胆固醇酯转移蛋白小分子抑制剂的研究进展

Recent progress on developing cholesterol ester transfer protein inhibitors

胆固醇酯转移蛋白(CETP)通过介导脂质在不同脂蛋白之间的转运,调节脂代谢。抑制CETP的转运活性,可提高高密度脂蛋白胆固醇(HDL-c)水平,因而CETP抑制剂有望发展成为新型的治疗心血管疾病的药物。该文按照结构类型对近年来文献报道的代表性小分子CETP抑制剂进行综述。

Cholesterol ester transfer protein （CETP） plays a major role in lipoprotein metabolism by facilitating the transfer of cholesterol esters from high-density lipoprotein （HI）L） to low-density lipoprotein （LDL） in exchange for triglyceride. The fact that inhibition of CETP could cause an increase in HDL-c led to structurally diverse CETP inhibitors developed. Herein, an array of small-molecule CETP inhibitors is summarized on the basis of their structural features.