Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00332

Target Information
NamemRNA of androgen receptor    
Type of targetClinical trial target    
SynonymsmRNA of Dihydrotestosterone receptor    
mRNA of Nuclear receptor subfamily 3 group C member 4    
DiseaseProstate cancer
[ICD9: 185   ICD10: C61]
[1]
Drug(s)EZN-4176Phase IProstate cancer[1]
UniProt IDP10275
PDB Structure1E3G; 1GS4; 1T5Z; 1T63; 1T65; 1XJ7; 1XOW; 1XQ3; 1Z95; 2AM9; 2AMA; 2AMB; 2AO6; 2AX6; 2AX7; 2AX8; 2AX9; 2AXA; 2HVC; 2OZ7; 2PIO; 2PIP; 2PIQ; 2PIR; 2PIT; 2PIU; 2PIV; 2PIW; 2PIX; 2PKL; 2PNU; 2Q7I; 2Q7J; 2Q7K; 2Q7L; 2Z4J; 3B5R; 3B65; 3B66; 3B67; 3B68; 3BTR; 3L3X; 3L3Z; 3RLJ; 3RLL.    
FunctionSteroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3.    
SequenceMEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ QQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSA LECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLK DILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKA VSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKS TEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQSR DYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAAGP GSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGGEAGAVAPY GYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRLE TARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRND CTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKLT VSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAK ALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRM YSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDR IIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIIS VQVPKILSGKVKPIYFHTQ
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,2-dibromo-4- (1,2-dibromoethyl)cyclohexane[2]
2'-Hydroxy-3-methoxy-biphenyl-4-carbonitrile[3]
2-chloro-4- (o-tolyloxy)benzonitrile[4]
2-methoxy-4- (2-methoxyphenylthio)benzonitrile[5]
2-methoxy-4- (m-tolyloxy)benzonitrile[5]
2-methoxy-4- (o-tolyloxy)benzonitrile[5]
2-methoxy-4- (p-tolyloxy)benzonitrile[5]
2-methoxy-4- (propylthio)benzonitrile[5]
3,2'-bis-trifluoromethyl-biphenyl-4-carbonitrile[6]
3-chloro-4- (o-tolyloxy)benzonitrile[4]
3-chloro-4- (o-tolylthio)benzonitrile[5]
3-methoxy-4- (m-tolyloxy)benzonitrile[5]
3-methoxy-4- (o-tolyloxy)benzonitrile[5]
3-methoxy-4- (p-tolyloxy)benzonitrile[5]
4- (2,6-dimethylphenylthio)-2-methoxybenzonitrile[5]
4- (butylthio)-2-[5]
4- (butylthio)-2-methoxybenzonitrile[5]
4- (cyclobutylmethylthio)-2-methoxybenzonitrile[5]
4- (cyclopropylmethylthio)-2-methoxybenzonitrile[5]
4- (isopentylthio)-2-[5]
4- (isopentylthio)-2-methoxybenzonitrile[5]
4- (isopropylthio)-2-[5]
4- (isopropylthio)-2-methoxybenzonitrile[5]
4- (m-tolyloxy)-2-[4]
4- (mesityloxy)-2-[4]
4- (mesitylthio)-2-[5]
4- (mesitylthio)-2-methoxybenzonitrile[5]
4- (o-tolyloxy)-2-[4]
4- (o-tolylthio)-2-[5]
4- (p-tolyloxy)-2-[4]
4- (propylthio)-2-[5]
5-Methoxyflavone[7]
6-Hydroxyflavanone[7]
6-N-propyl -4-trifluoromethylquinolin-2 (1H)-one[8]
6-amino-4-trifluoromethylquinolin-2 (1H)-one[8]
AL-43[9]
APIGENIN[7]
BMS-564929[10]
CP-394531[11]
CP-409069[11]
Doxorubicin-Formaldehyde Conjugate[12]
Doxorubicin-Formaldehyde Conjugate[12]
EPIERENONE[13]
EUGENOL[14]
KAEMPFEROL[7]
LG-120838[15]
LG-121071,   LGD-121071[16]
LGD-2226[17]
LGD-5552[18]
NSC-19028[7]
NSC-26745[7]
ONAPRISTONE[19]
PF-0998425[3]
RU-43044[11]
RU-56187[20]
RU-58841[3]
TESTOSTERONE PROPIONATE[21]
WAY-252623[22]
WAY-255348[23]
YM-175735[24]
ZK-230211[25]
AntisenseEZN-4176[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 12011 Pipeline of Santaris Pharma. To Reference
Ref 2J Med Chem. 2006 Dec 14;49(25):7366-72.Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist. To Reference
Ref 3J Med Chem. 2008 Nov 13;51(21):7010-4. Epub 2008 Oct 16.Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications. To Reference
Ref 4Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8. Epub 2009 Mar 3.Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production. To Reference
Ref 5Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production. To Reference
Ref 6Bioorg Med Chem Lett. 2007 Oct 15;17(20):5529-32. Epub 2007 Aug 19.Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production. To Reference
Ref 7Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. Epub 2009 Jun 23.Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay. To Reference
Ref 8J Med Chem. 2006 Oct 19;49(21):6143-6.Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator. To Reference
Ref 9J Med Chem. 2003 Mar 13;46(6):1016-30.Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. To Reference
Ref 10J Med Chem. 2009 May 14;52(9):2794-8.N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation. To Reference
Ref 11J Med Chem. 2002 Jun 6;45(12):2417-24.Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. To Reference
Ref 12J Med Chem. 2004 Nov 4;47(23):5690-9.Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera. To Reference
Ref 13J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor. To Reference
Ref 14Bioorg Med Chem Lett. 2010 Apr 1;20(7):2111-4. Epub 2010 Feb 21.Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay. To Reference
Ref 15J Med Chem. 1998 Oct 22;41(22):4354-9.5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. To Reference
Ref 16J Med Chem. 2007 May 17;50(10):2486-96. Epub 2007 Apr 17.Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. To Reference
Ref 17Bioorg Med Chem Lett. 2007 Mar 15;17(6):1527-31. Epub 2007 Jan 8.Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. To Reference
Ref 18Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. Epub 2007 Nov 21.Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. To Reference
Ref 19Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8.Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. To Reference
Ref 20Bioorg Med Chem. 2010 May 1;18(9):3159-68. Epub 2010 Mar 19.Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists. To Reference
Ref 21Bioorg Med Chem Lett. 2007 Aug 15;17(16):4487-90. Epub 2007 Jun 6.Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators. To Reference
Ref 22J Med Chem. 2008 Nov 27;51(22):7161-8.Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. To Reference
Ref 23J Med Chem. 2008 Mar 27;51(6):1861-73. Epub 2008 Mar 5.Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348). To Reference
Ref 24J Med Chem. 2006 Jan 26;49(2):716-26.(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist. To Reference
Ref 25J Med Chem. 2000 Dec 28;43(26):5010-6.Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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