P2Y12

P2Y12

Purinergic receptor P2Y, G-protein coupled, 12
Rendering based on PDB .
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols  ; ADPG-R; BDPLT8; HORK3; P2T(AC); P2Y(12)R; P2Y(AC); P2Y(ADP); P2Y(cyc); P2Y12; SP1999
External IDs IUPHAR: ChEMBL: GeneCards:
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)
RefSeq (protein)
Location (UCSC)
PubMed search

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 to people who have had a NSTEMI. They do however increase the risk of bleeding and decrease the risk of further cardiovascular problems. Thus their routine use is of questionable value.[6]

References

  1. ^ Dorsam RT, Kunapuli SP (2004). "Central role of the P2Y12 receptor in platelet activation". J. Clin. Invest. 113 (3): 340–5.  
  2. ^ Murugappa S, Kunapuli SP (2006). "The role of ADP receptors in platelet function". Front. Biosci. 11 (1): 1977–86.  
  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.  
  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.  
  5. ^ "Entrez Gene: P2RY12 purinergic receptor P2Y, G-protein coupled, 12". 
  6. ^ Bellemain-Appaix A, Kerneis M, O'Connor SA, Silvain J, Cucherat M, Beygu F, Barthelemy O, Collet J, Jacq L, Bernasconi F, Montalescot G (2014). "Reappraisal of thienopyridine pretreatment in patients with non-ST elevation acute coronary syndrome: a systematic review and meta-analysis". BMJ 347 (aug 06 2): g6269–g6269.  

External links

  • "12"P2Y Receptors: P2Y. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 
  • purinoceptor P2Y12 at the US National Library of Medicine Medical Subject Headings (MeSH)

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