETP inhibitory peptide P28 cuts CETP activity 50% and raises HDL/total-cholesterol ratio 150% in CETP-transgenic mice (J Biochem Mol Biol 2002)
- CETP TaqIB B1B1 genotype independently predicts coronary disease, arteriosclerosis, and stroke in Japanese type 2 diabetics (Diabetes 2002)
- CETP levels are elevated in Chinese heart attack and stroke patients, while CETP-deficient carriers show a favorable lipid profile despite low CETP mass (Chin Med J 2002)
- CETP TaqI B2 allele raises HDL cholesterol more strongly in men than women in a rural Japanese population (J Epidemiol 2002)
- CETP D442G mutation flips its effect in fetal blood, lowering cholesterol instead of raising HDL as it does in adults (Atherosclerosis 2002)
- The first CETP TaqI genotyping in Egyptians finds a B1:B2 allele split of 0.65:0.35, matching the pattern shared by other Arab-descended populations (Eur J Clin Pharmacol 2002)
- Novel splice-site mutation in the CETP gene found in a patient with hyperalphalipoproteinemia (Metabolism 2002)
- Chemical labeling localizes an unpaired active-site cysteine, likely residue 333, whose modification sterically blocks CETP's cholesteryl-ester transfer activity (Chem Phys Lipids 2002)
- Statins should benefit CETP TaqIB B1B1 carriers most, since they have the highest baseline CETP activity (J Atheroscler Thromb 2002)
- CETP promoter and intron 1 SNPs form haplotypes linked to HDL and LDL cholesterol, with sex-dependent strength (Hum Hered 2002)
2001 55
- AICAR lowers blood glucose and insulin by suppressing endogenous glucose production, without correcting dyslipidaemia, in diabetic CETP-expressing KKAy mice (Diabetologia 2001)
- PLTP, not CETP, drives generation of pre-beta HDL in transgenic mice, a 3-fold rise versus CETP-only or wild-type animals (Biochem J 2001)
- Serum CETP concentration falls in postmenopausal Chinese women and correlates positively with estradiol, negatively with FSH (Clin Chim Acta 2001)
- CETP activity runs 2-3 times higher in hyperlipoproteinemia patients, peaking in Type V dyslipidemia (Atherosclerosis 2001)
- CETP EcoN1 GG genotype linked to coronary heart disease risk in a Taiwanese population survey (Atherosclerosis 2001)
- First prospective study finds insulin therapy raises CETP without atherogenic lipid changes (Ann N Y Acad Sci 2001)
- CETP D442G and TaqIB variants track with higher HDL cholesterol in Taiwanese Chinese, but the link weakens with obesity (Hum Genet 2001)
- CETP found directly inside atherosclerotic plaque foam cells, revealing an anti-atherogenic role in cholesterol removal at the earliest step of reverse transport (Atherosclerosis 2001)
- CETP TaqIB B2B2 genotype protects against atherosclerosis only when it actually lowers CETP mass, angiography-based Japanese study finds (Atherosclerosis 2001)
- CETP TaqIB predicts heart attack risk and a 2-year later age of onset, but a linked promoter variant does not, Reykjavik Study finds (Atherosclerosis 2001)
- CETP TaqIB does not predict angiographically documented coronary artery disease risk, large case-control study finds (Clin Genet 2001)
- Review names CETP inhibitors among four novel drug classes targeting low HDL cholesterol (Expert Opin Investig Drugs 2001)
- High-trans-fat margarine trends toward higher CETP levels while lowering cholesterol esterification rate (J Lipid Res 2001)
- CETP-LDL associations are strongest with saturated fat, hinting at why it drives atherogenesis (J Lipid Res 2001)
- The CETP D442G mutation raises HDL cholesterol in adults but not children, first pediatric study of this variant finds (Pediatr Res 2001)
- Psyllium fiber lowers CETP activity 18% regardless of sex, while its triglyceride effects diverge by sex and menopausal status (Am J Clin Nutr 2001)
- Lipid transfer inhibitor protein rises 3-fold in hypercholesterolemia independent of CETP levels themselves (Arterioscler Thromb Vasc Biol 2001)
- HDL cholesteryl esters still reach LDL in ponies despite their total lack of CETP activity (Comp Biochem Physiol B Biochem Mol Biol 2001)
- Early review surveys progress toward antisense and small-molecule CETP inhibitors as HDL-raising therapies (Curr Opin Drug Discov Devel 2001)
- CETP deficiency slows parasite egg development, a possible reason it persists at high frequency across East Asia (Biochem Biophys Res Commun 2001)
- A review by Barter and Rye finds continuing conflict in the evidence on whether cholesteryl ester transfer protein is atherogenic or anti-atherogenic (Curr Opin Lipidol 2001)
- Replacing a tetrafluoroethoxy group with 2-furyl heteroaryl moieties yields submicromolar CETP inhibitors in a new trifluoro-propanol series (Bioorg Med Chem Lett 2001)
- Higher CETP levels roughly halve vascular disease risk in hemodialysis patients with normal or high HDL cholesterol, odds ratio 0.31 (Am J Kidney Dis 2001)
- Combined CETP gene polymorphisms explain up to 10 percent of the variation in carotid intima-media thickness (Eur J Clin Invest 2001)
- CETP activity rises 46% in nephrotic-range proteinuria, contributing to its atherogenic lipoprotein profile (Atherosclerosis 2001)
- Clamp-induced suppression of CETP activity is unrelated to whole-body insulin sensitivity, exercise-training study finds (Metabolism 2001)
- A fructose-enriched diet raises plasma and adipose CETP in hamsters despite lowering, not raising, insulin levels (Life Sci 2001)
- A review identifies apolipoprotein C-I as the major plasma inhibitor of CETP, one of several ways C-I and C-III modulate lipoprotein metabolism (Curr Opin Lipidol 2001)
- CETP TaqIB B2 allele produces a less atherogenic lipid profile and fewer clinical signs in familial hypercholesterolemia (Metabolism 2001)
- Small-for-gestational-age neonates have lower CETP mass but higher cholesteryl ester transfer, possibly explaining later CHD risk (Metabolism 2001)
- CETP transgenic mice reproduce the human-like cholesterol response to dietary fat type, with MUFA and PUFA lowering plasma cholesterol (Br J Nutr 2001)
- Growth hormone replacement transiently lowers CETP concentration and LDL cholesterol together, revealing a shared regulatory link (Lipids 2001)
- A dominant-negative CETP promoter mutation cuts transcriptional activity to 8% of wild type in Japanese hyperalphalipoproteinemia (ATVB 2001)
- Suppressing CETP synthesis in fat cells causes cholesteryl ester to pile up threefold by blocking its normal mobilization (J Biol Chem 2001)
- Immunohistochemistry and in situ hybridization localize CETP production to smooth muscle cells within the human aortic intima and media (Atherosclerosis 2001)
- CETP activity divides six animal species into two groups: low-CETP mouse/rat/dog with high HDL-C, versus high-CETP hamster/rabbit/monkey with low HDL-C (Biol Pharm Bull 2001)
- CETP Ile405Val predicts carotid intima-media thickness in men but not women in the Stanislas Cohort (Clin Genet 2001)
- Thyroid hormone excess doubles CETP activity and accelerates HDL clearance in transgenic mice (Metabolism 2001)
- A hidden CETP gene variant caused false positives in fluorescence-based TaqIB genotyping (Clin Chem 2001)
- CETP TaqIB genotype linked to macroangiopathy risk in Japanese patients with type 2 diabetes (Atherosclerosis 2001)
- Bile-acid feeding represses hepatic CETP expression in male mice but induces it in female mice, revealing a sex-specific regulatory response tied to LRH-1 (J Biol Chem 2001)
- Four CETP-transgenic mouse strains show lipoprotein cholesterol shifting between HDL and LDL in an allelic dose-dependent manner across a 2.9 to 37.4 microg/ml CETP range (Biochem Biophys Res Commun 2001)
- A review finds PLTP, not CETP, is the main driver shaping HDL size and composition via phospholipid transfer and HDL conversion (Atherosclerosis 2001)
- Polyunsaturated fatty acids arachidonic, eicosapentaenoic, and docosahexaenoic halve CETP mRNA expression in HepG2 liver cells (Lipids 2001)
- CETP activity differences do not explain how margarine and butter diets change HDL cholesterol (J Lipid Res 2001)
- A review names PLTP and CETP as joint targets of the nuclear receptors FXR and LXRalpha, central to reverse cholesterol transport (Curr Pharm Des 2001)
- Serum CETP is higher in women and higher still in Chinese myocardial infarction and stroke patients than in healthy controls (Clin Chim Acta 2001)
- Review traces how CETP deficiency reshapes HDL and LDL and raises coronary risk despite higher HDL-cholesterol (Front Biosci 2001)
- CETP TaqIB polymorphism proves noninformative for apo B levels linked to parental heart-attack history (Atherosclerosis 2001)
- Rising triglycerides redirect CETP-mediated cholesterol transfer from LDL toward VLDL1, fueling small dense LDL in type 2 diabetes (Arterioscler Thromb Vasc Biol 2001)
- LDL oxidation redirects CETP transfer backward, pulling cholesteryl ester out of LDL and into HDL instead (Clin Chim Acta 2001)
- Combining apoA-II and CETP transgenes triggers massive VLDL overproduction in mice (J Lipid Res 2001)
- Different dietary fatty acids produce distinct postprandial CETP activity responses in healthy young men (Am J Clin Nutr 2001)
- One week of a high-cholesterol diet paradoxically shrinks myocardial infarct size in CETP-transgenic mice (Coron Artery Dis 2001)
- A methods chapter frames CETP, also known as lipid transfer protein I, as the enzyme linking triglyceride-rich and cholesterol-rich lipoprotein metabolism (Methods Mol Med 2001)
2000 52
- Review details CETP's LBP-gene-family membership and the molecular basis of CETP-deficiency hyperalphalipoproteinemia (Biochim Biophys Acta 2000)
- Review highlights a paradox: CETP-inhibited rabbits show different atherogenicity than genetically CETP-deficient humans (Curr Opin Lipidol 2000)
- CETP TaqIB genotype shows no link to diabetic kidney disease severity in a large type 1 diabetes cohort (Nephrol Dial Transplant 2000)
