Kaihua Zhang, Jin Zhang, Zhan-Guo Gao, Dandan Zhang, Lan Zhu, Gye Won Han, Steven M Moss, Silvia Paoletta, Evgeny Kiselev, Weizhen Lu, Gustavo Fenalti, Wenru Zhang, Christa E Müller, Huaiyu Yang, Hualiang Jiang, Vadim Cherezov, Vsevolod Katritch, Kenneth A Jacobson, Raymond C Stevens, Beili Wu, Qiang Zhao
P2Y receptors (P2YRs), a family of purinergic G-protein-coupled receptors (GPCRs), are activated by extracellular nucleotides. There are a total of eight distinct functional P2YRs expressed in human, which are subdivided into P2Y1-like receptors and P2Y12-like receptors. Their ligands are generally charged molecules with relatively low bioavailability and stability in vivo, which limits our understanding of this receptor family. P2Y12R regulates platelet activation and thrombus formation, and several antithrombotic drugs targeting P2Y12R--including the prodrugs clopidogrel (Plavix) and prasugrel (Effient) that are metabolized and bind covalently, and the nucleoside analogue ticagrelor (Brilinta) that acts directly on the receptor--have been approved for the prevention of stroke and myocardial infarction...
May 1, 2014: Nature