Target Information

Target General Infomation
Target ID
T46937
Former ID
TTDS00113
Target Name
P2Y purinoceptor 12
Gene Name
P2RY12
Synonyms
ADP-glucose receptor; ADP-receptor; ADPG-R; Adenosine P2Y12 receptor; Nucleotide P2Y(12) receptor; P2T(AC); P2Y(AC); P2Y(ADP); P2Y(ADP)P2Y purinoceptor 12; P2Y(cyc); P2Y12; P2Y12 platelet ADP receptor; SP1999; P2RY12
Target Type
Successful
Disease Acute coronary syndrome [ICD9: 444; ICD10: I74]
Arterial thrombosis; Myocardial infarction [ICD9:437.6, 453, 671.5, 671.9, 410; ICD10: I80-I82, I21, I22]
Cardiovascular disorder [ICD10: I00-I99]
Myocardial infarction [ICD9: 410; ICD10: I21, I22]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Unspecified [ICD code not available]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T46937
UniProt ID
Q9H244
Sequence
MQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFI
IFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITI
DRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKS
EFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFI
IIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFF
LCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM
Drugs and Mode of Action
Drug(s) Brilinta Drug Info Approved Thrombosis [531783], [539115]
Cangrelor Drug Info Approved Thrombosis [521896], [539125]
Clopidogrel Drug Info Approved Thrombosis [542158], [548841]
Plavix Drug Info Approved Thrombosis [543771]
Prasugrel Drug Info Approved Acute coronary syndrome [530677], [542562]
Brilinta/Brilique Drug Info Phase 3 Arterial thrombosis; Myocardial infarction [524133]
INS-50589 Drug Info Phase 2 Cardiovascular disorder [521824], [539120]
ARL-67085 Drug Info Phase 1 Thrombosis [525640], [539107]
Elinogrel Drug Info Phase 1 Myocardial infarction [522795]
Agonist 2MeSADP Drug Info [527109]
adenosine diphosphate Drug Info [527109]
ARL-67085 Drug Info [525640]
[3H]2MeSADP Drug Info [526120]
Antagonist 2MeSAMP Drug Info [526120]
ARL66096 Drug Info [533775]
Brilinta Drug Info [550288]
BX 048 Drug Info [529525]
BX 667 Drug Info [529525]
Cangrelor Drug Info [543771]
Clopidogrel Drug Info [527109]
compound 20o Drug Info [532047]
compound 4 Drug Info [532047]
compound 4 Drug Info [532089]
Elinogrel Drug Info [530744]
INS49266 Drug Info [529277]
pCMPS Drug Info [527109]
Plavix Drug Info [543771]
PRT-060096 Drug Info [543771]
R-138727 Drug Info [527841]
[3H]PSB-0413 Drug Info [527789]
Modulator Brilinta/Brilique Drug Info [543771]
clopidogrel intravenous Drug Info
INS-50589 Drug Info [528959]
Inhibitor Prasugrel Drug Info [530677]
PSB-0702 Drug Info [530157]
PSB-0739 Drug Info [530157]
Pathways
KEGG Pathway Platelet activation
Reactome P2Y receptors
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Signal amplification
GPCR ligand binding
GPCR downstream signaling
References
Ref 521824ClinicalTrials.gov (NCT00316212) Study of INS50589 Intravenous Infusion in Subjects Undergoing Coronary Artery Bypass Grafting (CABG) Involving Cardiopulmonary Bypass. U.S. National Institutes of Health.
Ref 521896ClinicalTrials.gov (NCT00385138) Cangrelor Versus Standard Therapy to Achieve Optimal Management of Platelet Inhibition.. U.S. National Institutes of Health.
Ref 522795ClinicalTrials.gov (NCT00984113) Pharmacokinetics of Elinogrel in Healthy Volunteers and Patients With Mild, Moderate, and Severe Renal Impairment. U.S. National Institutes of Health.
Ref 524133ClinicalTrials.gov (NCT01732822) A Study Comparing Cardiovascular Effects of Ticagrelor and Clopidogrel in Patients With Peripheral Artery Disease. U.S. National Institutes of Health.
Ref 525640Pharmacological characterization of the human P2Y11 receptor. Br J Pharmacol. 1999 Nov;128(6):1199-206.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 539107(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1756).
Ref 539115(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1765).
Ref 539120(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1770).
Ref 539125(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1776).
Ref 542158(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7150).
Ref 542562(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7562).
Ref 543771(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 328).
Ref 548841Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029432)
Ref 525640Pharmacological characterization of the human P2Y11 receptor. Br J Pharmacol. 1999 Nov;128(6):1199-206.
Ref 526120Molecular 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.
Ref 527109P2Y12, a new platelet ADP receptor, target of clopidogrel. Semin Vasc Med. 2003 May;3(2):113-22.
Ref 527789Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5450-2. Epub 2005 Oct 5.
Ref 527841Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor. Thromb Haemost. 2005 Sep;94(3):593-8.
Ref 528959Rapid and reversible modulation of platelet function in man by a novel P2Y(12) ADP-receptor antagonist, INS50589. Platelets. 2007 Aug;18(5):346-56.
Ref 529277J Med Chem. 2008 Feb 28;51(4):1007-25. Epub 2008 Jan 31.Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptor.
Ref 529525Novel P2Y12 adenosine diphosphate receptor antagonists for inhibition of platelet aggregation (II): pharmacodynamic and pharmacokinetic characterization. Thromb Res. 2008;122(4):533-40.
Ref 530157J Med Chem. 2009 Jun 25;52(12):3784-93.High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 530744Elinogrel, a reversible P2Y12 receptor antagonist for the treatment of acute coronary syndrome and prevention of secondary thrombotic events. Curr Opin Investig Drugs. 2010 Mar;11(3):340-8.
Ref 532047Identification of high-affinity P2Y??? antagonists based on a phenylpyrazole glutamic acid piperazine backbone. J Med Chem. 2012 Oct 25;55(20):8615-29.
Ref 532089Modified diadenosine tetraphosphates with dual specificity for P2Y1 and P2Y12 are potent antagonists of ADP-induced platelet activation. J Thromb Haemost. 2012 Dec;10(12):2573-80.
Ref 533775FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T-purinoceptors. Br J Pharmacol. 1994 Nov;113(3):1057-63.
Ref 543771(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 328).
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).

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