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Target id: 628
Nomenclature: Androgen receptor
Systematic Nomenclature: NR3C4
Family: 3C. 3-Ketosteroid receptors
Gene and Protein Information ![]() |
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Species | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 920 | Xq12 | AR | androgen receptor | 7,19 |
Mouse | 899 | X 42.82 cM | Ar | androgen receptor | 21,56 |
Rat | 902 | Xq22 | Ar | androgen receptor | 81 |
Previous and Unofficial Names ![]() |
dihydrotestosterone receptor | AR | Andr | nuclear receptor subfamily 3 group C member 4 | AIS | DHTR | HUMARA | HYSP1 |
Database Links ![]() |
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Alphafold | P10275 (Hs), P19091 (Mm), P15207 (Rn) |
CATH/Gene3D | 2.130.10.10 |
ChEMBL Target | CHEMBL1871 (Hs), CHEMBL3056 (Mm), CHEMBL3072 (Rn) |
DrugBank Target | P10275 (Hs) |
Ensembl Gene | ENSG00000169083 (Hs), ENSMUSG00000046532 (Mm), ENSRNOG00000005639 (Rn) |
Entrez Gene | 367 (Hs), 11835 (Mm), 24208 (Rn) |
Human Protein Atlas | ENSG00000169083 (Hs) |
KEGG Gene | hsa:367 (Hs), mmu:11835 (Mm), rno:24208 (Rn) |
OMIM | 313700 (Hs) |
Orphanet | ORPHA132285 (Hs) |
Pharos | P10275 (Hs) |
RefSeq Nucleotide | NM_000044 (Hs), NM_001011645 (Hs), NM_013476 (Mm), NM_012502 (Rn) |
RefSeq Protein | NP_000035 (Hs), NP_001011645 (Hs), NP_038504 (Mm), NP_036634 (Rn) |
SynPHARM |
80692 (in complex with andarine) 6569 (in complex with cyproterone acetate) 6559 (in complex with dihydrotestosterone) 14316 (in complex with dihydrotestosterone) 14315 (in complex with hydroxyflutamide) 14314 (in complex with methyltrienolone) 8029 (in complex with [3H]methyltrienolone) |
UniProtKB | P10275 (Hs), P19091 (Mm), P15207 (Rn) |
Wikipedia | AR (Hs) |
Selected 3D Structures ![]() |
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Natural/Endogenous Ligands ![]() |
dihydrotestosterone |
testosterone |
Comments: Dihydrotestosterone has greater potency than testosterone |
Rank order of potency (Human) |
dihydrotestosterone > testosterone |
Download all structure-activity data for this target as a CSV file
Agonists ![]() |
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Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Combined treatment with drostanolone propionate and 5-fluoracil significantly increased the complete remission rate of induced mammary carcinomas in rats, compared to 5-fluoracil alone [83]. In a study comparing the competitive binding (displacement of [3H]methyltrienolone) of various anabolic steroids to the AR of skeletal muscle (rat and rabbit) and prostate tissue (rat), the binding of ethylestrenol was too low to determine its relative binding affinity [73]. A study by Krieg et al. (1976) examines the relative displaceable binding of nandrolone (aka 19-nortestosterone), testosterone and 5α-dihydrotestosterone to the rat androgen receptor [48]. |
Antagonists ![]() |
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Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific antagonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Enzalutamide antagonises testosterone-induced androgen-dependent gene transcription and nuclear translocation of the androgen receptor in human prostate LnCaP cells [28]. |
Co-binding Partners ![]() |
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Name | Interaction | Effect | Reference |
HMGB | Physical, Functional | DNA binding | 6,88 |
Hsp90 | Physical | Cellular localization, protein stability | 25,60 |
FKBP52 | Physical | Cellular Localization, Protein Stability, Development | 99 |
Co-binding Partners Comments | |||
FKBP52 (52 kDa FK506 binding protein) is a co-chaperone required for normal function of some, but not all steroid receptors. Elimination of FKBP52 in a mouse model reduces androgen receptor activity and yields a phenotype characteristic of partial androgen insensitivity syndrome (AIS). It is being tested as a therapeutic target in prostate cancer [99]. |
