Target Information
Target General Infomation | |||||
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Target ID |
T46937
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Former ID |
TTDS00113
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Target Name |
P2Y purinoceptor 12
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Gene Name |
P2RY12
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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
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Target Type |
Successful
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T46937
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UniProt ID | |||||
Sequence |
MQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFI
IFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITI DRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKS EFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFI IIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFF LCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM |
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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 521824 | ClinicalTrials.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 521896 | ClinicalTrials.gov (NCT00385138) Cangrelor Versus Standard Therapy to Achieve Optimal Management of Platelet Inhibition.. U.S. National Institutes of Health. | ||||
Ref 522795 | ClinicalTrials.gov (NCT00984113) Pharmacokinetics of Elinogrel in Healthy Volunteers and Patients With Mild, Moderate, and Severe Renal Impairment. U.S. National Institutes of Health. | ||||
Ref 524133 | ClinicalTrials.gov (NCT01732822) A Study Comparing Cardiovascular Effects of Ticagrelor and Clopidogrel in Patients With Peripheral Artery Disease. U.S. National Institutes of Health. | ||||
Ref 525640 | Pharmacological characterization of the human P2Y11 receptor. Br J Pharmacol. 1999 Nov;128(6):1199-206. | ||||
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 525640 | Pharmacological characterization of the human P2Y11 receptor. Br J Pharmacol. 1999 Nov;128(6):1199-206. | ||||
Ref 526120 | 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. | ||||
Ref 527109 | P2Y12, a new platelet ADP receptor, target of clopidogrel. Semin Vasc Med. 2003 May;3(2):113-22. | ||||
Ref 527789 | Synthesis 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 527841 | Stereoselective 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 528959 | Rapid 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 529277 | J 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 529525 | Novel P2Y12 adenosine diphosphate receptor antagonists for inhibition of platelet aggregation (II): pharmacodynamic and pharmacokinetic characterization. Thromb Res. 2008;122(4):533-40. | ||||
Ref 530157 | J Med Chem. 2009 Jun 25;52(12):3784-93.High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors. | ||||
Ref 530744 | Elinogrel, 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 532047 | Identification of high-affinity P2Y??? antagonists based on a phenylpyrazole glutamic acid piperazine backbone. J Med Chem. 2012 Oct 25;55(20):8615-29. | ||||
Ref 532089 | Modified 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 533775 | FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T-purinoceptors. Br J Pharmacol. 1994 Nov;113(3):1057-63. |
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