P2Y12

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Purinergic receptor P2Y, G-protein coupled, 12
Protein P2RY12 PDB 1T78.png
Rendering based on PDB 1T78.
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols P2RY12 ; ADPG-R; BDPLT8; HORK3; P2T(AC); P2Y(12)R; P2Y(AC); P2Y(ADP); P2Y(cyc); P2Y12; SP1999
External IDs OMIM600515 MGI1918089 HomoloGene11260 IUPHAR: P2Y12 ChEMBL: 2001 GeneCards: P2RY12 Gene
Orthologs
Species Human Mouse
Entrez 64805 70839
Ensembl ENSG00000169313 ENSMUSG00000036353
UniProt Q9H244 Q9CPV9
RefSeq (mRNA) NM_022788 NM_027571
RefSeq (protein) NP_073625 NP_081847
Location (UCSC) Chr 3:
151.06 – 151.1 Mb
Chr 3:
59.22 – 59.26 Mb
PubMed search [1] [2]

In the field of purinergic signaling, 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[edit]

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

References[edit]

  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. ^ 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. 
  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". 

External links[edit]

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