Target Information

Target General Infomation
Target ID
T67818
Former ID
TTDR00081
Target Name
P2Y purinoceptor 1
Gene Name
P2RY1
Synonyms
ATP receptor; Adenosine P2Y1 receptor; P2Y(1) receptor; P2Y1; Purinergic receptor; P2RY1
Target Type
Research
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T67818
UniProt ID
P47900
Sequence
MTEVLWPAVPNGTDAAFLAGPGSSWGNSTVASTAAVSSSFKCALTKTGFQFYYLPAVYIL
VFIIGFLGNSVAIWMFVFHMKPWSGISVYMFNLALADFLYVLTLPALIFYYFNKTDWIFG
DAMCKLQRFIFHVNLYGSILFLTCISAHRYSGVVYPLKSLGRLKKKNAICISVLVWLIVV
VAISPILFYSGTGVRKNKTITCYDTTSDEYLRSYFIYSMCTTVAMFCVPLVLILGCYGLI
VRALIYKDLDNSPLRRKSIYLVIIVLTVFAVSYIPFHVMKTMNLRARLDFQTPAMCAFND
RVYATYQVTRGLASLNSCVDPILYFLAGDTFRRRLSRATRKASRRSEANLQSKSEDMTLN
ILPEFKQNGDTSL
Structure
1Y36
Inhibitor 1-(3,4-dichlorophenyl)-3-(3,5-dichlorophenyl)urea Drug Info [1]
Urea derivative Drug Info [2]
Agonist 2',3'-ddATP Drug Info [3]
2-Cl-ADP(alpha-BH3) Drug Info [4]
2MeSADP Drug Info [5]
2MeSATP Drug Info [5]
adenosine diphosphate Drug Info [5]
ATPgammaS Drug Info [3]
compound 3a Drug Info [6]
dATPalphaS Drug Info [3]
MRS2365 Drug Info [7]
[35S]ADPbetaS Drug Info [8]
[3H]2MeSADP Drug Info [9]
Modulator (allosteric modulator) 2,2'-pyridylisatogen tosylate Drug Info [10]
Antagonist 2-chloroadenosine-5-triphosphate Drug Info [11]
A2P5P Drug Info [12]
adenosine-3'-5'-bisphosphate Drug Info [12]
BMS compound 16 Drug Info [13]
BMS compound 4c Drug Info [14]
GlaxoSmithKline compound 5h Drug Info [15]
GlaxoSmithKline compound 6i Drug Info [16]
MRS-2179 Drug Info [17], [18]
MRS2279 Drug Info [5]
MRS2298 Drug Info [19]
MRS2496 Drug Info [19]
MRS2500 Drug Info [20]
MRS2950 Drug Info [21]
N-(6)-methyl-2'-deoxyadenosine-3':5'-bisphosphate Drug Info [22]
P2Y1 antagonists Drug Info [8]
Pfizer compound 11 Drug Info [1]
Pfizer compound 67 Drug Info [1]
PPADS Drug Info [5]
[32P]MRS2500 Drug Info [23]
[3H]MRS2279 Drug Info [5]
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 1Bioorg Med Chem Lett. 2008 Jun 1;18(11):3338-43. Epub 2008 Apr 15.P2Y1 receptor antagonists as novel antithrombotic agents.
REF 2J Med Chem. 2005 Nov 3;48(22):7040-8.Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency.
REF 3An 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 4Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists. J Med Chem. 2013 Jun 27;56(12):4938-52.
REF 5Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist. Mol Pharmacol. 2002 Nov;62(5):1249-57.
REF 6Identification 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 7Induction 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 8(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: 323).
REF 9Molecular 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 102,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding. Biochem Pharmacol. 2004 Jul 15;68(2):231-7.
REF 11ATP derivatives are antagonists of the P2Y1 receptor: similarities to the platelet ADP receptor. Mol Pharmacol. 1998 Apr;53(4):727-33.
REF 12Identification of competitive antagonists of the P2Y1 receptor. Mol Pharmacol. 1996 Nov;50(5):1323-9.
REF 13Two disparate ligand-binding sites in the human P2Y1 receptor. Nature. 2015 Apr 16;520(7547):317-21.
REF 14New azole antagonists with high affinity for the P2Y(1) receptor. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3519-22.
REF 15Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4104-7.
REF 16Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6222-6.
REF 17The 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.
REF 18Inhibition of localized thrombosis in P2Y1-deficient mice and rodents treated with MRS2179, a P2Y1 receptor antagonist. J Thromb Haemost. 2003 Jun;1(6):1144-9.
REF 19Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor. Biochem Pharmacol. 2004 Nov 15;68(10):1995-2002.
REF 202-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 21Virtual screening leads to the discovery of novel non-nucleotide P2Y??receptor antagonists. Bioorg Med Chem. 2012 Sep 1;20(17):5254-61.
REF 22Key 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 23[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.

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