Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

TTD Target ID: TTDS00367

Target Information
NameAndrogen receptor    
Type of targetSuccessful target    
SynonymsDihydrotestosterone receptor    
Testosterone receptor    
DiseaseProstate cancer    [1][2][3]
Spinal and bulbar muscular atrophy    [1]
Drug(s)BicalutamideApprovedAdvanced prostatic cancer[4][1]
CyproteroneApprovedProstate cancer[5]
DromostanoloneApprovedFemale androgenresponsive recurrent mammary cancer[6][7]
FluoxymesteroneApprovedMale hypogonadism[8][9]
FlutamideApprovedProstate Cancer[1]
HydroxyflutamideApprovedProstate cancer[10][11][12]
NandroloneApprovedOsteoporosis in post-menopausal women[13]
NilutamideApprovedProstate Cancer[14]
OxandroloneApprovedAlcoholic hepatitis[15]
TestosteroneApprovedReplacement therapy and osteoporosis[16][17]
APC-100Phase I/IIaCastration-resistant prostate cancer[18]
OstarinePreclinicalHypogonadism[19]
BioChemical ClassZinc-finger    
PathwayPathways in cancer
Prostate cancer
UniProt IDP10275
PDB Structure1E3G; 1GS4; 1T5Z; 1T63; 1T65; 1XJ7; 1XOW; 1XQ3.    
FunctionThe steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues.    
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[20]
11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol[21]
6,11-dihydrothiochromeno[4,3-b]indol-8-ol[21]
9alpha-Fluorocortisol[22]
APC-100[18]
CYPROTERONE ACETATE[23]
Calusterone[24]
Dihydrotestosterone[25]
Flufenamic Acid[26]
Methyltrienolone[27]
Mibolerone[28]
OXENDLONE[29]
Palodesangren C[29]
Palodesangren D[29]
Palodesangren E[29]
RU-59063[28]
WIN-49596[23]
ZANOTERONE[30]
AgonistBoldenone[27]
Delta1-dihydrotestosterone[31]
Fluoxymesterone[8][9]
Nandrolone[13]
Oxandrolone[15]
Testosterone[16][17]
AntagonistARN34[11]
Alpha-estradiol[12]
Bicalutamide[4][1]
Cyproterone[5]
Flutamide[1]
Hydroxyflutamide[10][11][12]
Nilutamide[14]
ModulatorOstarine[19]
BinderDromostanolone[6][7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Androgen receptor as a target in androgen-independent prostate cancer. Urology. 2002 Sep;60(3 Suppl 1):132-8; discussion 138-9. To Reference
Ref 2Modulation of nuclear receptor dependent transcription. Biol Res. 2002;35(2):295-303. To Reference
Ref 3Androgen receptor alterations in patients with disturbances in male sexual development and in prostatic carcinoma. Urol Int. 1995;54(1):2-5. To Reference
Ref 4Androgen receptor overexpression induces tamoxifen resistance in human breast cancer cells. Breast Cancer Res Treat. 2009 Jun 17. [Epub ahead of print] To Reference
Ref 5Coactivator selective regulation of androgen receptor activity. Steroids. 2009 Aug;74(8):669-74. Epub 2009 Mar 9. To Reference
Ref 6Endocrinological and pathological effects of anabolic-androgenic steroid in male rats. Endocr J. 2004 Aug;51(4):425-34. To Reference
Ref 7Effects of 5-fluorouracil and 2 alpha-methyldihydrotestosterone propionate on the growth of human breast carcinoma MCF-7 in vitro. Eur J Cancer Clin Oncol. 1983 Sep;19(9):1231-7. To Reference
Ref 8An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate. Endocrinology. 2007 Jan;148(1):363-73. Epub 2006 Oct 5. To Reference
Ref 9Endocrine-responsive pancreatic carcinoma: steroid binding and cytotoxicity studies in human tumor cell lines. Cancer Res. 1986 May;46(5):2276-81. To Reference
Ref 10Drug insight: role of the androgen receptor in the development and progression of prostate cancer. Nat Clin Pract Oncol. 2007 Apr;4(4):236-44. To Reference
Ref 11Ectopic expression of the amino-terminal peptide of androgen receptor leads to androgen receptor dysfunction and inhibition of androgen receptor-mediated prostate cancer growth. Mol Cell Endocrinol. 2004 Feb 12;214(1-2):175-87. To Reference
Ref 12Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. Biochem Pharmacol. 1998 May 1;55(9):1427-33. To Reference
Ref 13Expression of androgen receptor on fibroblast and hepatocyte of rats after deep second-degree burn caused by scalding. Sichuan Da Xue Xue Bao Yi Xue Ban. 2005 May;36(3):362-4. To Reference
Ref 14CX3CR1 is expressed by prostate epithelial cells and androgens regulate the levels of CX3CL1/fractalkine in the bone marrow: potential role in prostate cancer bone tropism. Cancer Res. 2008 Mar 15;68(6):1715-22. To Reference
Ref 15The effect of oxandrolone treatment on human osteoblastic cells. J Burns Wounds. 2007 Mar 7;6:e4. To Reference
Ref 16Molecular mechanism of androgen action. Trends Endocrinol Metab. 1998 Oct 1;9(8):317-24. To Reference
Ref 17Complexities of androgen action. J Am Acad Dermatol. 2001 Sep;45(3 Suppl):S87-94. To Reference
Ref 182011 Pipeline of Adamis Pharmaceuticals. To Reference
Ref 19Emerging drugs for hypogonadism. Expert Opin Emerg Drugs. 2006 Nov;11(4):685-707. To Reference
Ref 20J 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 21Bioorg Med Chem Lett. 2006 Jun 15;16(12):3233-7. Epub 2006 Apr 5.Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands. To Reference
Ref 22Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 23J Med Chem. 2000 Nov 30;43(24):4629-35.Chiral derivatives of 2-cyclohexylideneperhydro-4,7-methanoindenes, a novel class of nonsteroidal androgen receptor ligand: synthesis, X-ray analysis, and biological activity. To Reference
Ref 24Meli RJ, Ros PR: MR appearance of intra-abdominal metastatic melanoma. Magn Reson Imaging. 1992;10(4):705-8. To Reference
Ref 25Askew EB, Gampe RT Jr, Stanley TB, Faggart JL, Wilson EM: Modulation of androgen receptor activation function 2 by testosterone and dihydrotestosterone. J Biol Chem. 2007 Aug 31;282(35):25801-16. Epub 2007 Jun 25. To Reference
Ref 26Ouellet M, Percival MD: Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms. Biochem J. 1995 Feb 15;306 ( Pt 1):247-51. To Reference
Ref 27Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 28J Med Chem. 2000 Aug 24;43(17):3344-7.Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand. To Reference
Ref 29J Nat Prod. 1997 Oct;60(10):997-1002.Antiandrogenic natural Diels--Alder-type adducts from Brosimum rubescens. To Reference
Ref 30J Med Chem. 1992 May 15;35(10):1663-70.Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. To Reference
Ref 31Friedel A, Geyer H, Kamber M, Laudenbach-Leschowsky U, Schanzer W, Thevis M, Vollmer G, Zierau O, Diel P: 17beta-hydroxy-5alpha-androst-1-en-3-one (1-testosterone) is a potent androgen with anabolic properties. Toxicol Lett. 2006 Aug 20;165(2):149-55. Epub 2006 Apr 18. 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