Benimana Oscar, Zhao Lulu, Kong Yi, Li Zhiyu, Xie Zhouling
Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
Future Med Chem. 2017 Jun;9(10):1087-1110. doi: 10.4155/fmc-2017-0001. Epub 2017 Jun 20.
Antiplatelet therapy displays a critical role in the treatment and prevention of antithrombotic disorders. Many new antiplatelet agents have been developed following the emergence of various clinical limitations of classical antiplatelet drugs. This review covers mainly the recent advances in the development of P2Y antagonists and GPIIb/IIIa antagonists. Meanwhile, it summarizes promising approaches to new platelet surface receptors such as prostanoid EP3 receptor, thromboxane A prostanoid receptor, protease-activated receptors, GPIb-IX-V receptor and P-selectin. In addition, PI3K, a critical protein at the inside signaling pathway of platelet activation is also mentioned as an important antiplatelet target. Moreover, the development of respective drug candidates is discussed in detail.
抗血小板治疗在抗血栓疾病的治疗和预防中发挥着关键作用。随着经典抗血小板药物出现各种临床局限性，许多新型抗血小板药物应运而生。本综述主要涵盖P2Y拮抗剂和糖蛋白IIb/IIIa拮抗剂开发的最新进展。同时，总结了针对新的血小板表面受体（如前列腺素EP3受体、血栓素A前列腺素受体、蛋白酶激活受体、糖蛋白Ib-IX-V受体和P-选择素）的有前景的方法。此外，血小板激活内在信号通路中的关键蛋白磷脂酰肌醇-3-激酶（PI3K）也作为重要的抗血小板靶点被提及。此外，还详细讨论了各自候选药物的开发情况。