Main Co-regulators ![]() |
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Name | Activity | Specific | Ligand dependent | AF-2 dependent | Comments | References |
RNF14 | Co-activator | Yes | Yes | Yes | 40,42,64 | |
TGFB1I1 | Co-activator | Yes | Yes | Yes | 23,63,65,97 | |
RAN | Co-activator | Yes | Yes | Yes | 36,97 | |
SMARCD1 | Co-activator | - | No | - | 87 | |
CARM1 | Co-activator | - | No | - | 58 | |
NCOR1 | Co-repressor | - | No | - | 13,75 | |
NCOR2 | Co-repressor | - | No | - | 13,75 | |
NCOA2 | Co-activator | No | Yes | Yes | Histone acetyl transferase, also a nucleating platform for recruitment of general coactivators (CBP, CARM1, p300) | 26,43,96 |
NCOA4 | Co-activator | Yes | Yes | Yes | Increases AR expression, protein stability, and nuclear translocation. | 26,38,97 |
FHL2 | Co-activator | Yes | Yes | Yes | Contains 4 1/2 LIM domains | 11,68 |
NCOA3 | Co-activator | - | No | - | 62 | |
NCOA1 | Co-activator | - | No | - | 62,70 | |
MED1 | Co-activator | - | No | - | 16 | |
EP300 | Co-activator | - | No | - | 22 | |
KAT5 | Co-activator | - | No | - | 24 | |
UBE3A | Co-activator | - | No | - | 45 | |
KAT2B | Co-activator | - | No | - | 72 | |
CCND1 | Co-repressor | - | No | - | This entry refers to the CCND1a variant | 8 |
Main Co-regulators Comments | ||||||
More than 100 nuclear receptor coregulators have been identified. Initially, some were described as specific to a single receptor. However, most, if not all, of the coregulators have been shown to regulate more than one receptor as well as other transcription factors. For a complete listing of coregulators and their nuclear receptor interactions, see NURSA. Listed above are some of the better characterized androgen receptor coregulators. |
Main Target Genes ![]() |
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Name | Species | Effect | Technique | Comments | References |
Pbsn | Rat | Activated | Transient transfection | 71 | |
rsl | Mouse | Activated | Transient transfection, EMSA | 74 | |
C3 | Rat | Activated | Transient transfection, EMSA | 82 | |
human secretory component | Human | Activated | Transient transfection, EMSA | 31,89 | |
KLK3 | Human | Activated | ChIP, Transient transfection, EMSA, Footprint | Also observed in rodents | 15,100 |
transmembrane protease, serine 2 | Human | Activated | ChIP, Transient transfection, Endogenous gene | TMPRSS2-ERG fusion is the most common type of TMPRSS2 gene and ETS transcription factor fusion found in prostate cancer. | 52,85,93 |
Tissue Distribution ![]() |
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Functional Assays ![]() |
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Physiological Consequences of Altering Gene Expression ![]() |
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Phenotypes, Alleles and Disease Models ![]() |
Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Clinically-Relevant Mutations and Pathophysiology ![]() |
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Biologically Significant Variants ![]() |
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General Comments |
For more details on Androgen Receptor gene mutations please see The Androgen Receptor Gene Mutations Database. |
1. Ahrens-Fath I, Politz O, Geserick C, Haendler B. (2005) Androgen receptor function is modulated by the tissue-specific AR45 variant. FEBS J, 272 (1): 74-84. [PMID:15634333]
2. Akita K, Harada K, Ichihara J, Takata N, Takahashi Y, Saito K. (2013) A novel selective androgen receptor modulator, NEP28, is efficacious in muscle and brain without serious side effects on prostate. Eur J Pharmacol, 720 (1-3): 107-14. [PMID:24177288]
3. Antonarakis ES, Lu C, Wang H, Luber B, Nakazawa M, Roeser JC, Chen Y, Mohammad TA, Chen Y, Fedor HL et al.. (2014) AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer. N Engl J Med, 371 (11): 1028-38. [PMID:25184630]
