蛋白酶激活受体拮抗剂在抗血小板领域的研究进展  

Research progress on protease-activated receptor antagonists in the field of antiplatelet

作　　者：李杉杉[1] 朱雄[1] LI Shanshan;ZHU Xiong(China Pharmaceutical University,Nanjing 210009,China)

机构地区：[1]中国药科大学

出　　处：《药学研究》2019年第9期543-549,共7页Journal of Pharmaceutical Research

摘　　要：蛋白酶激活受体(protease activated receptors,PARs)是G蛋白偶联受体的家族成员之一。研究发现蛋白酶激活受体可经凝血酶激活诱导血小板的聚集,参与血栓形成过程。人类血小板主要表达蛋白酶激活受体-1和蛋白酶激活受体-4两种受体,因此蛋白酶激活受体-1和蛋白酶激活受体-4可作为抗血小板药物的新靶点。本文介绍了凝血酶诱导蛋白酶激活受体-1、蛋白酶激活受体-4活化的作用机制,并对近年来蛋白酶激活受体-1和蛋白酶激活受体-4小分子拮抗剂的结构、药理活性的研究进展进行总结。Protease-activated receptors(PARs)are members of G-protein coupled receptors.In recent years,researchers have found that PARs can induce platelet aggregation via thrombin activation and participate in the thrombosis process.Human platelets mainly express PAR-1 and PAR-4,which may serve as new targets for antiplatelet drugs.This article summarized mechanism of thrombin-induced PAR-1 and PAR-4 activation,and advances in research on structure and pharmacological activities of small molecule antagonists of PAR-1 and PAR-4 were also reviewed.

关 键 词：蛋白酶激活受体 凝血酶 抗血小板药物 蛋白酶激活受体-1 蛋白酶激活受体-4 拮抗剂 

分 类 号：R972[医药卫生—药品]