PCSK9抑制剂多效性研究进展

Pleiotropic Effects of PCSK9 Inhibitors

前蛋白转化酶枯草溶菌素9(PCSK9)是一种主要由肝脏合成的分泌型丝氨酸蛋白酶,通过结合低密度脂蛋白受体促进其降解,从而减少低密度脂蛋白胆固醇的清除。PCSK9抑制剂是一种新型降脂药,主要通过与PCSK9结合而抑制其上述生理作用。近年来,越来越多的研究表明PCSK9抑制剂除降脂之外还有许多其他的作用。现主要针对其降脂之外的抗炎、抗动脉粥样硬化、抗血小板聚集与抗血栓形成以及抗肿瘤等作用进行综述。

Proprotein convertase subtilisin/kexin type 9(PCSK9),a secretory serine protease mainly synthesized by the liver, promotes the degradation of low density lipoprotein receptor after binding to the receptor, and reduces the clearance of low-density lipoprotein cholesterol.PCSK9 inhibitors constitute a new class of lipid-lowering drugs, of which main mechanism is binding to PCSK9 and inhibiting the above-mentioned physiological effects.Recently, abundant evidence has elucidated the pleiotropic effects of PCSK9 inhibitors beyond lipid-lowering.This review focuses on the pleiotropic effects of PCSK9 inhibitors independent of lipid-lowering, such as anti-inflammatory effect, anti-atherosclerotic effect, anti-platelet aggregation effect, anti-thrombotic effect and antineoplastic effect.