8E1A
 
 | | Structure-based study to overcome cross-reactivity of novel androgen receptor inhibitors | | 分子名称: | 1,2-ETHANEDIOL, 4-[4-(3-fluoro-2-methoxyphenyl)-1,3-thiazol-2-yl]morpholine, Androgen receptor | | 著者 | Lallous, N, Li, H, Radaeva, M, Dalal, K, Leblanc, E, Ban, F, Ciesielski, F, Chow, B, Morin, M, Singh, K, Rennie, P.S, Cherkasov, A. | | 登録日 | 2022-08-10 | | 公開日 | 2022-09-14 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (1.2 Å) | | 主引用文献 | Structure-Based Study to Overcome Cross-Reactivity of Novel Androgen Receptor Inhibitors.
Cells, 11, 2022
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7ZTZ
 | | Crystal structure of mutant AR-LBD (Y764C) bound to dihydrotestosterone | | 分子名称: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, IMIDAZOLE, ... | | 著者 | Alegre-Marti, A, Jimenez-Panizo, A, Estebanez-Perpina, E, Fuentes-Prior, P. | | 登録日 | 2022-05-11 | | 公開日 | 2023-03-22 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | | 主引用文献 | A hotspot for posttranslational modifications on the androgen receptor dimer interface drives pathology and anti-androgen resistance.
Sci Adv, 9, 2023
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4OHA
 | | Crystal structure of T877A-AR-LBD bound with co-regulator peptide | | 分子名称: | Androgen receptor, HYDROXYFLUTAMIDE, SULFATE ION, ... | | 著者 | Liu, J.S, Hsu, C.L, Wu, W.G. | | 登録日 | 2014-01-17 | | 公開日 | 2014-08-20 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.42 Å) | | 主引用文献 | Identification of a new androgen receptor (AR) co-regulator BUD31 and related peptides to suppress wild-type and mutated AR-mediated prostate cancer growth via peptide screening and X-ray structure analysis.
Mol Oncol, 8, 2014
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5V8Q
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2AX6
 | | Crystal Structure Of The Androgen Receptor Ligand Binding Domain T877A Mutant In Complex With Hydroxyflutamide | | 分子名称: | Androgen receptor, HYDROXYFLUTAMIDE | | 著者 | Bohl, C.E, Miller, D.D, Chen, J, Bell, C.E, Dalton, J.T. | | 登録日 | 2005-09-03 | | 公開日 | 2005-09-20 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Structural Basis for Accommodation of Nonsteroidal Ligands in the Androgen Receptor
J.Biol.Chem., 280, 2005
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3L3X
 | | Crystal structure of DHT-bound androgen receptor in complex with the first motif of steroid receptor coactivator 3 | | 分子名称: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, Nuclear receptor coactivator 3 | | 著者 | Zhou, X.E, Suino-Powell, K.M, Li, J, He, A, MacKeigan, J.P, Melcher, K, Yong, E.-L, Xu, H.E. | | 登録日 | 2009-12-18 | | 公開日 | 2010-01-12 | | 最終更新日 | 2017-11-01 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | Identification of SRC3/AIB1 as a Preferred Coactivator for Hormone-activated Androgen Receptor.
J.Biol.Chem., 285, 2010
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8FH2
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8FH0
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8FGZ
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2AM9
 | | Crystal structure of human androgen receptor ligand binding domain in complex with testosterone | | 分子名称: | 2,3-DIHYDROXY-1,4-DITHIOBUTANE, Androgen receptor, GLYCEROL, ... | | 著者 | Pereira de Jesus-Tran, K, Cote, P.-L, Cantin, L, Blanchet, J, Labrie, F, Breton, R. | | 登録日 | 2005-08-09 | | 公開日 | 2006-05-16 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (1.64 Å) | | 主引用文献 | Comparison of crystal structures of human androgen receptor ligand-binding domain complexed with various agonists reveals molecular determinants responsible for binding affinity.