4. Auerbach SS. DrugMatrix in vitro pharmacology data. Accessed on 30/04/2019. Modified on 30/04/2019. National Toxicology Program, https://ntp.niehs.nih.gov/drugmatrix/index.html
5. Bentvelsen FM, McPhaul MJ, Wilson CM, Wilson JD, George FW. (1996) Regulation of immunoreactive androgen receptor in the adrenal gland of the adult rat. Endocrinology, 137 (7): 2659-63. [PMID:8770883]
6. Boonyaratanakornkit V, Melvin V, Prendergast P, Altmann M, Ronfani L, Bianchi ME, Taraseviciene L, Nordeen SK, Allegretto EA, Edwards DP. (1998) High-mobility group chromatin proteins 1 and 2 functionally interact with steroid hormone receptors to enhance their DNA binding in vitro and transcriptional activity in mammalian cells. Mol Cell Biol, 18 (8): 4471-87. [PMID:9671457]
7. Brown CJ, Goss SJ, Lubahn DB, Joseph DR, Wilson EM, French FS, Willard HF. (1989) Androgen receptor locus on the human X chromosome: regional localization to Xq11-12 and description of a DNA polymorphism. Am J Hum Genet, 44 (2): 264-9. [PMID:2563196]
8. Burd CJ, Petre CE, Morey LM, Wang Y, Revelo MP, Haiman CA, Lu S, Fenoglio-Preiser CM, Li J, Knudsen ES et al.. (2006) Cyclin D1b variant influences prostate cancer growth through aberrant androgen receptor regulation. Proc Natl Acad Sci USA, 103 (7): 2190-5. [PMID:16461912]
9. Casimiro-Garcia A, Piotrowski DW, Ambler C, Arhancet GB, Banker ME, Banks T, Boustany-Kari CM, Cai C, Chen X, Eudy R et al.. (2014) Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist. J Med Chem, 57 (10): 4273-88. [PMID:24738581]
10. Chamness GC, Asch RH, Pauerstein CJ. (1980) Danazol binding and translocation of steroid receptors. Am J Obstet Gynecol, 136 (4): 426-9. [PMID:7355922]
11. Chan KK, Tsui SK, Ngai SM, Lee SM, Kotaka M, Waye MM, Lee CY, Fung KP. (2000) Protein-protein interaction of FHL2, a LIM domain protein preferentially expressed in human heart, with hCDC47. J Cell Biochem, 76 (3): 499-508. [PMID:10649446]
12. Chang C, Chen YT, Yeh SD, Xu Q, Wang RS, Guillou F, Lardy H, Yeh S. (2004) Infertility with defective spermatogenesis and hypotestosteronemia in male mice lacking the androgen receptor in Sertoli cells. Proc Natl Acad Sci USA, 101 (18): 6876-81. [PMID:15107499]
13. Cheng S, Brzostek S, Lee SR, Hollenberg AN, Balk SP. (2002) Inhibition of the dihydrotestosterone-activated androgen receptor by nuclear receptor corepressor. Mol Endocrinol, 16 (7): 1492-501. [PMID:12089345]
14. Choong CS, Sturm MJ, Strophair JA, McCulloch RK, Hurley DM. (1997) Reduced expression and normal nucleotide sequence of androgen receptor gene coding and promoter regions in a family with partial androgen insensitivity syndrome. Clin Endocrinol (Oxf), 46 (3): 281-8. [PMID:9156036]
15. Cleutjens KB, van Eekelen CC, van der Korput HA, Brinkmann AO, Trapman J. (1996) Two androgen response regions cooperate in steroid hormone regulated activity of the prostate-specific antigen promoter. J Biol Chem, 271 (11): 6379-88. [PMID:8626436]
16. Coulthard VH, Matsuda S, Heery DM. (2003) An extended LXXLL motif sequence determines the nuclear receptor binding specificity of TRAP220. J Biol Chem, 278 (13): 10942-51. [PMID:12556447]
17. Efstathiou E, Titus M, Wen S, Hoang A, Karlou M, Ashe R, Tu SM, Aparicio A, Troncoso P, Mohler J et al.. (2015) Molecular characterization of enzalutamide-treated bone metastatic castration-resistant prostate cancer. Eur Urol, 67 (1): 53-60. [PMID:24882673]
18. Fan W, Yanase T, Nomura M, Okabe T, Goto K, Sato T, Kawano H, Kato S, Nawata H. (2005) Androgen receptor null male mice develop late-onset obesity caused by decreased energy expenditure and lipolytic activity but show normal insulin sensitivity with high adiponectin secretion. Diabetes, 54 (4): 1000-8. [PMID:15793238]
19. Fang H, Tong W, Branham WS, Moland CL, Dial SL, Hong H, Xie Q, Perkins R, Owens W, Sheehan DM. (2003) Study of 202 natural, synthetic, and environmental chemicals for binding to the androgen receptor. Chem Res Toxicol, 16 (10): 1338-58. [PMID:14565775]
