Target Information
Target General Infomation | |||||
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Target ID |
T67818
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Former ID |
TTDR00081
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Target Name |
P2Y purinoceptor 1
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Gene Name |
P2RY1
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Synonyms |
ATP receptor; Adenosine P2Y1 receptor; P2Y(1) receptor; P2Y1; Purinergic receptor; P2RY1
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Target Type |
Research
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Disease | Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | ||||
Function |
Receptor for extracellular adenine nucleotides such as ATP and ADP. In platelets binding to ADP leads to mobilization of intracellular calcium ions via activation of phospholipase C, a change in platelet shape, and probably to platelet aggregation.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T67818
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UniProt ID | |||||
Sequence |
MTEVLWPAVPNGTDAAFLAGPGSSWGNSTVASTAAVSSSFKCALTKTGFQFYYLPAVYIL
VFIIGFLGNSVAIWMFVFHMKPWSGISVYMFNLALADFLYVLTLPALIFYYFNKTDWIFG DAMCKLQRFIFHVNLYGSILFLTCISAHRYSGVVYPLKSLGRLKKKNAICISVLVWLIVV VAISPILFYSGTGVRKNKTITCYDTTSDEYLRSYFIYSMCTTVAMFCVPLVLILGCYGLI VRALIYKDLDNSPLRRKSIYLVIIVLTVFAVSYIPFHVMKTMNLRARLDFQTPAMCAFND RVYATYQVTRGLASLNSCVDPILYFLAGDTFRRRLSRATRKASRRSEANLQSKSEDMTLN ILPEFKQNGDTSL |
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Structure |
1Y36
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Inhibitor | 1-(3,4-dichlorophenyl)-3-(3,5-dichlorophenyl)urea | Drug Info | [529445] | ||
Urea derivative | Drug Info | [527825] | |||
Agonist | 2',3'-ddATP | Drug Info | [534388] | ||
2-Cl-ADP(alpha-BH3) | Drug Info | [532391] | |||
2MeSADP | Drug Info | [526444] | |||
2MeSATP | Drug Info | [526444] | |||
adenosine diphosphate | Drug Info | [526444] | |||
ATPgammaS | Drug Info | [534388] | |||
compound 3a | Drug Info | [531995] | |||
dATPalphaS | Drug Info | [534388] | |||
MRS2365 | Drug Info | [527201] | |||
[35S]ADPbetaS | Drug Info | [543769] | |||
[3H]2MeSADP | Drug Info | [526120] | |||
Modulator (allosteric modulator) | 2,2'-pyridylisatogen tosylate | Drug Info | [527106] | ||
Antagonist | 2-chloroadenosine-5-triphosphate | Drug Info | [534603] | ||
A2P5P | Drug Info | [534268] | |||
adenosine-3'-5'-bisphosphate | Drug Info | [534268] | |||
BMS compound 16 | Drug Info | [533195] | |||
BMS compound 4c | Drug Info | [532349] | |||
GlaxoSmithKline compound 5h | Drug Info | [530970] | |||
GlaxoSmithKline compound 6i | Drug Info | [529752] | |||
MRS-2179 | Drug Info | [535699], [535768] | |||
MRS2279 | Drug Info | [526444] | |||
MRS2298 | Drug Info | [527243] | |||
MRS2496 | Drug Info | [527243] | |||
MRS2500 | Drug Info | [526866] | |||
MRS2950 | Drug Info | [531978] | |||
N-(6)-methyl-2'-deoxyadenosine-3':5'-bisphosphate | Drug Info | [535100] | |||
P2Y1 antagonists | Drug Info | [543769] | |||
Pfizer compound 11 | Drug Info | [529445] | |||
Pfizer compound 67 | Drug Info | [529445] | |||
PPADS | Drug Info | [526444] | |||
[32P]MRS2500 | Drug Info | [527877] | |||
[3H]MRS2279 | Drug Info | [526444] | |||
Pathways | |||||
KEGG Pathway | Rap1 signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Platelet activation | |||||
Reactome | G alpha (q) signalling events | ||||
P2Y receptors | |||||
ADP signalling through P2Y purinoceptor 1 | |||||
WikiPathways | Nucleotide GPCRs | ||||
GPCRs, Class A Rhodopsin-like | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Signal amplification | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
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 526444 | Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist. Mol Pharmacol. 2002 Nov;62(5):1249-57. | ||||
Ref 526866 | 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J Med Chem. 2003 Nov 6;46(23):4974-87. | ||||
Ref 527106 | 2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding. Biochem Pharmacol. 2004 Jul 15;68(2):231-7. | ||||
Ref 527201 | Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. J Pharmacol Exp Ther. 2004Dec;311(3):1038-43. Epub 2004 Sep 2. | ||||
Ref 527243 | Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor. Biochem Pharmacol. 2004 Nov 15;68(10):1995-2002. | ||||
Ref 527825 | J Med Chem. 2005 Nov 3;48(22):7040-8.Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. | ||||
Ref 527877 | [32P]2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([32P]MRS2500), a novel radioligand for quantification of native P2Y1 receptors. Br J Pharmacol. 2006 Mar;147(5):459-67. | ||||
Ref 529445 | Bioorg Med Chem Lett. 2008 Jun 1;18(11):3338-43. Epub 2008 Apr 15.P2Y1 receptor antagonists as novel antithrombotic agents. | ||||
Ref 529752 | Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6222-6. | ||||
Ref 530970 | Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4104-7. | ||||
Ref 531978 | Virtual screening leads to the discovery of novel non-nucleotide P2Y??receptor antagonists. Bioorg Med Chem. 2012 Sep 1;20(17):5254-61. | ||||
Ref 531995 | Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist. J Med Chem. 2012 Sep 13;55(17):7623-35. | ||||
Ref 532349 | New azole antagonists with high affinity for the P2Y(1) receptor. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3519-22. | ||||
Ref 532391 | Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists. J Med Chem. 2013 Jun 27;56(12):4938-52. | ||||
Ref 533195 | Two disparate ligand-binding sites in the human P2Y1 receptor. Nature. 2015 Apr 16;520(7547):317-21. | ||||
Ref 534268 | Identification of competitive antagonists of the P2Y1 receptor. Mol Pharmacol. 1996 Nov;50(5):1323-9. | ||||
Ref 534388 | An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor. Br J Pharmacol. 1997 May;121(2):338-44. | ||||
Ref 534603 | ATP derivatives are antagonists of the P2Y1 receptor: similarities to the platelet ADP receptor. Mol Pharmacol. 1998 Apr;53(4):727-33. | ||||
Ref 535100 | Key role of the P2Y(1) receptor in tissue factor-induced thrombin-dependent acute thromboembolism: studies in P2Y(1)-knockout mice and mice treated with a P2Y(1) antagonist. Circulation. 2001 Feb 6;103(5):718-23. | ||||
Ref 535699 | The P2Y(1) receptor as a target for new antithrombotic drugs: a review of the P2Y(1) antagonist MRS-2179. Cardiovasc Drug Rev. 2003 Spring;21(1):67-76. |
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