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Antithrombotic P2Y12 receptor antagonists: recent developments in drug discovery
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-10-03 , DOI: 10.1016/j.drudis.2018.09.021
Younis Baqi , Christa E. Müller

The P2Y12 receptor is one of eight known P2Y receptor subtypes, and belongs to the G-protein-coupled receptor (GPCR) family. The P2Y12 receptor is highly expressed on blood platelets and in the brain. Potent, selective, peripherally acting antagonists for the P2Y12 receptor are used clinically as antithrombotic drugs. Several different scaffolds have been identified as P2Y12 receptor antagonists, including irreversibly acting thienotetrahydropyridines (prodrugs), and reversible competitive antagonists, including adenine nucleotide analogs, piperazinyl-glutamate-quinolines, -pyridines, and -pyrimidines, and anthraquinone derivatives. Here, we provide an overview of the different scaffolds that have been developed as P2Y12 receptor antagonists, some of which have become important therapeutics.



中文翻译:

抗血栓性P2Y 12受体拮抗剂:药物发现的最新进展

P2Y 12受体是八种已知的P2Y受体亚型之一,属于G蛋白偶联受体(GPCR)家族。P2Y 12受体在血小板和大脑中高表达。P2Y 12受体的有效,选择性,作用于周围的拮抗剂在临床上用作抗血栓形成药物。几种不同的支架已被鉴定为P2Y 12受体拮抗剂,包括不可逆作用的硫代四氢吡啶类(前药)和可逆竞争性拮抗剂,包括腺嘌呤核苷酸类似物,哌嗪基-谷氨酸喹啉,-吡啶和-嘧啶和蒽醌衍生物。在这里,我们提供了已被开发为P2Y 12的不同支架的概述。 受体拮抗剂,其中一些已成为重要的治疗剂。

更新日期:2018-10-03
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