P2Y purinoceptor 12

Details

Name
P2Y purinoceptor 12
Synonyms
  • ADP-glucose receptor
  • ADPG-R
  • HORK3
  • P2T(AC)
  • P2Y(AC)
  • P2Y(ADP)
  • P2Y(cyc)
  • P2Y12
  • P2Y12 platelet ADP receptor
  • SP1999
Gene Name
P2RY12
UniProtKB Entry
Q9H244Swiss-Prot
Organism
Humans
NCBI Taxonomy ID
9606
Amino acid sequence
>lcl|BSEQ0009940|P2Y purinoceptor 12
MQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFI
IFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITI
DRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKS
EFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFI
IIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFF
LCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM
Number of residues
342
Molecular Weight
39438.355
Theoretical pI
9.99
GO Classification
Functions
G protein-coupled adenosine receptor activity / G protein-coupled ADP receptor activity / G protein-coupled purinergic nucleotide receptor activity
Processes
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway / calcium-mediated signaling / cell projection organization / cerebral cortex radial glia-guided migration / establishment of localization in cell / G protein-coupled receptor signaling pathway / lamellipodium assembly / monoatomic ion transport / phospholipase C-activating G protein-coupled receptor signaling pathway / positive regulation of cell adhesion mediated by integrin / positive regulation of chemotaxis / positive regulation of integrin activation by cell surface receptor linked signal transduction / positive regulation of microglial cell migration / positive regulation of monoatomic ion transport / positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction / positive regulation of ruffle assembly / regulation of chemotaxis / response to axon injury / visual system development
Components
cell body membrane / cell projection membrane / membrane
General Function
Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Required for normal platelet aggregation and blood coagulation
Specific Function
G protein-coupled adenosine receptor activity
Pfam Domain Function
Signal Regions
Not Available
Transmembrane Regions
28-50 62-82 98-118 143-162 186-207 234-259 279-298
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0009941|P2Y purinoceptor 12 (P2RY12)
ATGCAAGCCGTCGACAACCTCACCTCTGCGCCTGGTAACACCAGTCTGTGCACCAGAGAC
TACAAAATCACCCAGGTCCTCTTCCCACTGCTCTACACTGTCCTGTTTTTTGTTGGACTT
ATCACAAATGGCCTGGCGATGAGGATTTTCTTTCAAATCCGGAGTAAATCAAACTTTATT
ATTTTTCTTAAGAACACAGTCATTTCTGATCTTCTCATGATTCTGACTTTTCCATTCAAA
ATTCTTAGTGATGCCAAACTGGGAACAGGACCACTGAGAACTTTTGTGTGTCAAGTTACC
TCCGTCATATTTTATTTCACAATGTATATCAGTATTTCATTCCTGGGACTGATAACTATC
GATCGCTACCAGAAGACCACCAGGCCATTTAAAACATCCAACCCCAAAAATCTCTTGGGG
GCTAAGATTCTCTCTGTTGTCATCTGGGCATTCATGTTCTTACTCTCTTTGCCTAACATG
ATTCTGACCAACAGGCAGCCGAGAGACAAGAATGTGAAGAAATGCTCTTTCCTTAAATCA
GAGTTCGGTCTAGTCTGGCATGAAATAGTAAATTACATCTGTCAAGTCATTTTCTGGATT
AATTTCTTAATTGTTATTGTATGTTATACACTCATTACAAAAGAACTGTACCGGTCATAC
GTAAGAACGAGGGGTGTAGGTAAAGTCCCCAGGAAAAAGGTGAACGTCAAAGTTTTCATT
ATCATTGCTGTATTCTTTATTTGTTTTGTTCCTTTCCATTTTGCCCGAATTCCTTACACC
CTGAGCCAAACCCGGGATGTCTTTGACTGCACTGCTGAAAATACTCTGTTCTATGTGAAA
GAGAGCACTCTGTGGTTAACTTCCTTAAATGCATGCCTGGATCCGTTCATCTATTTTTTC
CTTTGCAAGTCCTTCAGAAATTCCTTGATAAGTATGCTGAAGTGCCCCAATTCTGCAACA
