Therapeutic Targets Database
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TTD Target ID: TTDS00189

Target Information
NameAdenosine A3 receptor    
Type of targetSuccessful target    
SynonymsA3 Adenosine receptor    
A3AR    
Adenosine 3 receptor    
Adenosine receptor A3A    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1][2][3]
Chronic ileitis
[ICD9: 555-558   ICD10: K50-K52]
[4]
Depression
[ICD9: 311   ICD10: F32]
[5]
Inflammatory bowel disease
[ICD9: 555, 556   ICD10: K50, K51]
[4]
Myocardial ischemia and reperfusion injury
[ICD9: 459.89   ICD10: I99.8]
[6][7]
Drug(s)AdenosineApprovedParoxysmal supraventricular tachycardia[1]
CF101Phase IIb completedRheumatoid arthritis[8]
CF101Phase II completedPsoriasis[8]
CF102Phase I/IIHepatocellular carcinoma, Hepatitis C infection[9]
CF502PreclinicalInflammation[9]
CF602PreclinicalInflammation[9]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP33765
PDB Structure1OEA; 1R7N.    
FunctionReceptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. possible role in reproduction.    
SequenceMPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIA VGVLVMPLAIVVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKR VTTHRRIWLALGLCWLVSFLVGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYF SFLTWIFIPLVVMCAIYLDIFYIIRNKLSLNLSNSKETGAFYGREFKTAKSLFLVLFLFA LSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPIVYAYKIKKFKETYLLILKAC VVCHPSDSLDTSIEKNSE
Related US Patent6,376,521
6,387,913
6,436,966
6,528,516
6,586,413
6,620,825
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (+)-BUTACLAMOL[10]
(+)-NIGULDIPINE[11]
(-)-NIGULDIPINE[11]
8-PHENYL THEOPHYLLINE[12]
9H-purine derivative[10]
9H-purine derivative[10]
BEMESETRON[10]
CGS-15943[13]
CGS-15943[14]
CGS-21680[15]
CIRSIMARITIN[16]
CVT-6883[17]
DIZOCILPINE[10]
GALANGIN[16]
GBR-12909[10]
GLUTAMATE[10]
GNF-PF-2224[18]
GW-328267[19]
ICI-118551[10]
KAINATE[10]
L-249313[20]
LUF-5417[21]
LUF-5433[21]
LUF-5767[22]
LUF-5816[23]
LUF-5956[24]
LUF-5957[24]
LUF-5962[24]
LUF-5978[23]
LUF-5980[23]
LUF-5981[23]
MESULERGINE[10]
METHOCTRAMINE[10]
METHYLTHIOADENOSINE[25]
METRIFUDIL[26]
N6-CYCLOPENTYLADENOSINE[27]
NECA[15]
NIPECOTIC ACID[10]
NITD609[28]
NSC-19028[16]
NSC-407228[16]
OSIP-339391[29]
REVERSINE[30]
SB-298[17]
SCH-442416[31]
SEROTONIN[10]
SLV-320[21]
Tonapofylline[21]
VUF-8504[13]
VUF-8507[13]
Agonist3-IB-MECA[5]
Adenosine[1]
CF101[8]
CF102[9]
CF502[9]
CF602[9]
Cl-IB-MECA[1][2][6]
IB-MECA[1]
AntagonistMRS-1220[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1A3 adenosine receptor as a target for cancer therapy. Anticancer Drugs. 2002 Jun;13(5):437-43. To Reference
Ref 2The A3 adenosine receptor as a new target for cancer therapy and chemoprotection. Exp Cell Res. 2001 Oct 1;269(2):230-6. To Reference
Ref 3Adenosine acts as an inhibitor of lymphoma cell growth: a major role for the A3 adenosine receptor. Eur J Cancer. 2000 Jul;36(11):1452-8. To Reference
Ref 4Rabbit chronic ileitis leads to up-regulation of adenosine A1/A3 gene products, oxidative stress, and immune modulation. Biochem Pharmacol. 2003 May 1;65(9):1529-38. To Reference
Ref 5A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 1993 Dec 20;336(1):57-60. To Reference
Ref 6A(3) adenosine receptor activation attenuates neutrophil function and neutrophil-mediated reperfusion injury. Am J Physiol. 1999 Nov;277(5 Pt 2):H1895-905. To Reference
Ref 7A physiological role of the adenosine A3 receptor: sustained cardioprotection. Proc Natl Acad Sci U S A. 1998 Jun 9;95(12):6995-9. To Reference
Ref 8Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96. To Reference
Ref 92011 Pipeline of Can-Fite BioPharm. To Reference
Ref 10J Med Chem. 2005 Nov 3;48(22):6887-96.2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. To Reference
Ref 11J Med Chem. 1999 Aug 12;42(16):3055-65.Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists. To Reference
Ref 12J Med Chem. 1982 Mar;25(3):197-207.Adenosine receptors: targets for future drugs. To Reference
Ref 13J Med Chem. 2006 Jul 13;49(14):4085-97.Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models. To Reference
Ref 14J Med Chem. 1998 Oct 8;41(21):3987-93.A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. To Reference
Ref 15J Med Chem. 1999 Apr 22;42(8):1384-92.5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. To Reference
Ref 16J Med Chem. 1996 Feb 2;39(3):781-8.Interactions of flavonoids and other phytochemicals with adenosine receptors. To Reference
Ref 17J Med Chem. 2009 Jul 9;52(13):3994-4006.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. To Reference
Ref 18Bioorg Med Chem. 2010 Nov 15;18(22):7890-9. Epub 2010 Sep 22.Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands. To Reference
Ref 19J Med Chem. 2004 Jul 29;47(16):4041-53.Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor. To Reference
Ref 20Bioorg Med Chem Lett. 2000 Jan 3;10(1):31-4.The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family. To Reference
Ref 21Bioorg Med Chem. 2010 Mar 15;18(6):2195-203. Epub 2010 Feb 4.2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. To Reference
Ref 22J Med Chem. 2004 Dec 16;47(26):6529-40.2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. To Reference
Ref 23J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. To Reference
Ref 24J Med Chem. 2006 May 18;49(10):2861-7.2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. To Reference
Ref 25J Med Chem. 2004 Apr 22;47(9):2243-55.Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative. To Reference
Ref 26J Med Chem. 2005 Mar 24;48(6):1745-58.(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. To Reference
Ref 27J Med Chem. 2005 Dec 29;48(26):8103-7.Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection. To Reference
Ref 28Science. 2010 Sep 3;329(5996):1175-80.Spiroindolones, a potent compound class for the treatment of malaria. To Reference
Ref 29Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. To Reference
Ref 30J Med Chem. 2005 Jul 28;48(15):4910-8."Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. To Reference
Ref 31Bioorg Med Chem Lett. 2010 Oct 1;20(19):5690-4. Epub 2010 Aug 10.Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. To Reference



 

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