- CETP activity falls in both growth hormone deficiency and acromegaly, tracking with IGF-1 and adrenal status (Atherosclerosis 2000)
- ApoC-I identified as the natural CETP inhibitor carried on HDL (J Biol Chem 2000)
- A chiral CETP inhibitor binds the protein 5,000-fold more efficiently than its natural lipid substrate (Biochemistry 2000)
- Extra-large HDL particles unique to genetic CETP deficiency may mark reduced atherosclerosis risk (Clin Chim Acta 2000)
- Heterozygous CETP D442G carrier shows apolipoprotein E trapped in HDL at triple the level of other carriers (Clin Chim Acta 2000)
- CETP mutations that lower HDL cholesterol paradoxically cut ischemic heart disease risk 36% in women, Copenhagen City Heart Study finds (Circulation 2000)
- Cys-13, positioned near CETP's neutral-lipid-binding site, is identified as essential for irreversible inhibitor binding via mutagenesis and mass spectrometry (J Lipid Res 2000)
- Phospholipid depletion shrinks reconstituted HDL from 9.2 to 8.0 nm and slows early cholesteryl ester transfer via CETP (J Lipid Res 2000)
- CETP B1B1 genotype predicts a larger cholesterol drop from switching to a low-saturated-fat diet, crossover trial finds (Atherosclerosis 2000)
- A lower CETP B2 allele frequency in Valencia may help explain the unexpectedly high heart disease rate in the region (Atherosclerosis 2000)
- Probucol raises CETP and LCAT activity despite lowering HDL, reframing its HDL reduction as pro-transport rather than atherogenic (Atherosclerosis 2000)
- CETP concentration and transfer activity are normal in well-matched type 1 diabetics, contradicting earlier reports (Eur J Intern Med 2000)
- A review argues CETP-TaqI-B polymorphism data support genetic testing, while cautioning that CETP-inhibitor cardioprotection remains unproven (Clin Chem Lab Med 2000)
- Review makes CETP deficiency the central explanation for hyperalphalipoproteinemia and its paradoxical coronary risk (Atherosclerosis 2000)
- Combining a CETP transgene with PLTP deficiency additively lowers HDL cholesteryl ester and apoA-I in mice, showing no functional redundancy (J Biol Chem 2000)
- Structure-activity studies identify JTT-705 as the optimum CETP inhibitor among a series of disulfide and thioester compounds (J Med Chem 2000)
- In a 24-week RCT, French-press coffee raises CETP activity up to 18% within two weeks, preceding the later rise in LDL cholesterol (J Intern Med 2000)
- A review names CETP, apoA-II, and hepatic lipase as prime targets for pharmacologic inhibition among new HDL-directed atherosclerosis therapies (Curr Atheroscler Rep 2000)
- Hypertriglyceridemia with low HDL cholesterol raises CETP activity and impairs cellular cholesterol efflux capacity in men (Atherosclerosis 2000)
- A CETP-targeting vaccine cuts plasma CETP activity, raises HDL by 42%, and shrinks aortic lesions 39.6% in rabbits (Arterioscler Thromb Vasc Biol 2000)
- CETP I405V genotype, unlike apoB EcoRI variation, does not predict cholesterol response to diet in an Israeli cohort (Atherosclerosis 2000)
- Infants have naturally high CETP activity that is unaffected by thyroid hormone status, unlike prior reports (Metabolism 2000)
- Apolipoprotein L levels rise in primary CETP deficiency and correlate with triglycerides across hyperlipidemic and diabetic subjects (J Lipid Res 2000)
- CETP mass and activity rise significantly after a meal, with the Taq 1B polymorphism predicting who has the lowest levels (Br J Nutr 2000)
- Review concludes CETP's atherogenic effect depends on metabolic background, proposing it as a therapeutic target in hyperlipidemia (Curr Opin Lipidol 2000)
- CETP-HDL relationships differ by sex, and CETP genotype does not explain Israel's low population HDL levels (Atherosclerosis 2000)
- Insulin fails to activate the CETP gene promoter in transfected rat fibroblasts, despite a role for C/EBPalpha (Mol Cell Biochem 2000)
- JTT-705, a disulfide-forming CETP inhibitor, raises HDL cholesterol and slows atherosclerosis in rabbits, the original discovery paper reports (Nature 2000)
- Ten CETP polymorphisms mapped in 568 heart-attack patients reveal alcohol-dependent effects on HDL cholesterol (Genet Epidemiol 2000)
- Feeding, not fasting, raises liver CETP mRNA two-fold and plasma CETP activity 20% in human-CETP transgenic mice, independent of insulin or glucose (J Nutr Biochem 2000)
- Chronic growth hormone replacement lowers CETP activity alongside LCAT, improving the lipoprotein profile (J Lipid Res 2000)
- No CETP mass is detected in human cerebrospinal fluid, unlike LCAT and phospholipid transfer protein (J Lipid Res 2000)
- New CETP promoter repeat marker links the gene to LDL particle size, triglycerides, and apoB in twins (Circulation 2000)
- Duff Memorial Lecture synthesizes how CETP and PLTP knockouts revealed the liver pathways governing HDL catabolism (Arterioscler Thromb Vasc Biol 2000)
- CETP TaqIB B2 allele lowers CHD risk in men in the Framingham Offspring Study (Arterioscler Thromb Vasc Biol 2000)
- Large Copenhagen study shows CETP-mutation-driven HDL elevation actually raises heart disease risk in women, not lowers it (Circulation 2000)
- Red wine, not alcohol alone, raises HDL cholesterol and cholesterol efflux capacity 7% in young men, without altering CETP (Nutr Metab Cardiovasc Dis 2000)
- CETP TaqIB genotype explains major HDL cholesterol differences in renal transplant patients, but only in those without abdominal obesity (Nephron 2000)
- CETP rises over time regardless of whether progestogen is added to low-dose estradiol in diabetic women (Diabet Med 2000)
- CETP genotype combined with apoB signal peptide variant is the strongest predictor of hepatic apoB-100 secretion in obese men (J Lipid Res 2000)
- Prebeta1-HDL concentration tracks LDL-cholesterol independent of CETP mass (Clin Chim Acta 2000)
- CETP and Cyp7a share an LXR-controlled sterol response, coordinating hepatic cholesterol ester catabolism with bile acid synthesis (J Clin Invest 2000)
- Improving glycemic control lowers postprandial CETP activity and chylomicron particle numbers in type 2 diabetes (Atherosclerosis 2000)
- Atorvastatin cuts CETP activity by up to 26.4% while reshaping apolipoprotein distribution in hypertriglyceridemia (Metabolism 2000)
- New CETP/-629 promoter variant lowers CETP mass and raises HDL cholesterol via Sp1/Sp3 repression (ATVB 2000)
- CETP variant R451Q lowers carotid artery thickness in men, while I405V harms only heavy drinkers (Eur J Clin Invest 2000)
- Atorvastatin preferentially reduces CETP-mediated cholesteryl ester transfer from HDL to the largest VLDL subfraction (Arterioscler Thromb Vasc Biol 2000)
- Review argues the role of CETP and reverse cholesterol transport defects in diabetic atherosclerosis remains unproven, despite altered HDL composition (Diabetes Metab Res Rev 2000)
- Blocking CETP-mediated cholesteryl ester transfer with an antibody makes LDL more resistant to oxidative modification (J Lipid Res 2000)
1999 42
- CETP expression cuts aortic lesion area 41% and restores HDL cholesteryl ester clearance in LCAT-transgenic mice with dysfunctional HDL (J Biol Chem 1999)
- Human CETP overexpression in hypertensive Dahl rats spontaneously causes combined hyperlipidemia, myocardial infarction and reduced survival, proving CETP can be proatherogenic (Nat Med 1999)
- Ferroverdins B and C, natural CETP inhibitors from Streptomyces, are elucidated as iron complexes of nitroso-hydroxybenzoate ligands (J Antibiot (Tokyo) 1999)
- VLDL-bound lipoprotein lipase boosts CETP-mediated cholesteryl ester transfer partly independent of its lipolytic action (J Lipid Res 1999)
- Ferroverdin B, isolated from a soil Streptomyces, is among the most potent microbial CETP inhibitors known, with an IC50 of 0.62 micromolar (J Antibiot (Tokyo) 1999)
- A domino Mukaiyama-Michael/Michael/Aldol cyclization efficiently builds pentasubstituted arene cores for potent CETP inhibitors (Angew Chem Int Ed Engl 1999)
- A refined CETP epitope map, built from eight monoclonal antibody binding sites, supports a BPI-based structural model of CETP's overall conformation (Protein Sci 1999)
- LDL acts as a secondary cholesteryl ester donor to chylomicrons via CETP during postprandial lipemia (Atherosclerosis 1999)
- Normal CETP activity in hypertriglyceridemic patients rules out CETP as the cause of reduced LDL receptor binding affinity (Atherosclerosis 1999)
- Mapping a monoclonal antibody's CETP epitope explains why it blocks triglyceride but not cholesteryl ester transfer (J Lipid Res 1999)
- CETP activity is lower in children and teens with insulin-dependent diabetes, alongside higher HDL cholesterol and apoA-I (Acta Paediatr 1999)
- Blocking CETP production in liver cells boosts secretion of the smallest, most protective HDL form (Atherosclerosis 1999)
- CETP TaqIB genotype raises HDL-cholesterol and lowers coronary disease only in men with type 2 diabetes (J Clin Endocrinol Metab 1999)
- An apoE-peptide carrier delivers antisense DNA into cell nuclei, cutting CETP mRNA over 50% and CETP activity to 53.8% of control in CHO cells (Arterioscler Thromb Vasc Biol 1999)
- Abdominal obesity blunts the HDL-raising benefit of the CETP B2 allele in men with insulin resistance features (Int J Obes 1999)
- C/EBP-beta binds the CETP gene promoter in liver cells but does not actually drive CETP expression (Atherosclerosis 1999)
- A review by the LTIP discoverer surveys how CETP expression, atherogenesis and lipid transfer inhibitor protein activity interconnect (Curr Opin Lipidol 1999)
- Insulin lowers CETP activity 9.5% in healthy adults but not in type 2 diabetes, while PLTP responds to both insulin and Acipimox in both groups (Diabetes 1999)