TCTCTGTCCCAGGACAATAGGAAAAAAGAACAGGATGGTGGTGACCCAAATGAAGAGACT
CCAATGTAA
Chromosome Location
3
Locus
3q25.1
External Identifiers
ResourceLink
UniProtKB IDQ9H244
UniProtKB Entry NameP2Y12_HUMAN
GenBank Protein ID12083902
GenBank Gene IDAF313449
GeneCard IDP2RY12
GenAtlas IDP2RY12
HGNC IDHGNC:18124
PDB ID(s)4NTJ, 4PXZ, 4PY0, 7PP1, 7XXI
KEGG IDhsa:64805
IUPHAR/Guide To Pharmacology ID328
NCBI Gene ID64805
General References
  1. Hollopeter G, Jantzen HM, Vincent D, Li G, England L, Ramakrishnan V, Yang RB, Nurden P, Nurden A, Julius D, Conley PB: Identification of the platelet ADP receptor targeted by antithrombotic drugs. Nature. 2001 Jan 11;409(6817):202-7. [Article]
  2. Zhang FL, Luo L, Gustafson E, Lachowicz J, Smith M, Qiao X, Liu YH, Chen G, Pramanik B, Laz TM, Palmer K, Bayne M, Monsma FJ Jr: ADP is the cognate ligand for the orphan G protein-coupled receptor SP1999. J Biol Chem. 2001 Mar 16;276(11):8608-15. Epub 2000 Dec 4. [Article]
  3. Takasaki J, Kamohara M, Saito T, Matsumoto M, Matsumoto S, Ohishi T, Soga T, Matsushime H, Furuichi K: Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor. Mol Pharmacol. 2001 Sep;60(3):432-9. [Article]
  4. Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S: Identification of G protein-coupled receptor genes from the human genome sequence. FEBS Lett. 2002 Jun 5;520(1-3):97-101. [Article]
  5. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
  6. Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q: Structure of the human P2Y12 receptor in complex with an antithrombotic drug. Nature. 2014 May 1;509(7498):115-8. doi: 10.1038/nature13083. Epub 2014 Mar 23. [Article]
  7. Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q: Agonist-bound structure of the human P2Y12 receptor. Nature. 2014 May 1;509(7498):119-22. doi: 10.1038/nature13288. [Article]
  8. Cattaneo M, Zighetti ML, Lombardi R, Martinez C, Lecchi A, Conley PB, Ware J, Ruggeri ZM: Molecular bases of defective signal transduction in the platelet P2Y12 receptor of a patient with congenital bleeding. Proc Natl Acad Sci U S A. 2003 Feb 18;100(4):1978-83. Epub 2003 Feb 10. [Article]
  9. Lecchi A, Razzari C, Paoletta S, Dupuis A, Nakamura L, Ohlmann P, Gachet C, Jacobson KA, Zieger B, Cattaneo M: Identification of a new dysfunctional platelet P2Y12 receptor variant associated with bleeding diathesis. Blood. 2015 Feb 5;125(6):1006-13. doi: 10.1182/blood-2013-07-517896. Epub 2014 Nov 26. [Article]

Associated Data

Bio-Entities
Bio-EntityType
P2Y purinoceptor 12 (Humans)protein
primary
P2 Purinoceptorsprotein
Drug Relations
DrugDrug groupPharmacological action?TypeActionsDetails
TiclopidineapprovedyestargetantagonistDetails
ClopidogrelapprovedyestargetantagonistDetails
EpoprostenolapprovedyestargetagonistDetails
Treprostinilapproved, investigationalunknowntargetagonistDetails
PrasugrelapprovedyestargetantagonistDetails
ElinogrelinvestigationalyestargetantagonistDetails
CangrelorapprovedyestargetinhibitorDetails
TicagrelorapprovedyestargetinhibitorDetails
RegrelorinvestigationalunknowntargetantagonistDetails
VicagrelinvestigationalunknowntargetantagonistinhibitorDetails
SelatogrelinvestigationalunknowntargetantagonistDetails
Adenosine disphosphateinvestigationalyestargetagonistDetails
Promethazineapproved, investigationalunknowntargetinhibitorDetails