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- W47439750 abstract "The P2Y receptors are a widely expressed group of eight nucleotide-activated G protein-coupled receptors (GPCRs). The P2Y1(ADP), P2Y2(ATP/UTP), P2Y4(UTP), P2Y6(UDP), and P2Y11(ATP) receptors activate Gq and therefore robustly promote inositol lipid signaling responses. The P2Y12(ADP), P2Y13(ADP), and P2Y14(UDP/UDP-glucose) receptors activate Gi leading to inhibition of adenylyl cyclase and to Gβγ-mediated activation of a range of effector proteins including phosphoinositide 3-kinase-γ, inward rectifying K+ (GIRK) channels, phospholipase C-β2 and -β3, and G protein-receptor kinases 2 and 3. A broad range of physiological responses occur downstream of activation of these receptors ranging from Cl− secretion by epithelia to aggregation of platelets to neurotransmission. Useful structural models of the P2Y receptors have evolved from extensive genetic analyses coupled with molecular modeling based on three-dimensional structures obtained for rhodopsin and several other GPCRs. Selective ligands have been synthesized for most of the P2Y receptors with the most prominent successes attained with highly selective agonist and antagonist molecules for the ADP-activated P2Y1 and P2Y12 receptors. The widely prescribed drug, clopidogrel, which results in irreversible blockade of the platelet P2Y12 receptor, is the most important therapeutic agent that targets a P2Y receptor." @default.
- W47439750 created "2016-06-24" @default.
- W47439750 creator A5030808105 @default.
- W47439750 creator A5060762284 @default.
- W47439750 date "2011-01-01" @default.
- W47439750 modified "2023-10-16" @default.
- W47439750 title "Molecular Pharmacology, Physiology, and Structure of the P2Y Receptors" @default.
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