20. Ferraboschi P, Legnani L, Celasco G, Moro L, Ragonesi L, Colombo D. (2014) A full conformational characterization of antiandrogen cortexolone-17-propionate and related compounds through theoretical calculations and nuclear magnetic resonance spectroscopy. MedChemComm, 5: 904-914. DOI: 10.1039/C4MD00049H
21. Francke U, Taggart RT. (1980) Comparative gene mapping: order of loci on the X chromosome is different in mice and humans. Proc Natl Acad Sci USA, 77 (6): 3595-9. [PMID:6251472]
22. Fu M, Wang C, Reutens AT, Wang J, Angeletti RH, Siconolfi-Baez L, Ogryzko V, Avantaggiati ML, Pestell RG. (2000) p300 and p300/cAMP-response element-binding protein-associated factor acetylate the androgen receptor at sites governing hormone-dependent transactivation. J Biol Chem, 275 (27): 20853-60. [PMID:10779504]
23. Fujimoto N, Yeh S, Kang HY, Inui S, Chang HC, Mizokami A, Chang C. (1999) Cloning and characterization of androgen receptor coactivator, ARA55, in human prostate. J Biol Chem, 274 (12): 8316-21. [PMID:10075738]
24. Gaughan L, Logan IR, Cook S, Neal DE, Robson CN. (2002) Tip60 and histone deacetylase 1 regulate androgen receptor activity through changes to the acetylation status of the receptor. J Biol Chem, 277 (29): 25904-13. [PMID:11994312]
25. Georget V, Térouanne B, Nicolas JC, Sultan C. (2002) Mechanism of antiandrogen action: key role of hsp90 in conformational change and transcriptional activity of the androgen receptor. Biochemistry, 41 (39): 11824-31. [PMID:12269826]
26. Geserick C, Meyer HA, Barbulescu K, Haendler B. (2003) Differential modulation of androgen receptor action by deoxyribonucleic acid response elements. Mol Endocrinol, 17 (9): 1738-50. [PMID:12791770]
27. Giwercman A, Kledal T, Schwartz M, Giwercman YL, Leffers H, Zazzi H, Wedell A, Skakkebaek NE. (2000) Preserved male fertility despite decreased androgen sensitivity caused by a mutation in the ligand-binding domain of the androgen receptor gene. J Clin Endocrinol Metab, 85 (6): 2253-9. [PMID:10852459]
28. Guerrero J, Alfaro IE, Gómez F, Protter AA, Bernales S. (2013) Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate, 73 (12): 1291-305. [PMID:23765603]
29. Guo C, Linton A, Kephart S, Ornelas M, Pairish M, Gonzalez J, Greasley S, Nagata A, Burke BJ, Edwards M et al.. (2011) Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem, 54 (21): 7693-704. [PMID:21936524]
30. Guo Z, Yang X, Sun F, Jiang R, Linn DE, Chen H, Chen H, Kong X, Melamed J, Tepper CG et al.. (2009) A novel androgen receptor splice variant is up-regulated during prostate cancer progression and promotes androgen depletion-resistant growth. Cancer Res, 69 (6): 2305-13. [PMID:19244107]
31. Haelens A, Verrijdt G, Callewaert L, Peeters B, Rombauts W, Claessens F. (2001) Androgen-receptor-specific DNA binding to an element in the first exon of the human secretory component gene. Biochem J, 353 (Pt 3): 611-20. [PMID:11171058]
32. Hamann LG, Higuchi RI, Zhi L, Edwards JP, Wang XN, Marschke KB, Kong JW, Farmer LJ, Jones TK. (1998) Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. J Med Chem, 41 (4): 623-39. [PMID:9484511]
33. Han X, Zhao L, Xiang W, Qin C, Miao B, Xu T, Wang M, Yang CY, Chinnaswamy K, Stuckey J et al.. (2019) Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem, 62 (24): 11218-11231. [PMID:31804827]
34. Handratta VD, Vasaitis TS, Njar VC, Gediya LK, Kataria R, Chopra P, Newman Jr D, Farquhar R, Guo Z, Qiu Y et al.. (2005) Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model. J Med Chem, 48 (8): 2972-84. [PMID:15828836]
35. Higuchi RI, Arienti KL, López FJ, Mani NS, Mais DE, Caferro TR, Long YO, Jones TK, Edwards JP, Zhi L et al.. (2007) Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. J Med Chem, 50 (10): 2486-96. [PMID:17439112]
36. Hsiao PW, Lin DL, Nakao R, Chang C. (1999) The linkage of Kennedy's neuron disease to ARA24, the first identified androgen receptor polyglutamine region-associated coactivator. J Biol Chem, 274 (29): 20229-34. [PMID:10400640]