- Pravastatin lowers serum CETP 21% while probucol raises it 23%, with baseline CETP predicting Achilles tendon xanthoma regression (Atherosclerosis 1999)
- A 24-hour intravenous fat load leaves CETP activity unchanged acutely but raises it a week later (J Lipid Res 1999)
- CETP genotype, not insulin sensitivity, predicts how PLTP activity falls during hyperinsulinemia in men (J Lipid Res 1999)
- CETP accounts for 5% of small dense LDL variability in Chinese diabetic patients despite unchanged CETP activity (Atherosclerosis 1999)
- CETP remodeling of HDL boosts SR-BI-mediated cholesteryl ester uptake 2- to 4-fold, synergizing with hepatic lipase in reverse cholesterol transport (J Lipid Res 1999)
- CETP D442G mutation more than doubles vascular disease prevalence in dialysis patients, but only when HDL cholesterol is already low (Kidney Int Suppl 1999)
- A cholesterol response element in the CETP promoter explains why CETP rises, not falls, with cholesterol loading (J Lipid Res 1999)
- A review finds increased plasma CETP is atheroprotective in transgenic mice even with low but functional HDL, against prior assumptions (Atherosclerosis 1999)
- Estrogen raises LDL cholesterol and atherosclerotic lesions in apoB100xCETP transgenic mice without altering CETP activity (Arterioscler Thromb Vasc Biol 1999)
- Probucol and bezafibrate change HDL-cholesterol in cholesterol-fed rabbits via CETP activity, not liver CETP mRNA (Jpn Circ J 1999)
- A new sandwich ELISA measures plasma CETP concentration with under 10% assay variability (Clin Biochem 1999)
- A retinoic acid receptor element is identified in the human CETP gene promoter (Biochem Biophys Res Commun 1999)
- Simvastatin lowers CETP mass and activity by 16 percent in type IIb hyperlipidemia without changing CETP specific activity (Atherosclerosis 1999)
- Human CETP transgene worsens atherosclerosis in apoE- and LDL-receptor-knockout mice, but effect flips with apoA-I overexpression (ATVB 1999)
- LTIP, not CETP itself, explains why cholesteryl ester transfer favors HDL over LDL, overturning a long-held assumption (Arterioscler Thromb Vasc Biol 1999)
- Dietary palmitic acid raises CETP activity and mass versus lauric and oleic acid diets, with opposite effects on PLTP (Atherosclerosis 1999)
- Two CETP variants jointly explain 12 percent of CETP activity variance in a European multi-country cohort, EARS study finds (Eur J Clin Invest 1999)
- CETP, unlike PLTP, rises with hyperlipidemia but stays flat in diabetes, a new ELISA study shows (Arterioscler Thromb Vasc Biol 1999)
- ApoE4 allele blunts the correlation between CETP activity and LDL cholesterol during colestipol and lovastatin treatment (Eur J Clin Pharmacol 1999)
- CETP is expressed early in human preadipocyte-to-adipocyte differentiation, ahead of known adipogenic transcription factors (Atherosclerosis 1999)
- Fungal azaphilones inhibit CETP by forming a covalent bond with a lysine amine, with potency tracking ketone placement on the isochromane ring (J Antibiot (Tokyo) 1999)
- Testosterone suppression by cetrorelix raises apoA-I, insulin, and leptin, with only small CETP and hepatic lipase decreases in pooled analysis (Exp Clin Endocrinol Diabetes 1999)
- Radiolabeled HDL cholesteryl ester lingers longer in rat plasma and clears more slowly from perfused liver after ex vivo CETP treatment (Proc Soc Exp Biol Med 1999)
- Simvastatin, unlike cholestyramine, lowers plasma CETP by 15 percent in primary hypercholesterolemia (Can J Clin Pharmacol 1999)
1998 55
- A review asks whether CETP is beneficial or harmful, weighing evidence for both proatherogenic and antiatherogenic roles (Crit Rev Clin Lab Sci 1998)
- Combined LCAT and CETP action in vitro converts VLDL and LDL into the small, dense particles seen in hypertriglyceridemia (Atherosclerosis 1998)
- High-viscosity pectin lowers plasma CETP activity along with cholesterol in hamsters (J Nutr 1998)
- Pravastatin lowers CETP activity in both fasting and postprandial states in hypercholesterolaemia (Atherosclerosis 1998)
- CETP and PLTP activity, not diabetes itself, drive elevated cholesteryl ester transfer in NIDDM (Atherosclerosis 1998)
- Beta-adrenergic stimulation drives CETP secretion from hamster adipose tissue through a cAMP pathway (Atherosclerosis 1998)
- Ovariectomy reduces CETP activity in liver and adipose tissue of transgenic mice, and hormone replacement fails to restore it (Metabolism 1998)
- SREBP-1 activates the CETP gene in transgenic mice but is not required for its cholesterol-driven up-regulation (J Biol Chem 1998)
- Modeled on BPI's crystal structure, a proposed CETP mechanism has C-terminal residues 461-476 forming a helix that gates lipid entry into a hydrophobic pocket (Curr Opin Struct Biol 1998)
- CETP activity rises in hyperthyroidism and falls in hypothyroidism, tracking free T4, though hepatic lipase drives the HDL2 changes (J Clin Endocrinol Metab 1998)
- Adipose tissue CETP mRNA strongly correlates with plasma CETP levels and falls with age in coronary patients (Atherosclerosis 1998)
- CETP mutation G1533A raises transfer activity and lowers HDL cholesterol, tested with a new simplified assay (Clin Chem Lab Med 1998)
- Low-dose testosterone in women lowers HDL cholesterol without changing CETP activity (Clin Endocrinol 1998)
- Probucol raises CETP mRNA up to 221% and boosts cholesterol efflux 354% in a dose-dependent manner in CETP-transfected hamster ovary cells (Biochim Biophys Acta 1998)
- Erabulenols A and B, new fungal metabolites from a soil Penicillium isolate, inhibit human CETP with IC50 values of 47.7 and 58.2 micromolar (J Antibiot (Tokyo) 1998)
- Erabulenols A and B, fungal CETP inhibitors, share a phenalenone-tetrahydrofuran core, with a hydroxy-methylketonyl benzyl group distinguishing erabulenol B (J Antibiot (Tokyo) 1998)
- Smoking cuts lipoprotein lipase and LCAT activity but leaves CETP activity unchanged, though CETP still tracks HDL3 in non-smokers (Eur J Clin Invest 1998)
- Smoking lowers CETP activity and worsens postprandial HDL loss in normolipidemic men (J Lipid Res 1998)
- Desialylation of lipoproteins boosts CETP-mediated cholesteryl ester transfer from HDL while impairing reverse cholesterol transport (Atherosclerosis 1998)
- CETP-driven cholesterol enrichment of remnant particles worsens atherosclerosis risk in diabetic dyslipidaemia (Eur Heart J 1998)
- CETP preferentially transfers cholesteryl ester over triglyceride when interacting with HDL, independent of its HDL binding (J Biochem 1998)
- Simvastatin lowers plasma CETP only in Japanese patients with elevated baseline CETP levels (Clin Chem 1998)
- CETP mRNA is 96% higher in the immature stromal-vascular fraction of human fat tissue than in mature adipocytes, unlike lipoprotein lipase or apoE (Biochim Biophys Acta 1998)
- A fungal depsipeptide, SCH 58149, shows weak CETP inhibitory activity with an IC50 of 50 micromolar (Bioorg Med Chem Lett 1998)
- Expressing simian CETP in obese diabetic KKAy mice cuts HDL from 159 to 25 mg/dl by enriching HDL with triglyceride 10-fold (Am J Physiol 1998)
- Two hyperalphalipoproteinemia profiles show elevated, not deficient, CETP activity, with differing atherosclerosis risk (Atherosclerosis 1998)
- A young man with familial hypercholesterolaemia is found to also carry heterozygous CETP deficiency (Intern Med 1998)
- Probucol sustains elevated prebeta1-HDL in hypercholesterolemic patients while a low-cholesterol diet lowers it, tracking CETP mass change (Atherosclerosis 1998)
- A bimodal CETP concentration pattern hints at hidden CETP mutations linked to I405V, raising heart disease risk in men with high triglycerides (J Lipid Res 1998)
- CETP B2 allele raises HDL cholesterol in diabetic men, but moderate alcohol intake shows no benefit unlike in non-diabetics (Scand J Clin Lab Invest 1998)
- Blocking apoB mRNA editing doubles plasma apoB-100 and shifts cholesterol from HDL to LDL specifically in CETP transgenic mice (Arterioscler Thromb Vasc Biol 1998)
- Bezafibrate, but not gemfibrozil, significantly lowers cholesteryl ester transfer activity in type IIb hyperlipoproteinaemia (Atherosclerosis 1998)
- An (i, i+4) residue array between His466 and Asp470 stabilizes an amphipathic alpha-helix in CETP's C-terminus (Biochim Biophys Acta 1998)
- Heat-induced loss of plasma gamma-LpE exceeds 80% but is independent of LCAT or CETP activity (J Lipid Res 1998)
- A rare CETP intron 14 mutation, usually found only in Japanese, is identified in a Finnish family with high HDL cholesterol (Arterioscler Thromb Vasc Biol 1998)
- CETP activity stays normal and unchanged with insulin lispro or regular insulin in type 1 diabetes (Metabolism 1998)
- A 28-residue peptide from hog plasma, related to apoC-III, inhibits CETP and clears 75 percent of plasma activity within an hour in vivo (Biochim Biophys Acta 1998)
- A new simple sandwich immunoassay for CETP mass correctly detects genetic CETP deficiency in human serum (Clin Chim Acta 1998)
- Probucol regresses established aortic plaques in hyperlipidemic rabbits and significantly raises CETP activity, likely via antioxidant action (Atherosclerosis 1998)
- Triglyceride enrichment, not CETP alone, is what makes PLTP remodel HDL into larger and smaller particles (J Lipid Res 1998)
- Simvastatin and cholestyramine both lower serum CETP activity in rabbits while leaving LCAT activity essentially unchanged (Cardiovasc Drugs Ther 1998)
- Phage-display screening yields a pentapeptide, WRMWY, that competitively inhibits CETP (J Pept Res 1998)
- Liver-targeted antisense oligonucleotides against CETP suppress atherosclerosis in cholesterol-fed rabbits (J Biol Chem 1998)
- New CETP mutation R451Q raises CETP activity in men but lowers cholesterol in women, a sex-divergent effect (Atherosclerosis 1998)
- First Caucasian North American case of CETP deficiency traced to a novel exon 9 stop mutation (J Lipid Res 1998)
