蛋白酶激活受体-4拮抗剂的研究进展

蛋白酶激活受体-4(PAR-4)是一个由300个氨基酸经过7次跨膜形成的G蛋白偶联受体,它可通过与凝血酶的结合诱导血小板聚集,参与凝血过程。因此,PAR-4受体可以作为抗血小板药物的新靶点。近年来研究者发现了3种不同结构类型的小分子PAR-4受体拮抗剂,分别含有吲唑、吲哚和咪唑并噻二唑结构。对这几种拮抗剂的结构、药理活性等方面的研究进展进行综述。

Research progress on PAR-4 inhibitors

Protease-activated receptor-4 (PAR-4) is a G protein-coupled receptor formed by 300 amino acids through 7 transmembrane. It can induce platelet aggregation by binding to the thrombin, and participate in the process of blood coagulation. As a result, PAR-4 can be considered as a very valuable potential treatment of antiplatelet target. In recent years, three type of small molecules PAR-4 inhibitors, including indazoles, indoles, and imidazothiadiazoles have been developed. Research progress on the structure and pharmacological activities of PAR-4 inhibitors are reviewed in this paper.