37. Hu R, Dunn TA, Wei S, Isharwal S, Veltri RW, Humphreys E, Han M, Partin AW, Vessella RL, Isaacs WB et al.. (2009) Ligand-independent androgen receptor variants derived from splicing of cryptic exons signify hormone-refractory prostate cancer. Cancer Res, 69 (1): 16-22. [PMID:19117982]
38. Hu YC, Yeh S, Yeh SD, Sampson ER, Huang J, Li P, Hsu CL, Ting HJ, Lin HK, Wang L, Kim E, Ni J, Chang C. (2004) Functional domain and motif analyses of androgen receptor coregulator ARA70 and its differential expression in prostate cancer. J Biol Chem, 279 (32): 33438-46. [PMID:15166229]
39. Iitsuka Y, Bock A, Nguyen DD, Samango-Sprouse CA, Simpson JL, Bischoff FZ. (2001) Evidence of skewed X-chromosome inactivation in 47,XXY and 48,XXYY Klinefelter patients. Am J Med Genet, 98 (1): 25-31. [PMID:11426451]
40. Ito K, Adachi S, Iwakami R, Yasuda H, Muto Y, Seki N, Okano Y. (2001) N-Terminally extended human ubiquitin-conjugating enzymes (E2s) mediate the ubiquitination of RING-finger proteins, ARA54 and RNF8. Eur J Biochem, 268 (9): 2725-32. [PMID:11322894]
41. Jung ME, Ouk S, Yoo D, Sawyers CL, Chen C, Tran C, Wongvipat J. (2010) Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC). J Med Chem, 53 (7): 2779-96. [PMID:20218717]
42. Kang HY, Yeh S, Fujimoto N, Chang C. (1999) Cloning and characterization of human prostate coactivator ARA54, a novel protein that associates with the androgen receptor. J Biol Chem, 274 (13): 8570-6. [PMID:10085091]
43. Kang Z, Pirskanen A, Jänne OA, Palvimo JJ. (2002) Involvement of proteasome in the dynamic assembly of the androgen receptor transcription complex. J Biol Chem, 277 (50): 48366-71. [PMID:12376534]
44. Kerkhofs S, Dubois V, De Gendt K, Helsen C, Clinckemalie L, Spans L, Schuit F, Boonen S, Vanderschueren D, Saunders PT et al.. (2012) A role for selective androgen response elements in the development of the epididymis and the androgen control of the 5α reductase II gene. FASEB J, 26 (10): 4360-72. [PMID:22798427]
45. Khan OY, Fu G, Ismail A, Srinivasan S, Cao X, Tu Y, Lu S, Nawaz Z. (2006) Multifunction steroid receptor coactivator, E6-associated protein, is involved in development of the prostate gland. Mol Endocrinol, 20 (3): 544-59. [PMID:16254014]
46. Kinoyama I, Taniguchi N, Toyoshima A, Nozawa E, Kamikubo T, Imamura M, Matsuhisa A, Samizu K, Kawanimani E, Niimi T et al.. (2006) (+)-(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. J Med Chem, 49 (2): 716-26. [PMID:16420057]
47. Kotula-Balak M, Bablok L, Fracki S, Jankowska A, Bilińska B. (2004) Immunoexpression of androgen receptors and aromatase in testes of patient with Klinefelter's syndrome. Folia Histochem Cytobiol, 42 (4): 215-20. [PMID:15704647]
48. Krieg M, Dennis M, Voigt KD. (1976) Comparison between the binding of 19-nortestosterone, 5alpha-dihydrotestosterone and testosterone in rat prostate and bulbocavernosus/levator ani muscle. J Endocrinol, 70 (3): 379-87. [PMID:978099]
49. Lee IR, Dawson SA, Wetherall JD, Hahnel R. (1987) Sex hormone-binding globulin secretion by human hepatocarcinoma cells is increased by both estrogens and androgens. J Clin Endocrinol Metab, 64 (4): 825-31. [PMID:3029159]
50. Li JJ, Iula DM, Nguyen MN, Hu LY, Dettling D, Johnson TR, Du DY, Shanmugasundaram V, Van Camp JA, Wang Z et al.. (2008) 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. J Med Chem, 51 (21): 7010-4. [PMID:18921992]
51. Liegibel UM, Sommer U, Boercsoek I, Hilscher U, Bierhaus A, Schweikert HU, Nawroth P, Kasperk C. (2003) Androgen receptor isoforms AR-A and AR-B display functional differences in cultured human bone cells and genital skin fibroblasts. Steroids, 68 (14): 1179-87. [PMID:14643880]
52. Lin B, Ferguson C, White JT, Wang S, Vessella R, True LD, Hood L, Nelson PS. (1999) Prostate-localized and androgen-regulated expression of the membrane-bound serine protease TMPRSS2. Cancer Res, 59 (17): 4180-4. [PMID:10485450]
