This review highlights the established role of P2Y12 receptors in antithrombotic therapy and the emerging potential of P2Y1 receptors as targets for new treatments.
Reinforces P2Y12 targeting in current practice; leaves open P2Y1 as a novel antithrombotic target pending clinical trials.
Blood platelets play a key role in arterial thrombosis which is one of the leading causes of mortality in western countries. They may also be involved in the pathogenesis of deep vein thrombosis. Adenosine 5′‐diphosphate ( ADP ) is one of the most important mediators of platelet activation. Two G protein‐coupled ADP receptors, P2Y1 and P2Y12 , selectively contribute to platelet aggregation and formation of a thrombus. Playing a central role in platelet activation and in growth and stabilization of a thrombus, the P2Y12 receptor is an established target of antithrombotic drugs like the thienopyridines clopidogrel or prasugrel, or direct reversible antagonists such as ticagrelor or cangrelor. Each of these drugs has proven efficacy in large clinical trials. At a preclinical stage, studies in P2Y1 deficient mice and using selective P2Y1 antagonists in experimental models of thrombosis and inflammation have shown that this receptor is also an attractive target for new antithrombotic compounds. WIREs Membr Transp Signal 2013. doi: 10.1002/wmts.97 Conflict of interest: The authors have declared no conflicts of interest for this article. For further resources related to this article, please visit the WIREs website .
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Gachet et al. (2013) studied this question.
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