Protein Sci., 15, 2006
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3B66
 | | Crystal structure of the androgen receptor ligand binding domain in complex with SARM S-21 | | 分子名称: | 4-{[(1R,2S)-1,2-dihydroxy-2-methyl-3-(4-nitrophenoxy)propyl]amino}-2-(trifluoromethyl)benzonitrile, Androgen receptor | | 著者 | Bohl, C.E, Miller, D.D, Dalton, J.T. | | 登録日 | 2007-10-27 | | 公開日 | 2008-09-09 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators
Bioorg.Med.Chem.Lett., 18, 2008
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2PNU
 | | Crystal structure of human androgen receptor ligand-binding domain in complex with EM-5744 | | 分子名称: | (5S,8R,9S,10S,13R,14S,17S)-13-{2-[(3,5-DIFLUOROBENZYL)OXY]ETHYL}-17-HYDROXY-10-METHYLHEXADECAHYDRO-3H-CYCLOPENTA[A]PHENANTHREN-3-ONE, 2,3-DIHYDROXY-1,4-DITHIOBUTANE, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... | | 著者 | Cantin, L, Faucher, F, Couture, J.F, Pereira de Jesus-Tran, K, Legrand, P, Ciobanu, C.L, Singh, S.M, Labrie, F, Breton, R. | | 登録日 | 2007-04-25 | | 公開日 | 2007-09-11 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Structural Characterization of the Human Androgen Receptor Ligand-binding Domain Complexed with EM5744, a Rationally Designed Steroidal Ligand Bearing a Bulky Chain Directed toward Helix 12.
J.Biol.Chem., 282, 2007
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2AX9
 | | Crystal Structure Of The Androgen Receptor Ligand Binding Domain In Complex With R-3 | | 分子名称: | (R)-3-BROMO-2-HYDROXY-2-METHYL-N-[4-NITRO-3-(TRIFLUOROMETHYL)PHENYL]PROPANAMIDE, Androgen receptor | | 著者 | Bohl, C.E, Miller, D.D, Chen, J, Bell, C.E, Dalton, J.T. | | 登録日 | 2005-09-03 | | 公開日 | 2005-09-20 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Structural Basis for Accommodation of Nonsteroidal Ligands in the Androgen Receptor
J.Biol.Chem., 280, 2005
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1T65
 | | Crystal structure of the androgen receptor ligand binding domain with DHT and a peptide derived form its physiological coactivator GRIP1 NR box 2 bound in a non-helical conformation | | 分子名称: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, Nuclear receptor coactivator 2 | | 著者 | Estebanez-Perpina, E, Moore, J.M.R, Mar, E, Nguyen, P, Delgado-Rodrigues, E, Baxter, J.D, Webb, P, Fletterick, R.J, Guy, R.K. | | 登録日 | 2004-05-05 | | 公開日 | 2005-01-25 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (1.66 Å) | | 主引用文献 | The Molecular Mechanisms of Coactivator Utilization in Ligand-dependent Transactivation by the Androgen Receptor.
J.Biol.Chem., 280, 2005
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7ZU1
 | | Crystal structure of mutant AR-LBD (V758A) bound to dihydrotestosterone | | 分子名称: | 2,3-DIHYDROXY-1,4-DITHIOBUTANE, 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, ... | | 著者 | Alegre-Marti, A, Jimenez-Panizo, A, Estebanez-Perpina, E, Fuentes-Prior, P. | | 登録日 | 2022-05-11 | | 公開日 | 2023-03-22 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.68 Å) | | 主引用文献 | A hotspot for posttranslational modifications on the androgen receptor dimer interface drives pathology and anti-androgen resistance.