- An overview of reverse cholesterol transport shows CETP pulling in the opposite direction from apoA-I (Eur Heart J 1998)
- Landmark REGRESS trial finds the CETP B1B1 genotype predicts who benefits from pravastatin against coronary atherosclerosis progression (N Engl J Med 1998)
- A review names LCAT, hepatic lipase, and CETP as the key HDL-remodeling enzymes suppressed during cytokine-driven hyperlipidemia (Z Ernahrungswiss 1998)
- Annual Review synthesizes CETP structure, the reverse cholesterol transport hypothesis, and the SREBP-driven regulation of the CETP gene (Annu Rev Nutr 1998)
- CETP Taq1B genotype predicts HDL cholesterol in diabetic patients independent of measured CETP concentration (J Lipid Res 1998)
- Nearly 50,000-subject Japanese study finds no excess coronary heart disease in CETP-deficient people with very high HDL cholesterol (Prev Med 1998)
- CETP preferentially enriches VLDL1 with cholesteryl ester during postprandial lipemia, marking it as atherogenic (Arterioscler Thromb Vasc Biol 1998)
- PLTP shares the same optimal HDL surface charge as CETP, showing both lipid transfer proteins are governed by electrostatics (J Lipid Res 1998)
- Plasma CETP activity rises in hyperthyroidism and falls in hypothyroidism, correcting with treatment (J Clin Endocrinol Metab 1998)
- Vitamin E blocks the CETP-lowering effect of pravastatin and raises CETP concentration on its own (Coron Artery Dis 1998)
1997 45
- Oleic acid roughly doubles full-length CETP transcription in Caco-2 intestinal cells without affecting exon-9-deleted splice variant (Mol Cell Biochem 1997)
- CETP TaqIB genotype predicts opposite lipid responses to a cholesterol-lowering diet in type 1 diabetics (Diabetes 1997)
- A novel CETP nonsense mutation produces a paradoxical combination of very high HDL cholesterol and extreme post-meal triglyceride levels (Arterioscler Thromb Vasc Biol 1997)
- Oleate suppresses LTIP activity over 80%, unleashing maximal CETP-mediated lipid transfer between all lipoproteins including LDL (Arterioscler Thromb Vasc Biol 1997)
- HDL and VLDL levels, not CETP activity, determine the direction of cholesteryl ester transfer in alcohol abusers (Arterioscler Thromb Vasc Biol 1997)
- Lipoprotein-bound free fatty acids drive elevated CETP specific activity in nephrotic syndrome (Arterioscler Thromb Vasc Biol 1997)
- CETP expression suppresses liver LDL receptor mRNA in ApoB/CETP double transgenic mice, reversible by oncostatin M (Arterioscler Thromb Vasc Biol 1997)
- A direct LDL isolation technique offers a simpler alternative for measuring CETP activity (Clin Chim Acta 1997)
- Low-HDL-cholesterol normolipidemic men show a shift from alpha1 to alpha3 HDL subpopulations, possibly via CETP-driven interconversion (Arterioscler Thromb Vasc Biol 1997)
- Acute hyperinsulinemia suppresses plasma CETP activity via a fall in free fatty acids, less so in NIDDM patients than healthy subjects (Metabolism 1997)
- CETP shares seven lipid-binding helical arrays with apoA-I, apoA-II, apoC-I/II/III, and apoE despite a smaller active surface (Mol Cell Biochem 1997)
- LPL activity predicts HDL cholesterol only when CETP is present in mice, revealing a species-specific LPL-CETP interaction (J Lipid Res 1997)
- ApoA-IV 360His variant, not CETP or LCAT activity, explains why some people respond more to dietary fat changes (J Lipid Res 1997)
- A new 1H NMR method tracks CETP-driven lipid transfer in lipoprotein mixtures without ultracentrifugation (NMR Biomed 1997)
- Human apoA-I transgenic mouse HDL lacks the heat-labile inhibitor that normally caps CETP activity at high HDL levels (J Biol Chem 1997)
- An antibody blocking CETP-mediated lipid transfer sharply cuts HDL cholesteryl ester uptake by human adipocytes, revealing a direct CETP-dependent route into fat cells (J Biol Chem 1997)
- A novel transposon-based method sequences 5kb of CETP's 5' regulatory region, revealing a 5.7kb fragment drives far stronger transcription than the minimal promoter (Gene 1997)
- Review contrasts how CETP and PLTP remodel HDL size distribution through distinct mechanisms (Trends Cardiovasc Med 1997)
- CETP deficiency raises HDL-C in familial hypercholesterolemia but fails to prevent coronary disease (Atherosclerosis 1997)
- Chemically blocking a single CETP cysteine residue selectively shuts off triglyceride transfer while leaving cholesteryl ester transfer intact (Biochim Biophys Acta 1997)
- A CETP mutation previously reported only once is surprisingly common in North Americans with high HDL cholesterol (Clin Biochem 1997)
- Exon-14 skipping explains why the common Japanese CETP splicing mutation produces essentially no detectable protein (Arterioscler Thromb Vasc Biol 1997)
- Cholestyramine lowers plasma CETP alongside LDL cholesterol, likely explaining its HDL-raising effect (Clin Pharmacol Ther 1997)
- ApoE-rich HDL is a better CETP substrate than apoA-II-containing HDL, three CETP-deficiency genotypes reveal (J Lipid Res 1997)
- Interferon alpha treatment for hepatitis C lowers CETP activity and mass alongside lipoprotein lipase and hepatic lipase (Hepatology 1997)
- CETP activity enhances plasma cholesteryl ester formation, confirmed in transgenic mice, hamsters, and humans with genetic CETP deficiency (Arterioscler Thromb Vasc Biol 1997)
- Landmark Omagari study first shows CETP-deficiency-driven high HDL cholesterol is not a longevity syndrome (Arterioscler Thromb Vasc Biol 1997)
- CETP gene screening finds no significant link to abdominal aortic aneurysm, ruling it out as a candidate gene (Clin Genet 1997)
- Review surveys the molecular genetics of CETP deficiency and its still-controversial link to atherosclerosis (Curr Opin Lipidol 1997)
- Continuous and cyclic HRT regimens both reshape HDL subclasses in postmenopausal women without altering CETP activity (Atherosclerosis 1997)
- Bile acid sequestrant cholebine shrinks large light LDL without touching CETP or LCAT activity (Atherosclerosis 1997)
- Species already low in CETP and high in lipoprotein lipase respond most to NO-1886, a compound that raises HDL cholesterol without touching CETP activity (Metabolism 1997)
- Intraperitoneal insulin normalizes elevated cholesteryl ester transfer in NIDDM, but injections alone do not (Diabetes 1997)
- Swapping dietary palmitic acid for trans elaidic acid raises CETP activity and lowers HDL more in cebus monkeys (J Nutr 1997)
- CETP gene locus heterogeneity explains why healthy men with low HDL cholesterol carry higher CETP concentrations (ATVB 1997)
- Increased CETP activity tracks with the atherogenic lipoprotein profile of obese children (Atherosclerosis 1997)
- Growth hormone excess raises CETP activity and shifts LDL toward the small dense subfraction in acromegaly (Atherosclerosis 1997)
- Negatively charged surface lipids slow CETP-mediated cholesteryl ester transfer between microemulsion particles, positively charged lipids speed it up (Biochem J 1997)
- CETP incubation shrinks reconstituted HDL from 9.4 to 7.8 nm while raising particle count 50%, the first direct evidence of CETP-driven particle fusion (J Biol Chem 1997)
- CETP activity, not LDL receptor pathways, may explain why LDL cholesterol rises with dietary fat in some people (Curr Opin Lipidol 1997)
- CGS 25159, a synthetic isoflavan CETP inhibitor, cuts VLDL+LDL cholesterol 28% and raises HDL cholesterol 29% in hamsters (Atherosclerosis 1997)
- CETP accounts for 15.2% of HDL cholesterol variation in hypertriglyceridemic men, more than LCAT, lipases, or triglycerides individually (Arterioscler Thromb Vasc Biol 1997)
- Cholesterol feeding raises rabbit CETP production 416% and plasma mass 230%, tracing CETP through fast and slow HDL-bound pools (Arterioscler Thromb Vasc Biol 1997)
- Non-smoking, alcohol-drinking men with the CETP V405 genotype may have up to 40 percent lower heart attack risk, Icelandic study suggests (Clin Genet 1997)
- CETP D442G mutation is found in two families with Lowe syndrome and elevated HDL cholesterol (Acta Paediatr 1997)
1996 48
- Transgenic mice map distinct CETP promoter regions controlling liver, intestine, and adrenal expression (J Biol Chem 1996)
- CETP predicts low HDL cholesterol independent of lipoprotein lipase in hypertriglyceridemic men but not in normotriglyceridemic men (Arterioscler Thromb Vasc Biol 1996)
- Lipopolysaccharides alter both HDL and LDL size and charge while blocking CETP activity, one of three distinct inhibitory mechanisms identified (Biochim Biophys Acta 1996)
- Purified recombinant CETP acts as a lipid carrier with Km of 700 nM for LDL and 2000 nM for HDL, establishing its core kinetic mechanism (Biochem J 1996)
- CETP mass and cholesteryl ester transfer are unchanged in normotriglyceridemic type II diabetics, fasting or fed (Atherosclerosis 1996)
- LpA-I:A-II is an efficient CE donor to triglyceride-rich lipoproteins despite low CETP affinity, fenofibrate raising HDL cholesterol 28% without changing CETP mass (Arterioscler Thromb Vasc Biol 1996)
- Plasma triglyceride level, not dietary fat saturation, is the rate-limiting factor for CETP-mediated cholesteryl ester transfer in hypercholesterolemic women (Atherosclerosis 1996)
- Antibodies raised against CETP residues 131-142 can immunoprecipitate CETP activity from serum without inhibiting the enzyme, marking a non-active-site epitope (Hybridoma 1996)
- A review identifies LCAT and CETP as the two key enzymes driving reverse cholesterol transport, though its antiatherogenic role remains unproven (Can J Cardiol 1996)
- Novel CETP nonsense mutation G181X found in 5 of 294 Japanese hyperalphalipoproteinemic subjects (J Lipid Res 1996)
- A novel intron 10 splice mutation causes exon 10 skipping and disrupts downstream splicing in CETP deficiency (J Lipid Res 1996)
