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: 328 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:
151.34 – 151.38 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

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

P2Y12 inhibitors do not change the risk of death when given as a pretreatment prior to routine percutaneous coronary intervention (PCI) in people who have had a non-ST-elevation myocardial infarction (NSTEMI). They do however increase the risk of bleeding and decrease the risk of further cardiovascular problems. Thus their routine use in this context is of questionable value. [6]

In patients undergoing primary PCI for an ST-segment elevation myocardial infarction (STEMI), a P2Y12 inhibitor should be administered as soon as possible. The use of clopidogrel in particular has been shown to improve morbidity and mortality endpoints including cardiovascular death, recurrent MI, and stroke at 30 days after PCI. [7]

References

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External links

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