Sci Adv, 9, 2023
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8FH1
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3V49
 | | Structure of ar lbd with activator peptide and sarm inhibitor 1 | | 分子名称: | 4-[(4R)-4-(4-hydroxyphenyl)-3,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile, Androgen receptor, activator peptide, ... | | 著者 | 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. | | 登録日 | 2011-12-14 | | 公開日 | 2012-09-05 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
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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 | | 分子名称: | (2S)-3-[(4-cyanonaphthalen-1-yl)oxy]-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide, Androgen receptor | | 著者 | Bohl, C.E, Duke, C.B, Jones, A, Dalton, J.T, Miller, D.D. | | 登録日 | 2011-04-19 | | 公開日 | 2011-05-04 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
J.Med.Chem., 54, 2011
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2AX8
 | | Crystal Structure Of The Androgen Receptor Ligand Binding Domain W741L Mutant In Complex With S-1 | | 分子名称: | Androgen receptor, S-3-(4-FLUOROPHENOXY)-2-HYDROXY-2-METHYL-N-[4-NITRO-3-(TRIFLUOROMETHYL)PHENYL]PROPANAMIDE | | 著者 | Bohl, C.E, Miller, D.D, Chen, J, Bell, C.E, Dalton, J.T. | | 登録日 | 2005-09-03 | | 公開日 | 2005-09-20 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Structural Basis for Accommodation of Nonsteroidal Ligands in the Androgen Receptor
J.Biol.Chem., 280, 2005
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7ZU2
 | | Crystal structure of mutant AR-LBD (Q799E) bound to dihydrotestosterone | | 分子名称: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, IMIDAZOLE | | 著者 | Alegre-Marti, A, Jimenez-Panizo, A, Estebanez-Perpina, E, Fuentes-Prior, P. | | 登録日 | 2022-05-11 | | 公開日 | 2023-03-22 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.74 Å) | | 主引用文献 | A hotspot for posttranslational modifications on the androgen receptor dimer interface drives pathology and anti-androgen resistance.
Sci Adv, 9, 2023
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2AMB
 | | Crystal structure of human androgen receptor ligand binding domain in complex with tetrahydrogestrinone | | 分子名称: | 17-HYDROXY-18A-HOMO-19-NOR-17ALPHA-PREGNA-4,9,11-TRIEN-3-ONE, 2,3-DIHYDROXY-1,4-DITHIOBUTANE, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... | | 著者 | Pereira de Jesus-Tran, K, Cote, P.-L, Cantin, L, Blanchet, J, Labrie, F, Breton, R. | | 登録日 | 2005-08-09 | | 公開日 | 2006-05-16 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Comparison of crystal structures of human androgen receptor ligand-binding domain complexed with various agonists reveals molecular determinants responsible for binding affinity.
Protein Sci., 15, 2006
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2PIT
 | | Androgen receptor LBD with small molecule | | 分子名称: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, SULFATE ION, ... | | 著者 | Estebanez-Perpina, E, Arnold, A.A, Baxter, J.D, Webb, P, Guy, R.K, Fletterick, K.R. | | 登録日 | 2007-04-13 | | 公開日 | 2007-09-25 | | 最終更新日 | 2017-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.76 Å) | | 主引用文献 | A surface on the androgen receptor that allosterically regulates coactivator binding.
Proc.Natl.Acad.Sci.Usa, 104, 2007
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1Z95
 | | Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide | | 分子名称: | Androgen Receptor, R-BICALUTAMIDE, SULFATE ION | | 著者 | Bohl, C.E, Gao, W, Miller, D.D, Bell, C.E, Dalton, J.T. | | 登録日 | 2005-03-31 | | 公開日 | 2005-04-19 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structural basis for antagonism and resistance of bicalutamide in prostate cancer.
Proc.Natl.Acad.Sci.Usa, 102, 2005
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2OZ7
 | | Crystal structure of the human androgen receptor T877A mutant ligand-binding domain with cyproterone acetate | | 分子名称: | Androgen receptor, CYPROTERONE ACETATE | | 著者 | Bohl, C.E, Wu, Z, Miller, D.D, Bell, C.E, Dalton, J.T. | | 登録日 | 2007-02-25 | | 公開日 | 2007-03-27 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | 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
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4OEZ
 | | Crystal structure of AR-LBD bound with co-regulator peptide | | 分子名称: | 5-ALPHA-DIHYDROTESTOSTERONE, Androgen receptor, SULFATE ION, ... | | 著者 | Liu, J.S, Hsu, C.L, Wu, W.G. | | 登録日 | 2014-01-14 | | 公開日 | 2014-08-20 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Identification of a new androgen receptor (AR) co-regulator BUD31 and related peptides to suppress wild-type and mutated AR-mediated prostate cancer growth via peptide screening and X-ray structure analysis.
Mol Oncol, 8, 2014
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