Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00081

Target Information
NameP2Y purinoceptor 1    
Type of targetResearch target    
SynonymsATP receptor    
Adenosine P2Y1 receptor    
P2Y(1) receptor    
P2Y1    
Purinergic receptor    
DiseaseThrombosis
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[1][2][3]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP47900
PDB Structure1Y36.    
FunctionReceptor 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.    
SequenceMTEVLWPAVPNGTDAAFLAGPGSSWGNSTVASTAAVSSSFKCALTKTGFQFYYLPAVYIL VFIIGFLGNSVAIWMFVFHMKPWSGISVYMFNLALADFLYVLTLPALIFYYFNKTDWIFG DAMCKLQRFIFHVNLYGSILFLTCISAHRYSGVVYPLKSLGRLKKKNAICISVLVWLIVV VAISPILFYSGTGVRKNKTITCYDTTSDEYLRSYFIYSMCTTVAMFCVPLVLILGCYGLI VRALIYKDLDNSPLRRKSIYLVIIVLTVFAVSYIPFHVMKTMNLRARLDFQTPAMCAFND RVYATYQVTRGLASLNSCVDPILYFLAGDTFRRRLSRATRKASRRSEANLQSKSEDMTLN ILPEFKQNGDTSL
Target ValidationClick to Find Target Validation Information.    
Inhibitor1- (3,4-dichlorophenyl)-3-[4]
Urea derivative[5]
Urea derivative[5]
Urea derivative[5]
Urea derivative[5]
AntagonistMRS-2179[2][6]
N: (6)-methyl-2'-deoxyadenosine-3':5'-bisphosphate[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Identification, characterization, and inhibition of the platelet ADP receptors. Int J Hematol. 2001 Dec;74(4):375-81. To Reference
Ref 2The 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. To Reference
Ref 3Platelet activation by ADP: the role of ADP antagonists. Ann Med. 2000 Dec;32 Suppl 1:15-20. To Reference
Ref 4Bioorg Med Chem Lett. 2008 Jun 1;18(11):3338-43. Epub 2008 Apr 15.P2Y1 receptor antagonists as novel antithrombotic agents. To Reference
Ref 5J Med Chem. 2005 Nov 3;48(22):7040-8.Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. To Reference
Ref 6Inhibition 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. To Reference
Ref 7Key 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. To Reference



 

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