Beijing Tiantan Hospital, China National Clinical Research Center for Neurological Diseases, Advanced Innovation Center for Human Brain Protection, The Capital Medical University, Beijing, China.
McGill University, Montreal, QC, Canada.
Adv Exp Med Biol. 2022;1377:13-26. doi: 10.1007/978-981-19-1592-5_2.
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.
胆固醇酯转移蛋白（CETP）在临床上很重要，是心血管疾病研究的主要靶点之一。由于具有高度的构象灵活性，其隧道结构允许高密度脂蛋白（HDL）、极低密度脂蛋白（VLDL）和低密度脂蛋白（LDL）自由运动。关于胆固醇逆向转运（RCT）的研究表明，CETP 活性的调节可以改变 HDL、VLDL 和 LDL 中胆固醇酯（CE）的浓度。这些分子见解表明了 CETP 活性的机制，并显示了 CETP 与 HDL 之间的相关性。然而，针对 CETP 的动物和细胞实验得出了相互矛盾的结果。抑制 CETP 被发现有利于增加血浆 HDL-C 以抗动脉粥样硬化，而也有研究声称 CETP 通过促进 RCT 来减弱动脉粥样硬化的形成。目前，CETP 相关药物还不成熟。CETP 抑制剂的研究旨在提高疗效和最小化不良反应。至于 CETP 激动剂，研究已经证明它们也可以用于抵抗动脉粥样硬化。
