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
- Organism
- Humans
- 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
- FunctionsADP receptor activity / G-protein coupled adenosine receptor activity / guanyl-nucleotide exchange factor activityProcessesadenylate cyclase-inhibiting G-protein coupled receptor signaling pathway / blood coagulation / calcium ion transmembrane transport / cellular response to ATP / G-protein coupled purinergic nucleotide receptor signaling pathway / G-protein coupled receptor signaling pathway / glial cell migration / hemostasis / negative regulation of cell differentiation / negative regulation of norepinephrine secretion / platelet activation / platelet aggregation / positive regulation of GTPase activity / positive regulation of ion transport / potassium ion transmembrane transport / protein kinase B signaling / regulation of calcium ion transport / regulation of microglial cell migration / substrate-dependent cell migration, cell extensionComponentsbasal plasma membrane / caveola / cell surface / external side of plasma membrane / integral component of plasma membrane / intrinsic component of membrane / mitochondrion / plasma membrane
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific 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.
- Pfam Domain Function
- 7tm_1 (PF00001)
- 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
- 3q24-q25
- External Identifiers
Resource Link UniProtKB ID Q9H244 UniProtKB Entry Name P2Y12_HUMAN GenBank Protein ID 12083902 GenBank Gene ID AF313449 GenAtlas ID P2RY12 HGNC ID HGNC:18124 - General References
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
Drug Relations
- Drug Relations
DrugBank ID Name Drug group Pharmacological action? Actions Details DB00208 Ticlopidine approved yes antagonist Details DB00758 Clopidogrel approved yes antagonist Details DB01240 Epoprostenol approved yes agonist Details DB00374 Treprostinil approved, investigational unknown agonist Details DB06209 Prasugrel approved yes antagonist Details DB06350 Elinogrel investigational unknown Details DB06441 Cangrelor approved yes inhibitor Details DB08816 Ticagrelor approved yes inhibitor Details DB05553 Regrelor investigational unknown antagonist Details DB16349 Vicagrel investigational unknown antagonistinhibitor Details DB15163 Selatogrel investigational unknown antagonist Details DB01069 Promethazine approved, investigational unknown inhibitor Details