5CJ6
 
 | | Crystal Structure of a Selective Androgen Receptor Modulator Bound to the Ligand Binding Domain of the Human Androgen Receptor | | Descriptor: | 2-chloro-4-{[(1R,2R)-2-hydroxy-2-methylcyclopentyl]amino}-3-methylbenzonitrile, Androgen receptor, small peptide | | Authors: | Luz, J.G, Saeed, A, Wang, Y. | | Deposit date: | 2015-07-14 | | Release date: | 2016-01-06 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.07 Å) | | Cite: | 2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.
J.Med.Chem., 59, 2016
|
|
2QPY
 | | AR LBD with small molecule | | Descriptor: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, Coactivator peptide, ... | | Authors: | Estebanez-Perpina, E, Fletterick, R. | | Deposit date: | 2007-07-25 | | Release date: | 2007-09-25 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | A surface on the androgen receptor that allosterically regulates coactivator binding.
Proc.Natl.Acad.Sci.Usa, 104, 2007
|
|
3V4A
 | | Structure of ar lbd with activator peptide and sarm inhibitor 2 | | Descriptor: | (5R)-3-(3,4-dichlorophenyl)-5-(4-hydroxyphenyl)-1,5-dimethyl-2-thioxoimidazolidin-4-one, Androgen receptor, SULFATE ION | | Authors: | Nique, F, Hebbe, S, Peixoto, C, Annoot, D, Lefrancois, J.-M, Duval, E, Michoux, L, Triballeau, N, Lemoullec, J.M, Mollat, P, Thauvin, M, Prange, T, Minet, D, Clement-Lacroix, P, Robin-Jagerschmidt, C, Fleury, D, Guedin, D, Deprez, P. | | Deposit date: | 2011-12-14 | | Release date: | 2012-09-05 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
|
|
3V49
 | | Structure of ar lbd with activator peptide and sarm inhibitor 1 | | Descriptor: | 4-[(4R)-4-(4-hydroxyphenyl)-3,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile, Androgen receptor, activator peptide, ... | | Authors: | Nique, F, Hebbe, S, Peixoto, C, Annoot, D, Lefrancois, J.-M, Duval, E, Michoux, L, Triballeau, N, Lemoullec, J.-M, Mollat, P, Thauvin, M, Prange, T, Minet, D, Clement-Lacroix, P, Robin-Jagerschmidt, C, Fleury, D, Guedin, D, Deprez, P. | | Deposit date: | 2011-12-14 | | Release date: | 2012-09-05 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
|
|
8RM6
 | | Crystal Structure of Human Androgen Receptor DNA Binding Domain Bound to its Response Element: C3(1)ARE | | Descriptor: | C3(1)ARE_Chain C, C3(1)ARE_Chain D, Isoform 2 of Androgen receptor, ... | | Authors: | Lee, X.Y, Helsen, C, Van Eynde, W, Voet, A, Claessens, F. | | Deposit date: | 2024-01-05 | | Release date: | 2024-04-24 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Structural mechanism underlying variations in DNA binding by the androgen receptor.
J.Steroid Biochem.Mol.Biol., 241, 2024
|
|
8RM7
 | | Crystal Structure of Human Androgen Receptor DNA Binding Domain Bound to its Response Element: MMTV-177 GRE/ARE | | Descriptor: | Isoform 2 of Androgen receptor, MMTV-177 GRE/ARE Chain C, MMTV-177 GRE/ARE, ... | | Authors: | Lee, X.Y, Helsen, C, Van Eynde, W, Voet, A, Claessens, F. | | Deposit date: | 2024-01-05 | | Release date: | 2024-04-24 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | Structural mechanism underlying variations in DNA binding by the androgen receptor.
