论文部分内容阅读
胆固醇酯转移蛋白(CETP)在脂蛋白之间转运中性脂肪,导致胆固醇酯从高密度脂蛋白(HDL)向极低密度脂蛋白(VLDL)和低密度脂蛋白(LDL)的净迁移。CETP在血浆HDL代谢中发挥着非常重要的作用,血浆HDL水平与冠心病(CHD)的发生和发展密切相关。基于流行病学和动物实验的研究结果,抑制CETP被认为是CHD预防和治疗的潜在靶标。CETP抑制剂的临床研究也证实了这一点。文中对近年来进入临床研究中的CETP抑制剂、合成的CETP抑制剂、天然产物来源和生物技术来源的CETP抑制剂进行了综述。
Cholesteryl ester transfer protein (CETP) transports neutral fats between lipoproteins, resulting in a net migration of cholesterol esters from high density lipoproteins (HDLs) to very low density lipoproteins (VLDLs) and low density lipoproteins (LDLs). CETP plays a very important role in plasma HDL metabolism. Plasma HDL levels are closely related to the occurrence and development of coronary heart disease (CHD). Based on the results of epidemiological and animal studies, inhibition of CETP is considered as a potential target for the prevention and treatment of CHD. Clinical studies with CETP inhibitors also confirm this. In this paper, CETP inhibitors, synthetic CETP inhibitors, natural product sources and biotechnology-derived CETP inhibitors that have entered clinical trials in recent years are reviewed.