P2Y12

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

OVerview

In the field of molecular biology, the P2Y12 protein is found mainly but not exclusively on the surface of blood platelets, and is an important regulator in blood clotting.[1]

P2Y12 belongs to the Gi class of a group of G protein-coupled (GPCR) purinergic receptors[2] and is a chemoreceptor for adenosine diphosphate (ADP).[3][4] The P2Y family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor is involved in platelet aggregation, and is a potential target for the treatment of thromboembolisms and other clotting disorders. Two transcript variants encoding the same isoform have been identified for this gene.[5]

Clinical significance

The drugs clopidogrel (PLAVIX), prasugrel (Efient, Effient), ticagrelor (BRILINTA), and cangrelor bind to this receptor and are marketed as antiplatelet agents.[3]

References

  1. Dorsam RT, Kunapuli SP (2004). "Central role of the P2Y12 receptor in platelet activation". J. Clin. Invest. 113 (3): 340–5. doi:10.1172/JCI200420986. PMC 324551. PMID 14755328.
  2. Murugappa S, Kunapuli SP (2006). "The role of ADP receptors in platelet function". Front. Biosci. 11 (1): 1977–86. doi:10.2741/1939. PMID 16368572.
  3. 3.0 3.1 Hollopeter G, Jantzen HM, Vincent D, Li G, England L, Ramakrishnan V, Yang RB, Nurden P, Nurden A, Julius D, Conley PB (2001). "Identification of the platelet ADP receptor targeted by antithrombotic drugs". Nature. 409 (6817): 202–7. doi:10.1038/35051599. PMID 11196645.
  4. Nicholas RA (2001). "Identification of the P2Y(12) receptor: a novel member of the P2Y family of receptors activated by extracellular nucleotides". Mol. Pharmacol. 60 (3): 416–20. PMID 11502870.
  5. "Entrez Gene: P2RY12 purinergic receptor P2Y, G-protein coupled, 12".

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This article incorporates text from the United States National Library of Medicine, which is in the public domain.