J.Steroid Biochem.Mol.Biol., 241, 2024
|
|
1XOW
 | | Crystal structure of the human androgen receptor ligand binding domain bound with an androgen receptor NH2-terminal peptide, AR20-30, and R1881 | | Descriptor: | (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE, androgen receptor, decamer fragment of androgen receptor | | Authors: | He, B, Gampe Jr, R.T, Kole, A.J, Hnat, A.T, Stanley, T.B, An, G, Stewart, E.L, Kalman, R.I, Minges, J.T, Wilson, E.M. | | Deposit date: | 2004-10-07 | | Release date: | 2004-11-16 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structural basis for androgen receptor interdomain and coactivator interactions suggests a transition in nuclear receptor activation function dominance
Mol.Cell, 16, 2004
|
|
3BTR
 | | AR-NLS:Importin-alpha complex | | Descriptor: | Androgen receptor, Importin subunit alpha-2 | | Authors: | Cutress, M.L, Whitaker, H.C, Mills, I.G, Stewart, M, Neal, D.E. | | Deposit date: | 2007-12-30 | | Release date: | 2008-12-30 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structural basis for the nuclear import of the human androgen receptor
J.Cell.Sci., 121, 2008
|
|
1Z95
 | | Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide | | Descriptor: | Androgen Receptor, R-BICALUTAMIDE, SULFATE ION | | Authors: | Bohl, C.E, Gao, W, Miller, D.D, Bell, C.E, Dalton, J.T. | | Deposit date: | 2005-03-31 | | Release date: | 2005-04-19 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structural basis for antagonism and resistance of bicalutamide in prostate cancer.
Proc.Natl.Acad.Sci.Usa, 102, 2005
|
|
5JJM
 | |
3ZQT
 | | TARGETING THE BINDING FUNCTION 3 SITE OF THE ANDROGEN RECEPTOR THROUGH IN SILICO MOLECULAR MODELING | | Descriptor: | 4-[(2R,3S)-3-[(3,4-DIHYDROXYPHENYL)METHYL]-2-METHYLBUTYL]BENZENE-1,2-DIOL, ANDROGEN RECEPTOR, SULFATE ION, ... | | Authors: | Lack, N.A, Axerio, P, Tavassoli, P, Kuchenbecker, K, Han, F.Q, Chan, K.H, Feau, C, LeBlanc, E, Tomlinson, E, Guy, R.K, Rennie, P.S, Cherkasov, A. | | Deposit date: | 2011-06-10 | | Release date: | 2011-12-07 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.29 Å) | | Cite: | Targeting the Binding Function 3 (Bf3) Site of the Human Androgen Receptor Through Virtual Screening.
J.Med.Chem., 54, 2011
|
|
4K7A
 | |
4HLW
 | | Targeting the Binding Function 3 (BF3) Site of the Human Androgen Receptor Through Virtual Screening. 2. Development of 2-((2-phenoxyethyl) thio)-1H-benzoimidazole derivatives. | | Descriptor: | 2-[(2-phenoxyethyl)sulfanyl]-1H-benzimidazole, Androgen receptor, GLYCEROL, ... | | Authors: | Ravi, S.N.M, Leblanc, E, Axerio-Cilies, P, Labriere, C, Frewin, K, Hassona, M.D.H, Lack, N.A, Han, F.Q, Guns, E.S, Young, R, Ban, F, Rennie, P.S, Cherkasov, A. | | Deposit date: | 2012-10-17 | | Release date: | 2013-01-23 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Targeting the Binding Function 3 (BF3) Site of the Androgen Receptor Through Virtual Screening. 2. Development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole Derivatives.
J.Med.Chem., 56, 2013
|
|
2HVC
 | | The Crystal Structure of Ligand-binding Domain (LBD) of human Androgen Receptor in Complex with a selective modulator LGD2226 | | Descriptor: | 6-[BIS(2,2,2-TRIFLUOROETHYL)AMINO]-4-(TRIFLUOROMETHYL)QUINOLIN-2(1H)-ONE, Androgen receptor | | Authors: | Wang, F, Liu, X.-Q, Li, H, Liang, K.-N, Miner, J.N, Hong, M, Kallel, E.A, van Oeveren, A, Zhi, L, Jiang, T. | | Deposit date: | 2006-07-28 | | Release date: | 2007-07-31 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226
ACTA CRYSTALLOGR.,SECT.F, 62, 2006
|
|
2OZ7
 | | Crystal structure of the human androgen receptor T877A mutant ligand-binding domain with cyproterone acetate | | Descriptor: | Androgen receptor, CYPROTERONE ACETATE | | Authors: | Bohl, C.E, Wu, Z, Miller, D.D, Bell, C.E, Dalton, J.T. | | Deposit date: | 2007-02-25 | | Release date: | 2007-03-27 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal structure of the T877A human androgen receptor ligand-binding domain complexed to cyproterone acetate provides insight for ligand-induced conformational changes and structure-based drug design.
