血小板受体GPVI作为抗血栓靶点的研究进展

Advances of Studies on Platelet GPVI as Antithrombotic Target——Review

血小板活化是生理性止血中的关键步骤,在病理性血栓形成中也起着重要的作用。通过抑制血小板活化以预防和治疗血栓是血栓性疾病防治的重要手段之一。然而,目前临床抗血栓药物的高效性以出血风险增加为代价。血小板糖蛋白受体VI(GPVI)是血小板特异性受体,其与胶原的结合是血小板活化的关键。它作为一种新型抗血栓药物靶点,其拮抗剂能抑制血栓及其炎症反应,又不干扰正常止血机制,既安全又有效。本文对血小板GPVI的结构与功能,在出血和血栓形成中的作用及其拮抗剂的最新研究进展作一综述,并对未来开发出具有临床意义的以GPVI为靶点的抗血小板药物进行展望,以期为血栓栓塞性疾病提供可靠的药物治疗。

Platelet activation is a crucial step in both physiological hemostasis and pathological thrombosis,which is an important mean to prevent and treat thrombotic diseases by inhibition of platelet activation.The current clinical antithrombotic therapy showed a high efficiency,but at risk of bleeding.Platelet glycoprotein VI（GPVI） is a plateletspecific receptor and its binding with collagen is critical for platelet activation.GPVI antagonists were shown to effectively inhibit thrombosis and inflammation without influence on normal hemostasis.As a novel target for antithrombotic therapy,it ideally combines efficacy with safety.This review summarizes the recent advances of studies on GPVI structure,function and its role in hemostasis,thrombosis,and anti-GPVI agents.The potential clinical strategies of antiplatelet drugs targeting GPVI are discussed so as to provide a reliable regimen for thrombotic diseases.