摘要/Abstract

摘要： [ 摘要 ] 低密度脂蛋白胆固醇 ( LDL-C) 水平升高是心血管疾病的主要危险因素。前蛋白转换酶枯草溶菌素 9（proprotein convertase
subtilisin/kexin type 9，PCSK9）来源于肝细胞，能降解低密度脂蛋白受体，导致肝摄取的胆固醇减少、循环中的 LDL-C 增多。PCSK9
抑制剂能够使肝细胞表面的低密度脂蛋白受体的水平升高，进而结合更多的 LDL-C，从而降低血 LDL-C 的水平。因此，PCSK9 成为
防治心血管疾病、开发新型降脂药物的热门靶点。现主要对 PCSK9 的作用机制及其抑制剂的研发历史、作用机制、体内代谢过程以
及主要临床试验结果进行总结。
关键词: &ensp, 前蛋白转化酶枯草溶菌素 9；低密度脂蛋白受体；心血管疾病；PCSK9 抑制剂；临床试验
Abstract:
Elevated low density lipoprotein cholesterol (LDL-C) is a major risk factor for cardiovascular disease. Studies show that proprotein convertase subtilisin/kexin type 9 (PCSK9) is a circulation enzyme and serves a pivotal function in the degradation of low density lipoprotein receptor, which contributes to the decrease in hepatic cholesterol uptake and increase in circulating LDL-C. PCSK9 inhibitor can significantly elevate the surface of low density lipoprotein receptor of liver cells and bond more LDL-C to decrease the level of LDL-C. Thus PCSK9 has emerged as a popular target for the development of new cholesterol lowering drugs and therapeutic intervention of cardiovascular disease. In this article, the history, mechanism of action, metabolic effects of PCSK9 and the clinical outcomes of PCSK9 inhibitors will be briefly reviewed.
Key words: proprotein convertase subtilisin/kexin type 9 (PCSK9), low density lipoprotein receptor, cardiovascular disease, PCSK9 inhibitor, clinical trial


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