Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00113

Target Information
NameP2Y purinoceptor 12    
Type of targetSuccessful target    
SynonymsADP-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    
DiseaseAggregation and activation of platelets[1]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[2]
Thrombosis
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[3][4][5]
Drug(s)ClopidogrelApprovedCoronary artery disease[3][4][5]
PrasugrelApprovedReduction of thrombotic cardiovascular events in patients with acute coronary syndrome undergoing percutaneous coronary intervention[6]
TiclopidineApprovedStroke[4][7]
BrilintaMAA and NDA FiledArterial thrombosis[8]
AR-C69931 MXPhase IIIAtherosclerosis; Percutaneous Coronary Intervention; Acute Coronary Syndrome; Cardiovascular diseases[9][10][5]
Brilinta/BriliquePhase IIIArterial thrombosis
Brilinta/BriliquePhase IIIOutcomes study in patients with PAD
Brilinta/BriliquePhase IIIOutcomes study in patients with prior MI
ClopidogrelINDThrombosis[11]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
UniProt IDQ9H244
PDB Structure1T78; 1VZ1; 1Y9C.    
FunctionReceptor for adp and atp coupled to g-proteins that inhibit the adenylyl cyclase second messenger system, which is not activated by udp and utp. Involved in platelets aggregation.    
SequenceMQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFI IFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITI DRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKS EFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFI IIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFF LCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM
Target ValidationClick to Find Target Validation Information.    
InhibitorADENOSINETRIPHOSPHATE[12]
PSB-0702[13]
PSB-0739[13]
Prasugrel[6]
AntagonistAR-C69931 MX[9][10][5]
Adenosine triphosphate analogues[3]
Brilinta[8]
Clopidogrel[11]
Clopidogrel[3][4][5]
Ticlopidine[4][7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1An elusive receptor is finally caught: P2Y(12'), an important drug target in platelets. Trends Pharmacol Sci. 2001 Aug;22(8):388-91. To Reference
Ref 2The P2Y12 receptor as a therapeutic target in cardiovascular disease. Platelets. 2001 Jun;12(4):197-209. To Reference
Ref 3Identification, characterization, and inhibition of the platelet ADP receptors. Int J Hematol. 2001 Dec;74(4):375-81. To Reference
Ref 4Scientific and therapeutic insights into the role of the platelet P2Y12 receptor in thrombosis. Curr Opin Hematol. 2003 Sep;10(5):333-8. To Reference
Ref 5In vivo blockade of platelet ADP receptor P2Y12 reduces embolus and thrombus formation but not thrombus stability. Arterioscler Thromb Vasc Biol. 2003 Mar 1;23(3):518-23. Epub 2003 Jan 23. To Reference
Ref 6Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. To Reference
Ref 7Molecular identification and characterization of the platelet ADP receptor targeted by thienopyridine antithrombotic drugs. J Clin Invest. 2001 Jun;107(12):1591-8. To Reference
Ref 8AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 9DG-041 inhibits the EP3 prostanoid receptor--a new target for inhibition of platelet function in atherothrombotic disease. Platelets. 2008 Dec;19(8):605-13. To Reference
Ref 10Detection of P2Y(14) protein in platelets and investigation of the role of P2Y(14) in platelet function in comparison with the EP(3) receptor. Thromb Haemost. 2008 Aug;100(2):261-70. To Reference
Ref 11Pharma & Vaccines. Product Development Pipeline. April 29 2009. To Reference
Ref 12J 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. To Reference
Ref 13J Med Chem. 2009 Jun 25;52(12):3784-93.High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543