Proprotein convertase subtilisin/ kexin type 9 (PCSK9) is a newly discovered serine protease belonging to the pro-protein family. After being synthesized and secreted by the liver, PCSK9 can be transported in conjunction with low density lipoprotein receptor (LDLR) on the cell surface into lysosomes for degrading LDLR, so that the plasma level of low density lipoprotein cholesterol (LDL-C) failed to be degraded due to the receptor deficiency, which resulted in a rise in plasma LDL-C.PCSK9 inhibitors can effectively inhibit the function of PCSK9 to reduce the level of blood lipids suggested a therapeutic target for the treatment of hypercholesterolemia, which can not only reduce the incidence of cardiovascular events together with the adverse reactions, but also can reverse the development of atherosclerosis and coronary heart disease.This review mainly states that the discovery of PCSK9 targets, the function of PCSK9, and the current status of major PCSK9 inhibitors.%前蛋白转化酶枯草溶菌素9(PCSK9)是一种新发现的丝氨酸蛋白酶,属于前蛋白家族,由肝脏合成分泌后,可与细胞表面的低密度脂蛋白受体(LDLR)结合将其转运至溶酶体,降解LDLR,从而使血浆中的低密度脂蛋白胆固醇(LDL-C)水平因受体缺乏无法降解,血浆LDL-C水平升高.PCSK9抑制药可以有效抑制PCSK9的功能达到降低血脂水平的作用,用于治疗高胆固醇血症,可减少不良反应,同时降低心血管事件的发生率,还可以逆转动脉粥样硬化和冠心病的发生发展.该文对PCSK9靶点的发现,PCSK9功能和主要PCSK9抑制药的研究现状进行综述.
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