- 13-cis-retinoic acid strongly activates CETP through its negatively charged carboxylic group (Eur J Biochem 1996)
- First demonstration that liver-targeted antisense oligonucleotides against CETP lower LDL and raise HDL in cholesterol-fed rabbits (J Biol Chem 1996)
- CETP and PLTP push HDL particle size in opposite directions, and alcohol withdrawal reveals the effect in patients (J Biol Chem 1996)
- Vitamin E blocks 85% of the HCSF-diet-induced rise in hamster adipose CETP release and 70% of the plasma CETP activity increase (Atherosclerosis 1996)
- A newly found CETP 3-prime-UTR variant lowers CETP activity by nearly 30 percent, replicated in two independent samples (Atherosclerosis 1996)
- CETP gene variation explains one-fifth of the variability in plasma CETP levels, but not HDL cholesterol, family study finds (J Lipid Res 1996)
- Lipoprotein lipase deficiency cuts cholesteryl ester transfer despite normal CETP mass, restored by adding lipoprotein lipase (J Lipid Res 1996)
- Hepatic CETP secretion rises with dietary cholesterol in a dose-dependent, strain-independent manner in rabbits (Comp Biochem Physiol B Biochem Mol Biol 1996)
- HDL3 electronegative charge density, peaking near minus 2,200 esu per square centimeter, governs maximal CETP activity (Biochim Biophys Acta 1996)
- Landmark Honolulu Heart Program study first shows CETP gene mutations raise coronary heart disease risk despite raising HDL cholesterol (J Clin Invest 1996)
- CETP contains an essential free cysteine in a hydrophobic pocket, inactivated by thiol-modifying reagents at nanomolar concentrations (Biochem Biophys Res Commun 1996)
- A review names CETP among four enzyme mutations that reshape HDL particle size and regulate HDL cholesterol and apoA-I levels (Curr Opin Lipidol 1996)
- Adding CETP to apoA-I transgenic mice doubles prebeta-HDL apoA-I and raises cholesterol efflux and LCAT esterification 1.7-fold (J Lipid Res 1996)
- Endotoxin cuts CETP levels below 20 percent of normal in hamsters, partly via TNF and interleukin-1 (J Clin Invest 1996)
- Combined hyperlipidaemia blocks net CETP-mediated cholesteryl ester transfer from HDL to LDL despite elevated CETP mass (Eur J Clin Invest 1996)
- Fenofibrate cuts CETP-driven cholesteryl ester transfer from HDL to VLDL by 38% and normalizes dense LDL (ATVB 1996)
- Net cholesteryl ester transfer roughly doubles in NIDDM even though CETP activity itself is unchanged (Atherosclerosis 1996)
- Exon-9-deleted CETP mRNA yields an inactive protein, while hypercholesterolemia and development favor full-length transcript accumulation (J Biol Chem 1996)
- SW872 liposarcoma cells offer a high-output model for studying cholesterol-driven CETP secretion (J Lipid Res 1996)
- ApoA-IV activates CETP lipid transfer as effectively as apoA-I, binding lipid emulsions with similar affinity (Biochim Biophys Acta 1996)
- N-linked glycosylation, not the N-terminal cysteine, proves essential for CETP lipid-transfer activity in a new Pichia pastoris recombinant expression system (J Lipid Res 1996)
- Analbuminemic patients show elevated CETP activity toward LDL, likely driven by lipoprotein-bound free fatty acids (Arterioscler Thromb Vasc Biol 1996)
- Free fatty acids fluidize the lipoprotein surface, offering a physical explanation for how they modulate CETP activity (Eur J Biochem 1996)
- CETP activity rises 20% postprandially in controls but falls in NIDDM patients, despite 35% higher fasting CETP activity in diabetics (Atherosclerosis 1996)
- CETP activity rises in the second trimester of pregnancy alongside falling hepatic lipase and rising estradiol (J Lipid Res 1996)
- A palmitic acid diet raises CETP activity 12 percent more than a stearic acid diet in young women (Metabolism 1996)
- CETP activity correlates with LDL-cholesterol but not HDL-cholesterol in 586 healthy Japanese adults (Atherosclerosis 1996)
- Polyacetylene compounds isolated from Korean ginseng roots inhibit human CETP (Chem Pharm Bull (Tokyo) 1996)
- Ethanol oxidation, not reduced CETP synthesis, explains alcohol's redistribution of CETP among lipoproteins (ATVB 1996)
- CETP activity, not mass, is elevated in Type 2 diabetes and tracks free cholesterol and apoA-I only in non-diabetic subjects (Atherosclerosis 1996)
- Net cholesteryl ester transfer is elevated in hypertriglyceridemic hemodialysis patients, tracking triglyceride levels rather than renal status (Am J Nephrol 1996)
- A panel of 16 new antibodies maps four distinct CETP regions essential for cholesteryl ester transfer activity (J Lipid Res 1996)
- CETP mediates the transfer of esterified oxysterols between lipoproteins, limiting their uptake into cells (J Lipid Res 1996)
- ApoE or LDL receptor knockout raises hepatic CETP transgene expression eightfold, revealing a cholesterol-sensing mechanism independent of both (J Clin Invest 1996)
- CETP activity exceeds that of adults and control children in kids on peritoneal dialysis for end-stage renal disease (Nephron 1996)
- Review weighs whether cholesterol redistribution by CETP is proatherogenic or a step in protective reverse cholesterol transport (Horm Res 1996)
- Review surveys the biochemistry and molecular basis of CETP deficiency disorders (J Atheroscler Thromb 1996)
1995 56
- ARP-1 acts as both repressor and activator of the CETP gene promoter depending on flanking sequence context, via a defined 105-bp regulatory element (J Biol Chem 1995)
- HDL particles from CETP-transgenic mice are more efficient cholesterol acceptors than from apoA-I-only transgenic mice, despite lower HDL levels (J Clin Invest 1995)
- CETP-mediated cholesteryl ester and triglyceride transfer in plasma is not an equimolar exchange (J Lipid Res 1995)
- CETP mRNA abundance in human adipose tissue tracks membrane cholesterol content, not stored lipid droplet cholesterol (J Lipid Res 1995)
- Gemfibrozil raises HDL3 cholesterol 34.5% and plasma CETP activity 15.8% in hypertriglyceridaemic patients (J Intern Med 1995)
- An apoA-I promoter variant does not affect HDL cholesterol regardless of CETP deficiency status in Japanese subjects (Hum Genet 1995)
- Combined CETP and hepatic lipase deficiency drives atherosclerotic disease in some patients with marked high HDL (Arterioscler Thromb Vasc Biol 1995)
- Plasma triglycerides, not LCAT or CETP concentration, drive cholesterol esterification and HDL remodeling (ATVB 1995)
- Two novel compounds inhibit CETP by distinct mechanisms: U-95,594 competitively blocks all lipid transfer, U-617 selectively and irreversibly blocks CE transfer (Biochemistry 1995)
- A Tall-lab review reconciles CETP deficiency and CETP overexpression both showing antiatherogenic signals, via its role in reverse cholesterol transport (Curr Opin Lipidol 1995)
- In mice, whether CETP protects against or promotes atherosclerosis depends entirely on triglyceride status, protective only when hypertriglyceridemic (J Clin Invest 1995)
- Etophylline clofibrate lowers CETP mass while improving lipoprotein profile in mixed hyperlipidemia (Atherosclerosis 1995)
- Two independent inhibitors reveal separate CETP binding sites for cholesteryl ester and triglyceride transfer, uncoupled in vivo (J Biol Chem 1995)
- Plasma free fatty acids raise CETP mass and HDL-to-VLDL/LDL transfer but not LDL-to-HDL transfer, a directionally selective effect (Arterioscler Thromb Vasc Biol 1995)
- Landmark ECTIM study is the first to show alcohol intake determines whether the CETP B2 allele protects against heart attack (J Clin Invest 1995)
- Pravastatin cuts CETP-mediated cholesteryl ester transfer to LDL by 24 percent in familial hypercholesterolemia without changing CETP mass (Arterioscler Thromb Vasc Biol 1995)
- CETP-deficient humans clear LDL apoB faster, explaining their low LDL despite reduced apoB production (J Clin Invest 1995)
- CETP shuttles oxidized cholesteryl linoleate between LDL and HDL without distinguishing it from the unoxidized form (J Lipid Res 1995)
- The ApoA-IHelsinki mutation lowers HDL cholesterol and cuts CETP activity by 25% in a Finnish kindred (ATVB 1995)
- Smoking lowers and drinking raises HDL2-C and HDL3-C in healthy men, but neither affects CETP or LCAT activity (Jpn Circ J 1995)
- A fluorescence assay tracks CETP-mediated lipid transfer to equilibrium in under 30 minutes, supporting an adsorption-exchange-desorption-diffusion mechanism (Chem Phys Lipids 1995)
- The ratio of CETP mass to HDL3 cholesterol predicts carotid wall thickness better than HDL cholesterol itself (J Mol Med 1995)
- Review questions whether CETP-mediated cholesterol transfer to apoB lipoproteins undermines the antiatherogenic label of reverse cholesterol transport (Atherosclerosis 1995)
- A new immunoassay measuring CETP activity via radiolabeled cholesteryl ester transfer matches the ultracentrifugation method with r=0.94, without separating donor and acceptor lipoproteins (Clin Chem 1995)
- K233 and R259 are essential CETP residues for lipoprotein binding, conserved across the CETP/PLTP/LPS-binding-protein gene family (Biochemistry 1995)
- CETP binds preferentially to the edge of nascent discoidal HDL particles, with affinity boosted 3- to 10-fold by cholesteryl ester or cholesterol content (J Biol Chem 1995)
- A high trans fatty acid diet raises serum CETP activity compared with linoleic or stearic acid diets (Atherosclerosis 1995)
- LDL particles from CETP-deficient patients bind LDL receptors two to three times less avidly than normal LDL (Eur J Clin Invest 1995)
- ApoB/CETP double transgenic mice recreate a human-like lipoprotein cholesterol distribution on chow diet (J Lipid Res 1995)
- CETP mutation 442D:G is found in nearly a third of Japanese with very high HDL cholesterol, including the first documented case with atherosclerosis (Atherosclerosis 1995)
