Inserm, UMRS_698, Paris, France.
J Thromb Haemost. 2012 Dec;10(12):2418-27. doi: 10.1111/jth.12009.
The treatment of acute coronary syndromes has been considerably improved in recent years with the introduction of highly efficient antiplatelet drugs. However, there are still significant limitations: the recurrence of adverse vascular events remains a problem, and the improvement in efficacy is counterbalanced by an increased risk of bleeding, which is of particular importance in patients at risk of stroke. One of the most attractive targets for the development of new molecules with potential antithrombotic activity is platelet glycoprotein (GP)VI, because its blockade appears to ideally combine efficacy and safety. This review summarizes current knowledge on GPVI regarding its structure, its function, and its role in physiologic hemostasis and thrombosis. Strategies for inhibiting GPVI are presented, and evidence of the antithrombotic efficacy and safety of GPVI antagonists is provided.
近年来，随着高效抗血小板药物的引入，急性冠状动脉综合征的治疗有了显著改善。然而，仍存在着显著的局限性：不良血管事件的复发仍然是一个问题，疗效的提高被出血风险的增加所抵消，这在有中风风险的患者中尤为重要。开发具有潜在抗血栓活性的新分子的最有吸引力的目标之一是血小板糖蛋白 (GP)VI，因为其阻断似乎理想地结合了疗效和安全性。这篇综述总结了关于 GPVI 的结构、功能及其在生理止血和血栓形成中的作用的最新知识。提出了抑制 GPVI 的策略，并提供了 GPVI 拮抗剂的抗血栓疗效和安全性的证据。
