HDL biology
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)
Original title: HDL and Cholesterol Ester Transfer Protein (CETP)
A book chapter on CETP, a clinically important cardiovascular drug target, describing how its high conformational flexibility and tunnel structure allow movement of cholesteryl esters between HDL, VLDL and LDL. The authors summarise research on reverse cholesterol transport showing CETP activity changes cholesteryl ester concentration across lipoprotein classes, and note that animal and cell experiments have given controversial results: inhibiting CETP is reported to fight atherosclerosis by raising plasma HDL-C, while others claim CETP itself weakens atherosclerosis formation by promoting reverse cholesterol transport. The chapter states CETP-targeted drugs remain immature, with CETP inhibitor research focused on improving efficacy and reducing adverse reactions, and notes CETP agonists have also been studied as an anti-atherosclerotic approach. A general textbook-style overview rather than a report of new data.
Original abstract
Cholesterol ester transfer protein (CETP) is important clinically and is one of the major targets in cardiovascular disease studies. With high conformational flexibility, its tunnel structure allows unforced movement of high-density lipoproteins (HDLs), VLDLs, and LDLs. Research in reverse cholesterol transports (RCT) reveals that the regulation of CETP activity can change the concentration of cholesteryl esters (CE) in HDLs, VLDLs, and LDLs. These molecular insights demonstrate the mechanisms of CETP activities and manifest the correlation between CETP and HDL. However, animal and cell experiments focused on CETP give controversial results. Inhibiting CETP is found to be beneficial to anti-atherosclerosis in terms of increasing plasma HDL-C, while it is also claimed that CETP weakens atherosclerosis formation by promoting RCT. Currently, the CETP-related drugs are still immature. Research on CETP inhibitors is targeted at improving efficacy and minimizing adverse reactions. As for CETP agonists, research has proved that they also can be used to resist atherosclerosis.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.