- Oleic acid, unlike linoleic acid, blocks the cholesterol-induced rise in CETP activity in hamsters (Atherosclerosis 1995)
- Simvastatin cuts CETP activity 30 percent in type II hyperlipoproteinemia, but the change is unrelated to lipoprotein subfraction shifts (Atherosclerosis 1995)
- Gemfibrozil enlarges LDL particles and trends toward lowering CETP activity without changing LDL receptor binding (Atherosclerosis 1995)
- Liver-specific CETP transgenic mice show 30-40% lower HDL cholesterol and loss of the apoE-rich HDL1 subclass (Biochim Biophys Acta 1995)
- CETP activity splits into two distinct subgroups among low-HDL men, with the high-CETP subgroup showing only 30% coronary disease prevalence versus 70% (Arterioscler Thromb Vasc Biol 1995)
- A multi-step synthesis from diosgenin yields two novel cholest-15-one steroids tested for CETP-inhibiting activity (Bioorg Med Chem 1995)
- CETP deficiency enlarges apoA-I lipoprotein particles and impairs their cholesterol-handling function (J Lipid Res 1995)
- CETP TaqIB genotype distribution differs significantly between cholesterol gallstone patients and controls (J Lipid Res 1995)
- Antibody-mediated CETP inhibition in hamsters produces apoE-rich, apoA-I-poor HDL particles that revert toward baseline within two weeks (Lipids 1995)
- Endotoxin suppresses CETP via adrenal corticosteroid release, raising HDL in transgenic mice (J Clin Invest 1995)
- Diabetic cynomolgus monkeys show accelerated cholesteryl ester transfer, mirroring human diabetic dyslipidaemia (J Lipid Res 1995)
- New monoclonal-antibody immunoassays quantify CETP mass down to nanogram levels in plasma and cell culture (J Lipid Res 1995)
- Hepatic lipase, insulin, and triglycerides, not CETP or LPL activity, independently predict low HDL2b in men with NIDDM and coronary disease (J Lipid Res 1995)
- CETP and LCAT activity rise postprandially in NIDDM, but neither differs from controls at baseline (Atherosclerosis 1995)
- Palmitic and lauric acid diets do not differ in CETP activity from each other, but lauric acid raises CETP activity above baseline (J Nutr 1995)
- Dietary cholesterol raises both LDL and HDL cholesterol in young women without changing fasting plasma CETP levels (Arterioscler Thromb Vasc Biol 1995)
- Recombinant cynomolgus monkey CETP is expressed and purified 176-fold from CHO cells for structural study (J Protein Chem 1995)
- CETP deficiency yields abnormally large, cholesterol-rich apoA-I lipoprotein particles that bind but internalize poorly (Eur J Biochem 1995)
- Deleting six carboxyl-terminal residues of CETP abolishes cholesteryl ester and triglyceride binding without affecting HDL association (J Biol Chem 1995)
- CETP shrinks reconstituted HDL from 9.2 to 8.0 nm by swapping cholesteryl ester for triglyceride and losing an apoA-I molecule (J Biol Chem 1995)
- A comprehensive Annual Review of Biochemistry synthesis by Alan Tall concludes CETP is dominantly antiatherogenic in vivo despite lowering HDL cholesterol (Annu Rev Biochem 1995)
- A review synthesizes transgenic-mouse evidence that CETP links plasma triglyceride metabolism to low HDL cholesterol levels (Trends Cardiovasc Med 1995)
- CETP activity is 42 percent higher in hypercholesterolemia and correlates strongly with LDL cholesterol (Arterioscler Thromb Vasc Biol 1995)
- CETP is localized to brain astrocytes, with increased expression in Alzheimer's disease gray matter (Acta Neuropathol 1995)
- Adding bezafibrate to long-term probucol therapy can trigger severe HDL and apolipoprotein A-I deficiency (Eur J Clin Pharmacol 1995)
- Molecular genetics reveals CETP as both anti-atherogenic in human deficiency and pro-atherogenic when overexpressed in mice (J Intern Med 1995)
1994 48
- CETP co-expression halves HDL cholesterol and roughly doubles VLDL cholesterol in mice modeling type III hyperlipoproteinemia (J Biol Chem 1994)
- The first competitive ELISA for CETP detects 1 nanogram per well with a coefficient of variation under 6% (Clin Chim Acta 1994)
- CETP transgenic mice develop more severe, faster-progressing fatty liver than controls, worse in males (Biochem Biophys Res Commun 1994)
- Unesterified cholesterol up to 17 mol% speeds CETP-mediated lipid exchange without increasing CETP binding to the donor emulsion (Biochem J 1994)
- A silver-stained PCR-SSCP assay rapidly detects the intron 14 CETP-deficiency mutation without radioactivity (Clin Chem 1994)
- CETP mutations I14A and D442G together explain a graded rise in HDL cholesterol across 226 Japanese patients (J Clin Endocrinol Metab 1994)
- ApoA-II shields HDL from CETP-driven shrinkage by inhibiting hepatic lipase in transgenic mice (J Clin Invest 1994)
- CETP activity is lower in diabetic men without coronary disease than in disease-free non-diabetic men (Metabolism 1994)
- PD 140195, a triazole-thiol CETP inhibitor that mimics cholesteryl ester structurally, works noncompetitively and selectively blocks cholesteryl ester over triglyceride transfer (Lipids 1994)
- Alcohol-induced HDL cholesterol rise is driven by lipoprotein lipase, not CETP, hepatic lipase, or LCAT activity (Atherosclerosis 1994)
- CETP deficiency from two prevalent mutations is identified as the first common genetic cause of high HDL cholesterol in the general population (J Clin Invest 1994)
- Acute hyperinsulinemia lowers plasma CETP activity in diabetic patients but not in healthy subjects (Metabolism 1994)
- A review proposes CETP as the mechanistic switch converting protective HDL2 into atherogenic lipoproteins when triglyceride-rich particles accumulate (Atherosclerosis 1994)
- CETP and LCAT localize mainly to LpA-I, not LpA-I:A-II, particles, a review finds, explaining why LpA-I promotes more cholesterol efflux (Atherosclerosis 1994)
- A monoclonal antibody against CETP raises hamster HDL cholesterol 33% and cuts HDL triglyceride 42% in vivo (Atherosclerosis 1994)
- CETP TaqI B polymorphism predicts CETP activity and HDL cholesterol in non-smoking men, but alcohol and smoking alter the association (Atherosclerosis 1994)
- CETP EcoNI genotype 2-2 predicts higher rates of coronary disease and neuropathy in type 2 diabetes (Clin Genet 1994)
- Antibody-mediated CETP inhibition raises HDL 30 to 40 percent and produces large apoE-rich HDL particles in hamsters, peaking at day 4 (J Lipid Res 1994)
- Review weighs the shuttle versus ternary-complex models for how CETP transfers lipids and flags evidence for a pro-atherogenic role (Clin Exp Pharmacol Physiol 1994)
- Recombination experiments trace accelerated cholesteryl ester transfer in IDDM to a CETP-containing plasma fraction (Eur J Clin Invest 1994)
- CETP mRNA sequences are detected in ovary, lung, intestine, and heart tissue, not just liver, suggesting a locally active membrane-bound CETP form (Biochem Biophys Res Commun 1994)
- Dietary cholesterol raises plasma CETP activity in baboons regardless of dietary fat type (Metabolism 1994)
- Enlarged HDL2 from CETP-deficient patients fails to protect macrophages from cholesterol accumulation (J Biochem 1994)
- Elevated CETP activity, correlated with low HDL, may explain reduced HDL cholesterol in obesity (Arterioscler Thromb 1994)
- CETP triggers dissociation of lipid-free apoA-I from HDL only when VLDL or LDL are also present (J Lipid Res 1994)
- A family study traces complete CETP deficiency to an intron 14 splicing defect found on a routine health check (Intern Med 1994)
- A review names CETP, LCAT, and lipases as the enzymes driving HDL subclass interconversion in mature HDL formation and reverse cholesterol transport (Curr Opin Lipidol 1994)
- Intraperitoneal insulin delivery raises CETP activity 25 percent independent of glucose control in type 1 diabetes (Metabolism 1994)
- A marker linked to the CETP locus shows significant linkage to plasma HDL-cholesterol levels in coronary disease families (Hum Genet 1994)
- Triazine-dye affinity chromatography purifies human CETP up to 100,000-fold from lipoprotein-depleted plasma (Protein Expr Purif 1994)
- ApoA-II binds CETP and shuts down its cholesteryl ester transfer activity while apoA-I and apoA-IV enhance it at low doses (J Lipid Res 1994)
- CETP activity is higher in IDDM patients with macroalbuminuria but does not correlate with HDL, HDL2, or HDL3 cholesterol (Diabetes Care 1994)
- LpA-I-associated CETP concentration is significantly higher in women than men, while hyperlipidemic men shift CETP toward LpA-I:A-II particles (J Lipid Res 1994)
- PTP boosts the cholesteryl ester transfer activity of CETP even though the two proteins move phospholipids by distinct mechanisms (J Lipid Res 1994)
- A bicycle marathon cuts CETP mass 29 percent and activity 14 percent while raising HDL cholesterol (Metabolism 1994)
- Fasting CETP levels rise only on the highest dietary cholesterol dose and track LDL cholesterol changes in young men (Arterioscler Thromb 1994)
- A fast two-site immunoassay measures CETP mass in 6 hours with under 9% assay variability (Clin Chem 1994)
- Bezafibrate suppresses CETP activity by 17% and LCAT by 21% while shrinking small, heavy LDL (Atherosclerosis 1994)
- CETP enriches HDL with triglyceride, accelerating lipolysis-driven apoA-I shedding and shortening apoA-I half-life, explaining low HDL in CETP mice (J Biol Chem 1994)
- CETP TaqIB B2B2 genotype raises HDL2 by 45 percent independent of CETP exchange activity itself (Arterioscler Thromb 1994)
- Trans-elaidic acid raises CETP activity more than cis-oleic acid, correlating with falling HDL cholesterol (Atherosclerosis 1994)
- ApoAII enrichment of HDL3 acts as an uncompetitive inhibitor of CETP-mediated cholesteryl ester transfer (J Biol Chem 1994)
- LpA-I, not LpA-I:A-II, shows an inverse relationship with plasma CETP mass within the HDL3 density region (J Lipid Res 1994)
- CETP TaqI polymorphism predicts HDL cholesterol in Greek but not Italian migrants to Australia (Hum Biol 1994)