53. Lin HY, Xu Q, Yeh S, Wang RS, Sparks JD, Chang C. (2005) Insulin and leptin resistance with hyperleptinemia in mice lacking androgen receptor. Diabetes, 54 (6): 1717-25. [PMID:15919793]
54. Linja MJ, Visakorpi T. (2004) Alterations of androgen receptor in prostate cancer. J Steroid Biochem Mol Biol, 92 (4): 255-64. [PMID:15663988]
55. Liu G, Sprenger C, Sun S, Epilepsia KS, Haugk K, Zhang X, Coleman I, Nelson PS, Plymate S. (2013) AR variant ARv567es induces carcinogenesis in a novel transgenic mouse model of prostate cancer. Neoplasia, 15 (9): 1009-17. [PMID:24027426]
56. Lyon MF, Hawkes SG. (1970) X-linked gene for testicular feminization in the mouse. Nature, 227 (5264): 1217-9. [PMID:5452809]
57. MacLean HE, Choi WT, Rekaris G, Warne GL, Zajac JD. (1995) Abnormal androgen receptor binding affinity in subjects with Kennedy's disease (spinal and bulbar muscular atrophy). J Clin Endocrinol Metab, 80 (2): 508-16. [PMID:7852512]
58. Majumder S, Liu Y, Ford 3rd OH, Mohler JL, Whang YE. (2006) Involvement of arginine methyltransferase CARM1 in androgen receptor function and prostate cancer cell viability. Prostate, 66 (12): 1292-301. [PMID:16705743]
59. Manfredi MC, Bi Y, Nirschl AA, Sutton JC, Seethala R, Golla R, Beehler BC, Sleph PG, Grover GJ, Ostrowski J et al.. (2007) 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. Bioorg Med Chem Lett, 17 (16): 4487-90. [PMID:17574413]
60. Marivoet S, Van Dijck P, Verhoeven G, Heyns W. (1992) Interaction of the 90-kDa heat shock protein with native and in vitro translated androgen receptor and receptor fragments. Mol Cell Endocrinol, 88 (1-3): 165-74. [PMID:1459337]
61. Maruyama K, Nakamura M, Tomoshige S, Sugita K, Makishima M, Hashimoto Y, Ishikawa M. (2013) Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist. Bioorg Med Chem Lett, 23 (14): 4031-6. [PMID:23768907]
62. McKenna NJ, Xu J, Nawaz Z, Tsai SY, Tsai MJ, O'Malley BW. (1999) Nuclear receptor coactivators: multiple enzymes, multiple complexes, multiple functions. J Steroid Biochem Mol Biol, 69 (1-6): 3-12. [PMID:10418975]
63. Mestayer C, Blanchère M, Jaubert F, Dufour B, Mowszowicz I. (2003) Expression of androgen receptor coactivators in normal and cancer prostate tissues and cultured cell lines. Prostate, 56 (3): 192-200. [PMID:12772188]
64. Miyamoto H, Rahman M, Takatera H, Kang HY, Yeh S, Chang HC, Nishimura K, Fujimoto N, Chang C. (2002) A dominant-negative mutant of androgen receptor coregulator ARA54 inhibits androgen receptor-mediated prostate cancer growth. J Biol Chem, 277 (7): 4609-17. [PMID:11673464]
65. Miyoshi Y, Ishiguro H, Uemura H, Fujinami K, Miyamoto H, Miyoshi Y, Kitamura H, Kubota Y. (2003) Expression of AR associated protein 55 (ARA55) and androgen receptor in prostate cancer. Prostate, 56 (4): 280-6. [PMID:12858356]
66. Mohler ML, Bohl CE, Jones A, Coss CC, Narayanan R, He Y, Hwang DJ, Dalton JT, Miller DD. (2009) Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. J Med Chem, 52 (12): 3597-617. [PMID:19432422]
67. Moilanen AM, Riikonen R, Oksala R, Ravanti L, Aho E, Wohlfahrt G, Nykänen PS, Törmäkangas OP, Palvimo JJ, Kallio PJ. (2015) Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. Sci Rep, 5: 12007. [PMID:26137992]
68. Müller JM, Isele U, Metzger E, Rempel A, Moser M, Pscherer A, Breyer T, Holubarsch C, Buettner R, Schüle R. (2000) FHL2, a novel tissue-specific coactivator of the androgen receptor. EMBO J, 19 (3): 359-69. [PMID:10654935]
69. Neuschmid-Kaspar F, Gast A, Peterziel H, Schneikert J, Muigg A, Ransmayr G, Klocker H, Bartsch G, Cato AC. (1996) CAG-repeat expansion in androgen receptor in Kennedy's disease is not a loss of function mutation. Mol Cell Endocrinol, 117 (2): 149-56. [PMID:8737374]
70. Powell SM, Christiaens V, Voulgaraki D, Waxman J, Claessens F, Bevan CL. (2004) Mechanisms of androgen receptor signalling via steroid receptor coactivator-1 in prostate. Endocr Relat Cancer, 11 (1): 117-30. [PMID:15027889]
