Hamilton Justin R
Australian Centre for Blood Diseases, Monash University L6, 89 Commercial Road, Melbourne, Victoria 3004, Australia.
Blood Rev. 2009 Mar;23(2):61-5. doi: 10.1016/j.blre.2008.06.002. Epub 2008 Jul 21.
Arterial thrombosis, manifesting as acute myocardial infarction or ischaemic stroke, is the single most common cause of morbidity and mortality in industrialised societies. Platelets are a pre-requisite for the formation of arterial thrombi and, as a consequence, novel antiplatelet agents are sought to meet the significant clinical need for a potent, safe, and orally available therapy for the management of cardiovascular disease. Platelet thrombin receptors, termed protease-activated receptors (PARs), represent one promising candidate for the development of such therapy. This review outlines the role of platelet PARs in haemostasis and thrombosis and discusses the preclinical and clinical evidence supporting the potential of PAR antagonists as novel antiplatelet therapy.
动脉血栓形成,表现为急性心肌梗死或缺血性中风,是工业化社会中发病和死亡的最常见单一原因。血小板是动脉血栓形成的必要条件,因此,人们正在寻找新型抗血小板药物,以满足对有效、安全且口服可用的心血管疾病治疗药物的重大临床需求。血小板凝血酶受体,即蛋白酶激活受体(PARs),是开发此类治疗方法的一个有前景的候选靶点。本文综述概述了血小板PARs在止血和血栓形成中的作用,并讨论了支持PAR拮抗剂作为新型抗血小板治疗潜力的临床前和临床证据。