- CETP activity peaks in the second trimester of pregnancy and tracks HDL-triglyceride accumulation (Clin Biochem 1994)
- A review identifies probucol as the sole drug shown to stimulate CETP activity and boost reverse cholesterol transport (Pharmacol Ther 1994)
- Cholesterol esterification is 16% slower in Alzheimer's disease, echoing earlier findings in Down's syndrome (Mech Ageing Dev 1994)
- CETP TaqI RFLP frequencies are remarkably uniform across Italian, Greek, and other Caucasian populations (Hum Hered 1994)
1993 33
- CETP expression suppresses hepatic LDL receptor mRNA dose-dependently, explaining apoB-lipoprotein accumulation (J Biol Chem 1993)
- Sodium butyrate induces a 3- to 4-fold rise in CETP mRNA in HepG2 liver cells, a model for CETP hepatic regulation (Eur J Biochem 1993)
- Recombination experiments trace accelerated cholesteryl ester transfer in NIDDM to the VLDL plus LDL fraction (Atherosclerosis 1993)
- Rabbit liver's nonparenchymal cells express more CETP mRNA than the parenchymal cells that dominate most other lipid genes (J Lipid Res 1993)
- Stable-isotope kinetics show CETP deficiency raises HDL by slowing apoA-I and apoA-II catabolism, not by increasing production (J Clin Invest 1993)
- The original discovery of CETP mutation D442G reveals a dominant-negative multimeric mechanism causing threefold HDL elevation in heterozygotes (J Clin Invest 1993)
- Heart transplant recipients' paradoxically high HDL traces to partial CETP and hepatic lipase deficiency (Atherosclerosis 1993)
- A new self-quenching BODIPY-cholesteryl-ester microemulsion assay enables simple fluorescence-based measurement of CETP activity in plasma (J Lipid Res 1993)
- CETP shrinks HDL from 10.3 to 7.6 nm and increases apoA-I catabolic rate 35% in hypertriglyceridemic transgenic mice, revealing the kinetic basis of low HDL (J Clin Invest 1993)
- Horses show no significant cholesteryl ester transfer protein activity despite having VLDL, LDL, and HDL (Comp Biochem Physiol B 1993)
- Nine to twelve months of exercise training lowers plasma CETP concentration by about 14 percent (Arterioscler Thromb 1993)
- An alternatively spliced CETP variant lacking exon 9 sequences blocks secretion of full-length CETP by forming inactive heteromeric complexes (J Biol Chem 1993)
- Gemfibrozil raises HDL3 cholesterol 16% and CETP activity in NIDDM patients, alongside 14.7% and 18.8% rises in LPL and hepatic lipase (Atherosclerosis 1993)
- Pravastatin lowers LDL and raises apoA-I but leaves CETP levels and abnormal HDL subpopulation composition unchanged (Atherosclerosis 1993)
- A natural CETP inhibitor in selectively bred high-HDL baboons is identified as an N-terminal apoC-I fragment that binds apoA-I (J Lipid Res 1993)
- A CETP nonsense mutation at codon 309, detected via macrophage mRNA, is identified as a new cause of familial hyperalphalipoproteinemia (Biochem Biophys Res Commun 1993)
- CETP activity and mass rise in primary biliary cirrhosis, more so with hyperalphalipoproteinemia, correlating tightly with each other (r=0.90) (Hepatology 1993)
- Elevated LCAT and CETP activities help explain abnormal HDL composition in nephrotic-range proteinuria (Kidney Int 1993)
- Landmark Nature paper shows CETP-expressing transgenic mice develop far worse atherosclerosis than non-expressing controls (Nature 1993)
- CHO-cell expression and site-directed mutagenesis show all four potential N-glycosylation sites of CETP are occupied, explaining its glycoprotein doublet on SDS gels (Biochemistry 1993)
- Probucol raises plasma CETP 31% while paradoxically lowering adipose CETP mRNA, suggesting effects beyond local synthesis (J Lipid Res 1993)
- Intron 14 CETP splicing defect is found in 3.5% of Japanese patients with marked hyperalphalipoproteinemia and an estimated 1/42,000 homozygote frequency (Atherosclerosis 1993)
- Review forecasts CETP activity as a promising future pharmaceutical target beyond conventional lipid-lowering (Circulation 1993)
- A polyclonal-antibody immunoradiometric assay detects CETP down to 0.1 nanograms with under 9% variability (J Lipid Res 1993)
- A rapid NdeI-based PCR screen finds the intron 14 CETP splicing defect in 21 of 121 Japanese patients with hyperalphalipoproteinemia (Hum Genet 1993)
- ApoE genotype has opposite effects on CETP and HDL-cholesterol responses to dietary cholesterol (J Lipid Res 1993)
- Simvastatin lowers cholesteryl ester transfer by reducing CETP concentration itself, not by altering HDL (Atherosclerosis 1993)
- A PCR-based site-directed mutagenesis method detects one CETP-deficiency homozygote and three heterozygotes among 554 Japanese subjects (Biochim Biophys Acta 1993)
- ApoE boosts CETP-mediated lipid exchange by raising the affinity of VLDL for CETP (J Lipid Res 1993)
- Bulky hydrophobic residues Leu475, Phe471, Leu468, Phe461 and Phe454 on one face of a C-terminal helix drive CETP's cholesteryl-ester transfer activity, distinct from the antibody-binding face (J Biol Chem 1993)
- CETP activity shows no relation to LDL subfraction composition, unlike lipoprotein and hepatic lipase (Atherosclerosis 1993)
- HepG2 cells secrete an unidentified factor that reshapes nascent HDL into HDL2b particles, with cholesteryl ester transfer detected but not attributable to CETP (J Lipid Res 1993)
- Probucol significantly raises CETP activity while shrinking large LDL and both HDL subfractions (Artery 1993)
1992 23
- CETP generates pre-beta HDL-like particles from alpha HDL, completing a cyclical model with LCAT (J Lipid Res 1992)
- Elevated plasma CETP correlates with cholesteryl ester-enriched VLDL and normalizes with corticosteroid treatment in nephrotic syndrome (J Lipid Res 1992)
- Heavy alcohol drinkers with sky-high HDL show sharply reduced CETP activity and mass, mimicking genetic deficiency (Metabolism 1992)
- C/EBP binds the CETP gene promoter and boosts its reporter-gene activity in liver cells, with C/EBP and CETP mRNA loss occurring in parallel in cultured hepatocytes (J Biol Chem 1992)
- Natural flanking sequences enable dietary cholesterol to boost human CETP gene transcription up to fivefold in transgenic mice (J Clin Invest 1992)
- Deletion mutagenesis pinpoints residues Phe463 to Leu475 as essential for both TP2 antibody binding and CETP's neutral-lipid-transfer activity (J Biol Chem 1992)
- CETP activity is 26% lower in alcoholics, detecting 63% of cases at 82% specificity, but insufficient alone as an alcoholism marker (Alcohol Alcohol 1992)
- CETP drives HDL apolipoproteins A-I and A-II onto LDL particles, an effect greatly amplified by oleic acid (Biochim Biophys Acta 1992)
- CETP crossed with human apoA-I transgenic mice deepens HDL cholesterol loss to 66%, revealing an enhanced human-CETP/human-apoA-I interaction (J Clin Invest 1992)
- CETP reshapes HDL3 differently depending on whether particles carry apoA-II alongside apoA-I (Biochim Biophys Acta 1992)
- A monoclonal antibody that blocks CETP's triglyceride transfer but not cholesteryl-ester transfer suggests the two lipids use distinct binding sites (J Biochem 1992)
- A review by Alan Tall names CETP and hepatic lipase as key genetic determinants of HDL catabolism, with lipoprotein lipase driving HDL formation (J Intern Med 1992)
- Primate CETP transgene dose-dependently depletes large HDL1/HDL2 particles in mice, correlating -0.81 with plasma apoA-I levels (Arterioscler Thromb 1992)
- CETP activity is twofold higher in familial hypercholesterolemia, linked to worse IDL and HDL composition (Horm Metab Res 1992)
- CETP and lipoprotein lipase together, not separately, shrink HDL particles via free fatty acid synergy (Biochim Biophys Acta 1992)
- Baculovirus-expressed CETP deletion mutants pinpoint residues Phe-Leu-Leu-Leu (454-457) as essential for lipid transfer, a motif shared with LCAT, LBP, BPI and other lipid-binding enzymes (Proc Natl Acad Sci U S A 1992)
- A review names LCAT and CETP as the joint enzymatic drivers of reverse cholesterol transport from tissues to the liver (J Am Osteopath Assoc 1992)
- Alcohol abusers have 27 percent lower plasma CETP concentration and 22 percent lower CETP activity than controls (J Lipid Res 1992)
- Trans-elaidic acid increases CETP-mediated cholesteryl ester transfer while cis-oleic acid inhibits it at high concentration (Biochim Biophys Acta 1992)
- The human CETP gene transcript is alternatively spliced to skip exon 9, producing an inactive, poorly secreted protein variant (Biochemistry 1992)
- CETP and hepatic lipase together shed apoA-I from HDL, which reassembles into new discoidal particles (Biochim Biophys Acta 1992)
- ApoA-II blocks CETP-driven conversion of reconstituted HDL into small particles, while apoA-I-only HDL splits into both large and small particles (J Lipid Res 1992)
- CETP is locally synthesized and secreted within the human brain, not just imported from plasma (Int J Clin Lab Res 1992)
1991 22
- CETP activity tracks its own mRNA closely in cholesterol-fed rabbits, while hepatic lipase regulation appears mostly post-transcriptional (Biochim Biophys Acta 1991)
- Homozygous and heterozygous CETP deficiency show graded shifts toward cholesteryl-ester-rich HDL and cholesteryl-ester-poor IDL that track with serum CETP level (Atherosclerosis 1991)
- CETP and PLTP occupy different HDL-sized macromolecular complexes across four vertebrate species (Atherosclerosis 1991)
- Medium and long chain nonesterified fatty acids boost CETP-mediated cholesteryl ester transfer while short chains do not (Biochim Biophys Acta 1991)
- A 50% rise in CETP activity after probucol tracks plasma drug levels and inversely predicts the fall in HDL cholesterol (Eur J Clin Invest 1991)
- Hepatic sinusoidal cells, not hepatocytes, are the principal source of CETP mRNA in primate liver (J Biol Chem 1991)
