抗血栓新药糖蛋白GPⅡb/Ⅲa受体拮抗剂研究近况

Glycoprotein Ⅱb/Ⅲa Receptor Antagonists, Novel Antithrombotic Drugs in Development

糖蛋白GP Ⅲb/Ⅲa在血小板表面上的功能表达是血小板抑制剂的最终作用部位。GP Ⅱb/Ⅲa可以与纤维蛋白原桥联而导致血小板凝集。拮抗剂能有效地阻断这一步骤而起拮抗血栓作用。与von Willebrand因子(vWF)或凝血因子Ⅷ的结合是血小板凝集中的重要步骤。本文综述了7E3Fab(abciximab),SK &F106760,蛇毒多肽,及RGD肽类和拟肽等GPⅡb/Ⅲa拮抗剂的药理研究近况。

The functional expression of glycoptotein Ⅱb/Ⅲa on the platelet surface plays a critical role in platetet aggregation. GP Ⅱb/Ⅲa ligates fibrinogen to platelets together and results in platelet aggregation. GP Ⅱb/Ⅲa antagonists can block this step and stop the platelet aggregation. In this review, antagonists of GP Ⅱb/Ⅲa, such as 7E3Fab (abciximab), SK&F106760, disintegrins, peptides containing Arg—Gly—Asp (RGD) and non—peptide RGD mimetics are discussed, and the future researchs on GP Ⅱb/Ⅲa àntagonists are considered, too.