71. Rennie PS, Bruchovsky N, Leco KJ, Sheppard PC, McQueen SA, Cheng H, Snoek R, Hamel A, Bock ME, MacDonald BS. (1993) Characterization of two cis-acting DNA elements involved in the androgen regulation of the probasin gene. Mol Endocrinol, 7 (1): 23-36. [PMID:8446105]
72. Reutens AT, Fu M, Wang C, Albanese C, McPhaul MJ, Sun Z, Balk SP, Jänne OA, Palvimo JJ, Pestell RG. (2001) Cyclin D1 binds the androgen receptor and regulates hormone-dependent signaling in a p300/CBP-associated factor (P/CAF)-dependent manner. Mol Endocrinol, 15 (5): 797-811. [PMID:11328859]
73. Saartok T, Dahlberg E, Gustafsson JA. (1984) Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin. Endocrinology, 114 (6): 2100-6. [PMID:6539197]
74. Scheller A, Scheinman RI, Thompson E, Scarlett CO, Robins DM. (1996) Contextual dependence of steroid receptor function on an androgen-responsive enhancer. Mol Cell Endocrinol, 121 (1): 75-86. [PMID:8865168]
75. Shang Y, Myers M, Brown M. (2002) Formation of the androgen receptor transcription complex. Mol Cell, 9 (3): 601-10. [PMID:11931767]
76. Simard J, Singh SM, Labrie F. (1997) Comparison of in vitro effects of the pure antiandrogens OH-flutamide, Casodex, and nilutamide on androgen-sensitive parameters. Urology, 49 (4): 580-6; discussion 586-9. [PMID:9111629]
77. Sun F, Chen HG, Li W, Yang X, Wang X, Jiang R, Guo Z, Chen H, Huang J, Borowsky AD et al.. (2014) Androgen receptor splice variant AR3 promotes prostate cancer via modulating expression of autocrine/paracrine factors. J Biol Chem, 289 (3): 1529-39. [PMID:24297183]
78. Sun S, Sprenger CC, Vessella RL, Haugk K, Soriano K, Mostaghel EA, Page ST, Coleman IM, Nguyen HM, Sun H et al.. (2010) Castration resistance in human prostate cancer is conferred by a frequently occurring androgen receptor splice variant. J Clin Invest, 120 (8): 2715-30. [PMID:20644256]
79. Sułek A, Hoffman-Zacharska D, Krysa W, Szirkowiec W, Fidziańska E, Zaremba J. (2005) CAG repeat polymorphism in the androgen receptor (AR) gene of SBMA patients and a control group. J Appl Genet, 46 (2): 237-9. [PMID:15876692]
80. Takeda H, Chodak G, Mutchnik S, Nakamoto T, Chang C. (1990) Immunohistochemical localization of androgen receptors with mono- and polyclonal antibodies to androgen receptor. J Endocrinol, 126 (1): 17-25. [PMID:2199591]
81. Tan JA, Joseph DR, Quarmby VE, Lubahn DB, Sar M, French FS, Wilson EM. (1988) The rat androgen receptor: primary structure, autoregulation of its messenger ribonucleic acid, and immunocytochemical localization of the receptor protein. Mol Endocrinol, 2 (12): 1276-85. [PMID:3216867]
82. Tan JA, Marschke KB, Ho KC, Perry ST, Wilson EM, French FS. (1992) Response elements of the androgen-regulated C3 gene. J Biol Chem, 267 (7): 4456-66. [PMID:1537831]
83. Teller MN, Stock CC, Bowie M, Chou TC, Budinger JM. (1982) Therapy of 7,12-dimethylbenz(a)anthracene-induced rat mammary carcinomas with combinations of 5-fluorouracil and 2 alpha-methyldihydrotestosterone propionate. Cancer Res, 42 (11): 4408-12. [PMID:6812946]
84. Tilley WD, Marcelli M, Wilson JD, McPhaul MJ. (1989) Characterization and expression of a cDNA encoding the human androgen receptor. Proc Natl Acad Sci USA, 86 (1): 327-31. [PMID:2911578]
85. Tomlins SA, Rhodes DR, Perner S, Dhanasekaran SM, Mehra R, Sun XW, Varambally S, Cao X, Tchinda J, Kuefer R et al.. (2005) Recurrent fusion of TMPRSS2 and ETS transcription factor genes in prostate cancer. Science, 310 (5748): 644-8. [PMID:16254181]
86. Tran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, Wongvipat J, Smith-Jones PM, Yoo D, Kwon A et al.. (2009) Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 324 (5928): 787-90. [PMID:19359544]
87. van de Wijngaart DJ, Dubbink HJ, Molier M, de Vos C, Trapman J, Jenster G. (2009) Functional screening of FxxLF-like peptide motifs identifies SMARCD1/BAF60a as an androgen receptor cofactor that modulates TMPRSS2 expression. Mol Endocrinol, 23 (11): 1776-86. [PMID:19762545]