- CETP deficiency dose-dependently raises HDL2 cholesterol up to sixfold in homozygotes and twofold in heterozygotes (Metabolism 1991)
- First human CETP transgenic mice show that active plasma CETP causally reduces HDL cholesterol (J Biol Chem 1991)
- A review credits probucol as the only drug shown to directly raise CETP activity and mass, potentially aiding cholesterol removal from tissues (Atherosclerosis 1991)
- Linker-insertion mutagenesis maps three CETP regions essential for lipid transfer, at residues 48-53, 165, and 373-379 (Biochemistry 1991)
- A monounsaturated-fat diet lowers CETP activity more than a polyunsaturated diet, paralleling LDL cholesterol reductions (Atherosclerosis 1991)
- CETP activity is 70% higher in smoking IDDM men than controls and 30% higher than nonsmoking IDDM men (Diabetes Care 1991)
- Medium-chain saturated fatty acids boost CETP-driven formation of very small HDL particles, while arachidonic acid blocks it (Biochim Biophys Acta 1991)
- CETP-mediated cholesteryl ester transfer rises with acyl chain length while selective cellular uptake falls, an inverse relationship across four cell types (J Lipid Res 1991)
- Copper-induced plasma oxidation frees CETP from HDL and shifts it onto LDL more sensitively than known oxidation markers (J Lipid Res 1991)
- Plasma CETP rises as an adaptive response to peripheral cholesterol flux and jumps further with probucol treatment (Clin Cardiol 1991)
- Doubling plasma CETP activity via diet does not speed cholesteryl ester clearance from hepatic reticuloendothelial cells in hamsters (Biochim Biophys Acta 1991)
- CETP-deficient patients carry two distinct LDL particle species in every density subfraction, suggesting a second LDL formation pathway (Arterioscler Thromb 1991)
- Probucol raises plasma CETP by 64 percent while lowering HDL cholesterol, consistent with enhanced remnant-pathway reverse cholesterol transport (Arterioscler Thromb 1991)
- Plasma CETP rises up to 85 percent in dysbetalipoproteinemia and severe chylomicronemia, correcting with dietary treatment (Arterioscler Thromb 1991)
- In CETP deficiency, LDL cholesteryl esters trace back to intracellular ACAT rather than CETP-mediated transfer from HDL (J Lipid Res 1991)
- Cloning cynomolgus monkey CETP reveals hepatic mRNA rises fourfold with diet and correlates inversely with HDL cholesterol (ATVB 1991)
1990 19
- A new immunoassay confirms plasma CETP protein, not just activity, is absent in patients with CE transfer deficiency (Clin Chim Acta 1990)
- A symposium report names LCAT and CETP as joint mediators of the Glomset reverse cholesterol transport hypothesis, still clinically unproven (J Lipid Res 1990)
- CETP TaqIB genotype tracks with HDL cholesterol at the population extremes, with the B2 allele enriched among high-HDL subjects (Clin Sci 1990)
- CETP activity falls 15 percent in hypothyroidism, tracking changes in HDL lipid composition (Eur J Clin Invest 1990)
- Alcoholics have 28 percent lower CETP activity than controls, explaining their elevated HDL cholesterol (Eur J Clin Invest 1990)
- A common CETP gene splicing mutation causes markedly elevated HDL in Japan without excess atherosclerosis (N Engl J Med 1990)
- An anti-CETP antibody fully blocks CETP-driven HDL3 size conversion, proving CETP drives structural remodeling beyond lipid transfer (J Lipid Res 1990)
- Sodium oleate disrupts the CETP-mediated LDL-HDL equilibrium, driving cholesteryl esters into a shrunken, lipid-depleted HDL fraction (Atherosclerosis 1990)
- ApoE-rich HDL that accumulates in CETP deficiency binds the LDL receptor with far higher affinity than LDL itself (J Clin Invest 1990)
- The original discovery of the intron 14 splice-site mutation identifies the molecular cause of CETP deficiency in four Japanese families (Biochem Biophys Res Commun 1990)
- CETP and apoA-I gene polymorphisms show no association with coronary heart disease in a Sri Lankan population, though the CETP B1 allele tracks with lower HDL cholesterol (Atherosclerosis 1990)
- CETP-driven lipid transfer from HDL enlarges LDL particles, a candidate mechanism for LDL subfraction polymorphism (J Lipid Res 1990)
- CETP is identical to the mysterious HDL conversion factor, and fatty acids greatly amplify its particle-shrinking effect (Biochim Biophys Acta 1990)
- Hepatic lipase shrinks HDL particles only when VLDL and CETP are both present, and lipoprotein lipase blocks the effect (Atherosclerosis 1990)
- The human CETP gene spans 25 kb with 16 exons and shares a signal-sequence motif with lipoprotein lipase and apoA-I/A-IV (Biochemistry 1990)
- Within three days, an atherogenic diet raises rabbit liver CETP mRNA 2.8-fold and plasma CETP mass 3.2-fold, while other liver mRNAs stay unchanged (J Clin Invest 1990)
- Plasma CETP levels vary nearly fourfold and correlate with apoA-I and apoE, with CETP concentrated in 129-154 kD HDL3/VHDL particles (J Clin Invest 1990)
- CETP locus DNA polymorphism acts as both a level gene for apoA-I and HDL cholesterol and a variability gene for LDL cholesterol (Acta Genet Med Gemellol 1990)
- A single-incubation isotopic assay simultaneously measures LCAT esterification and CETP-mediated cholesteryl ester transfer (Atherosclerosis 1990)
1989 13
- Two Japanese siblings with markedly increased HDL are found homozygous for a CETP intron-14 splice-site mutation eliminating the protein (Nature 1989)
- HDL triglyceride and free cholesterol content noncompetitively inhibit CETP, while HDL apoprotein composition uncompetitively modulates it (J Lipid Res 1989)
- A neutralizing antibody's epitope maps to CETP's C-terminal lipid-binding region, revealing its inhibition mechanism (J Biol Chem 1989)
- CETP retains lipid-transfer activity after protease fragmentation but not as isolated E. coli-expressed fragments, showing no independent catalytic subunit exists (J Biol Chem 1989)
- Inhibiting CETP amplifies apoA-IV and apoE redistribution among lipoproteins during ex vivo plasma incubation (J Lipid Res 1989)
- A neutralizing monoclonal antibody doubles HDL cholesteryl ester in rabbits by blocking CETP in vivo (J Clin Invest 1989)
- A neutralizing anti-CETP antibody eliminates all neutral lipid mass transfer in human plasma, while HDL serves as the main early LCAT substrate (J Clin Invest 1989)
- A twin study introduces the CETP locus as a variability gene that shapes the spread, not the average, of cholesterol levels (Clin Genet 1989)
- Impaired cholesteryl ester transfer to the HDL3 pool is linked to vascular disease across several hyperlipidemic disorders (Atherosclerosis 1989)
- HepG2 hepatocytes secrete CETP activity bound mainly to apoA-I and apoA-II, unlike plasma's strong apoA-I skew, alongside a distinct heat-labile lipid-transfer inhibitor tied to apoE particles (Atherosclerosis 1989)
- A minor pre-beta lipoprotein containing apoD, LCAT, and CETP channels newly esterified cell cholesterol into HDL (J Biol Chem 1989)
- CETP boosts Hep G2 cell uptake of HDL cholesteryl esters indirectly, via LDL receptor-mediated re-uptake of secreted lipoproteins, not directly (J Biol Chem 1989)
- CETP TaqI B polymorphism shows a dosage effect on apoA-I levels, limited to nonsmokers (Clin Genet 1989)
1988 5
- A newly purified phospholipid transfer protein, LTP-II, lacks CETP cross-reactivity but boosts CETP-mediated cholesteryl ester transfer (J Lipid Res 1988)
- Cloning rabbit CETP reveals 81% homology to the human protein and liver-dominant tissue expression across primates and rabbit (J Lipid Res 1988)
- CaCo-2 enterocytes secrete CETP (LTP-I) exclusively from their basolateral surface at twice the rate of HepG2 cells, and uniquely regulate secretion by fatty acid levels (J Biol Chem 1988)
- Neutralizing antibodies against the 74kDa CETP eliminate essentially all plasma cholesteryl ester and triglyceride transfer activity, proving CETP is the responsible protein (J Biol Chem 1988)
- CETP has dedicated binding sites for cholesteryl ester, triglyceride, and phospholipid that let it ferry lipids between particles (J Biol Chem 1988)
1987 8
- Liver Hep G2 cells secrete CETP, acquiring asparagine-linked sugar and sialic acid during processing (J Biol Chem 1987)
- The human CETP gene is first mapped to chromosome 16q12-21 using somatic cell hybrids and in situ hybridization (Genomics 1987)
- The human CETP gene is cloned and sequenced for the first time (Nature 1987)
- The original isolation of the 74kDa human plasma CETP reveals a leucine-rich, highly hydrophobic protein specific for cholesteryl ester over triglyceride transfer (Proc Natl Acad Sci U S A 1987)
- CETP activity and cholesteryl ester transfer rise two- to fourfold in hypercholesterolemic and dysbetalipoproteinemic plasma (J Clin Invest 1987)
- CETP boosts HDL cholesteryl ester uptake into HepG2 liver cells 2.8-fold, the original demonstration of CETP-facilitated selective cellular cholesterol delivery (J Biol Chem 1987)
- Landmark purification establishes human CETP as a unique 74-kDa hydrophobic plasma apolipoprotein (J Biol Chem 1987)
- HepG2 human liver cells synthesize and secrete a protein immunochemically identical to plasma LTP-I, identifying hepatocytes as a candidate source (Arteriosclerosis 1987)
1985 4
- Radiation inactivation puts the functional size of CETP at 70 000 daltons, consistent with a monomer (FEBS Lett 1985)
- Stripping cholesteryl arachidonate from HDL via CETP-mediated transfer reduces its ability to trigger endothelial prostacyclin release (J Lipid Res 1985)
- Lipolysis products bind CETP directly to VLDL remnants and HDL, driving faster cholesteryl ester transfer (J Biol Chem 1985)
- Human but not rat lipoprotein-deficient serum drives cholesteryl ester efflux from cultured arterial smooth muscle cells, implicating CETP in interstitial cholesterol removal (Biochim Biophys Acta 1985)