P2Y12

Purinergic receptor P2Y, G-protein coupled, 12
	; Rendering based on PDB 1T78.
Available structures
PDB	1T78, 1VZ1, 1Y9C
Identifiers
Symbols	P2RY12; ADPG-R; HORK3; P2T(AC); P2Y(AC); P2Y(ADP); P2Y(cyc); P2Y12; SP1999
External IDs	OMIM: 600515 MGI: 1918089 HomoloGene: 11260 IUPHAR: P2Y12 GeneCards: P2RY12 Gene
Gene Ontology
Molecular function	• adenosine receptor activity, G-protein coupled; • ADP receptor activity; • receptor activity; • guanyl-nucleotide exchange factor activity;
Cellular component	• mitochondrion; • plasma membrane; • plasma membrane; • membrane; • integral to membrane;
Biological process	• G-protein signaling, coupled to cAMP nucleotide second messenger; • blood coagulation; • hemostasis; • platelet activation; • positive regulation of ion transport; • protein kinase B signaling cascade;
	Sources: Amigo / QuickGO
Orthologs

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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]

[edit] Clinical significance

The drugs clopidogrel (Plavix) and ticagrelor (Brilinta) bind to this receptor and are marketed as antiplatelet agents.^[3]

^ 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. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=324551.
^ 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.
^ ^a ^b 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.
^ 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. http://molpharm.aspetjournals.org/cgi/content/full/60/3/416.
^ "Entrez Gene: P2RY12 purinergic receptor P2Y, G-protein coupled, 12". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=64805.

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