J.Biol.Chem., 282, 2007
|
|
1E3G
 | | Human Androgen Receptor Ligand Binding in complex with the ligand metribolone (R1881) | | Descriptor: | (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE, ANDROGEN RECEPTOR | | Authors: | Matias, P.M, Donner, P, Coelho, R, Thomaz, M, Peixoto, C, Macedo, S, Otto, N, Joschko, S, Scholz, P, Wegg, A, Basler, S, Schafer, M, Ruff, M, Egner, U, Carrondo, M.A. | | Deposit date: | 2000-06-14 | | Release date: | 2001-06-14 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.
J. Biol. Chem., 275, 2000
|
|
5VO4
 | |
3L3Z
 | | Crystal structure of DHT-bound androgen receptor in complex with the third motif of steroid receptor coactivator 3 | | Descriptor: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, Nuclear receptor coactivator 3 | | Authors: | Zhou, X.E, Suino-Powell, K.M, Li, J, He, A, MacKeigan, J.P, Melcher, K, Yong, E.-L, Xu, H.E. | | Deposit date: | 2009-12-18 | | Release date: | 2010-01-12 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Identification of SRC3/AIB1 as a Preferred Coactivator for Hormone-activated Androgen Receptor.
J.Biol.Chem., 285, 2010
|
|
5T8J
 | |
5T8E
 | |
5V8Q
 | | Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs): Part III | | Descriptor: | 4-[(2S,3S)-2-ethyl-3-hydroxy-5-oxopyrrolidin-1-yl]-2-(trifluoromethyl)benzonitrile, Androgen receptor, GLYCEROL | | Authors: | Wilson, K.P. | | Deposit date: | 2017-03-22 | | Release date: | 2017-05-24 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (1.44 Å) | | Cite: | Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.
Bioorg. Med. Chem., 25, 2017
|
|
3RLL
 | | Crystal structure of the T877A androgen receptor ligand binding domain in complex with (S)-N-(4-Cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanonaphthalen-1-yloxy)-2-hydroxy-2-methylpropanamide | | Descriptor: | (2S)-3-[(4-cyanonaphthalen-1-yl)oxy]-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide, Androgen receptor | | Authors: | Bohl, C.E, Duke, C.B, Jones, A, Dalton, J.T, Miller, D.D. | | Deposit date: | 2011-04-19 | | Release date: | 2011-05-04 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
J.Med.Chem., 54, 2011
|
|
3L3X
 | | Crystal structure of DHT-bound androgen receptor in complex with the first motif of steroid receptor coactivator 3 | | Descriptor: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, Nuclear receptor coactivator 3 | | Authors: | Zhou, X.E, Suino-Powell, K.M, Li, J, He, A, MacKeigan, J.P, Melcher, K, Yong, E.-L, Xu, H.E. | | Deposit date: | 2009-12-18 | | Release date: | 2010-01-12 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Identification of SRC3/AIB1 as a Preferred Coactivator for Hormone-activated Androgen Receptor.
J.Biol.Chem., 285, 2010
|
|
3RLJ
 | | Crystal structure of the androgen receptor ligand binding domain in complex with SARM S-22 | | Descriptor: | (2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide, Androgen receptor | | Authors: | Bohl, C.E, Duke, C.B, Jones, A, Dalton, J.T, Miller, D.D. | | Deposit date: | 2011-04-19 | | Release date: | 2011-05-04 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
J.Med.Chem., 54, 2011
|
|
1GS4
 | | Structural basis for the glucocorticoid response in a mutant human androgen receptor (ARccr) derived from an androgen-independent prostate cancer | | Descriptor: | 9ALPHA-FLUOROCORTISOL, ANDROGEN RECEPTOR, PHOSPHATE ION | | Authors: | Matias, P.M, Carrondo, M.A, Coelho, R, Thomaz, M, Zhao, X.-Y, Wegg, A, Crusius, K, Egner, U, Donner, P. | | Deposit date: | 2001-12-27 | | Release date: | 2003-01-16 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structural Basis for the Glucocorticoid Response in a Mutant Human Androgen Receptor (Ar(Ccr)) Derived from an Androgen-Independent Prostate Cancer
J.Med.Chem., 45, 2002
|
|