88. Verrijdt G, Haelens A, Schoenmakers E, Rombauts W, Claessens F. (2002) Comparative analysis of the influence of the high-mobility group box 1 protein on DNA binding and transcriptional activation by the androgen, glucocorticoid, progesterone and mineralocorticoid receptors. Biochem J, 361 (Pt 1): 97-103. [PMID:11742533]
89. Verrijdt G, Schoenmakers E, Alen P, Haelens A, Peeters B, Rombauts W, Claessens F. (1999) Androgen specificity of a response unit upstream of the human secretory component gene is mediated by differential receptor binding to an essential androgen response element. Mol Endocrinol, 13 (9): 1558-70. [PMID:10478846]
90. von Geldern TW, Tu N, Kym PR, Link JT, Jae HS, Lai C, Apelqvist T, Rhonnstad P, Hagberg L, Koehler K et al.. (2004) Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. J Med Chem, 47 (17): 4213-30. [PMID:15293993]
91. Wakabayashi K, Imai K, Miyachi H, Hashimoto Y, Tanatani A. (2008) 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. Bioorg Med Chem, 16 (14): 6799-812. [PMID:18571420]
92. Wang LG, Liu XM, Kreis W, Budman DR. (1998) Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. Biochem Pharmacol, 55 (9): 1427-33. [PMID:10076535]
93. Wang Q, Li W, Liu XS, Carroll JS, Jänne OA, Keeton EK, Chinnaiyan AM, Pienta KJ, Brown M. (2007) A hierarchical network of transcription factors governs androgen receptor-dependent prostate cancer growth. Mol Cell, 27 (3): 380-92. [PMID:17679089]
94. Wilson CM, McPhaul MJ. (1994) A and B forms of the androgen receptor are present in human genital skin fibroblasts. Proc Natl Acad Sci USA, 91 (4): 1234-8. [PMID:8108393]
95. Wilson CM, McPhaul MJ. (1996) A and B forms of the androgen receptor are expressed in a variety of human tissues. Mol Cell Endocrinol, 120 (1): 51-7. [PMID:8809738]
96. Ye X, Han SJ, Tsai SY, DeMayo FJ, Xu J, Tsai MJ, O'Malley BW. (2005) Roles of steroid receptor coactivator (SRC)-1 and transcriptional intermediary factor (TIF) 2 in androgen receptor activity in mice. Proc Natl Acad Sci USA, 102 (27): 9487-92. [PMID:15983373]
97. Yeh S, Sampson ER, Lee DK, Kim E, Hsu CL, Chen YL, Chang HC, Altuwaijri S, Huang KE, Chang C. (2000) Functional analysis of androgen receptor N-terminal and ligand binding domain interacting coregulators in prostate cancer. J Formos Med Assoc, 99 (12): 885-94. [PMID:11155740]
98. Yin D, Gao W, Kearbey JD, Xu H, Chung K, He Y, Marhefka CA, Veverka KA, Miller DD, Dalton JT. (2003) Pharmacodynamics of selective androgen receptor modulators. J Pharmacol Exp Ther, 304 (3): 1334-40. [PMID:12604714]
99. Yong W, Yang Z, Periyasamy S, Chen H, Yucel S, Li W, Lin LY, Wolf IM, Cohn MJ, Baskin LS et al.. (2007) Essential role for Co-chaperone Fkbp52 but not Fkbp51 in androgen receptor-mediated signaling and physiology. J Biol Chem, 282 (7): 5026-36. [PMID:17142810]
100. Zhang S, Murtha PE, Young CY. (1997) Defining a functional androgen responsive element in the 5' far upstream flanking region of the prostate-specific antigen gene. Biochem Biophys Res Commun, 231 (3): 784-8. [PMID:9070893]
101. Zhang Z, Connolly PJ, Lim HK, Pande V, Meerpoel L, Teleha C, Branch JR, Ondrus J, Hickson I, Bush T et al.. (2021) Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC). J Med Chem, 64 (2): 909-924. [PMID:33470111]
102. Zhou T, Xu W, Zhang W, Sun Y, Yan H, Gao X, Wang F, Zhou Q, Hou J, Ren S et al.. (2020) Preclinical profile and phase I clinical trial of a novel androgen receptor antagonist GT0918 in castration-resistant prostate cancer. Eur J Cancer, 134: 29-40. [PMID:32460179]
103. Zhou XE, Suino-Powell KM, Li J, He Y, Mackeigan JP, Melcher K, Yong EL, Xu HE. (2010) Identification of SRC3/AIB1 as a preferred coactivator for hormone-activated androgen receptor. J Biol Chem, 285 (12): 9161-71. [PMID:20086010]
104. Zierau O, Kolodziejczyk A, Vollmer G, Machalz D, Wolber G, Thieme D, Keiler AM. (2019) Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay. J Steroid Biochem Mol Biol, 189: 81-86. [PMID:30825507]