7NKE
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![BU of 7nke by Molmil](/molmil-images/mine/7nke) | Crystal structure of human RXRalpha ligand binding domain in complex with 2,4-di-tert-butylphenol and a coactivator fragment | 分子名称: | 2,4-di~{tert}-butylphenol, FORMIC ACID, Nuclear receptor coactivator 2, ... | 著者 | Carivenc, C, Bourguet, W. | 登録日 | 2021-02-17 | 公開日 | 2022-03-02 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | 主引用文献 | 2,4-Di-tert-butylphenol Induces Adipogenesis in Human Mesenchymal Stem Cells by Activating Retinoid X Receptors. Endocrinology, 164, 2023
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7MSA
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![BU of 7msa by Molmil](/molmil-images/mine/7msa) | GDC-9545 in complex with estrogen receptor alpha | 分子名称: | (2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol, 3-[(1R,3R)-1-(2,6-difluoro-4-{[1-(3-fluoropropyl)azetidin-3-yl]amino}phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol, Estrogen receptor | 著者 | Kiefer, J.R, Vinogradova, M, Liang, J, Zbieg, J.R, Wang, X, Ortwine, D.F. | 登録日 | 2021-05-10 | 公開日 | 2021-06-02 | 最終更新日 | 2024-05-22 | 実験手法 | X-RAY DIFFRACTION (2.24 Å) | 主引用文献 | GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer. J.Med.Chem., 64, 2021
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7N9O
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![BU of 7n9o by Molmil](/molmil-images/mine/7n9o) | Estrogen Receptor Alpha Ligand Binding Domain in Complex with Aliphatic SERD S-C10(15) | 分子名称: | 10-{[3,17beta-dihydroxyestra-1,3,5(10)-trien-7beta-yl]sulfanyl}-N-methyl-N-propyldecanamide, Estrogen receptor | 著者 | Diennet, M, El Ezzy, M, Thiombane, K, Cotnoir-White, D, Poupart, J, Gao, Z, Mendoza, S.R, Marinier, A, Gleason, J, Mader, S.C, Fanning, S.W. | 登録日 | 2021-06-18 | 公開日 | 2022-07-06 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Estrogen Receptor Alpha Ligand Binding Domain in Complex with Aliphatic SERD S-C10(15) To Be Published
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8WFE
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![BU of 8wfe by Molmil](/molmil-images/mine/8wfe) | The Crystal Structure of PPARg from Biortus. | 分子名称: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, Peroxisome proliferator-activated receptor gamma | 著者 | Wang, F, Cheng, W, Lv, Z, Guo, S, Lin, D. | 登録日 | 2023-09-19 | 公開日 | 2023-11-22 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | The Crystal Structure of PPARg from Biortus. To Be Published
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2R6Y
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![BU of 2r6y by Molmil](/molmil-images/mine/2r6y) | Estrogen receptor alpha ligand-binding domain in complex with a SERM | 分子名称: | Estrogen receptor, [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone | 著者 | Wang, Y. | 登録日 | 2007-09-06 | 公開日 | 2008-04-08 | 最終更新日 | 2023-08-30 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Prediction of the tissue-specificity of selective estrogen receptor modulators by using a single biochemical method. Proc.Natl.Acad.Sci.Usa, 105, 2008
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7T2X
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![BU of 7t2x by Molmil](/molmil-images/mine/7t2x) | Estrogen Receptor Alpha Ligand Binding Domain Y537S in Complex with 2-chloro-4-((4-hydroxybenzyl)amino)-5-phenylthieno[2,3-d]pyrimidin-6-ol and GRIP Peptide | 分子名称: | Estrogen receptor, Nuclear receptor coactivator 2, S-(2-chloro-6-{[(4-hydroxyphenyl)methyl]amino}pyrimidin-4-yl) phenylethanethioate | 著者 | Joiner, C, Sammeta, V.K.R, Norris, J.D, McDonnell, D.P, Wilson, T.M, Fanning, S.W. | 登録日 | 2021-12-06 | 公開日 | 2022-06-22 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3- d ]pyrimidine Core. Acs Med.Chem.Lett., 13, 2022
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2REW
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![BU of 2rew by Molmil](/molmil-images/mine/2rew) | Crystal Structure of PPARalpha ligand binding domain with BMS-631707 | 分子名称: | (2S,3S)-1-(4-METHOXYPHENYL)-3-(3-(2-(5-METHYL-2-PHENYLOXAZOL-4-YL)ETHOXY)BENZYL)-4-OXOAZETIDINE-2-CARBOXYLIC ACID, N,N-BIS(3-D-GLUCONAMIDOPROPYL)DEOXYCHOLAMIDE, Peroxisome proliferator-activated receptor alpha | 著者 | Muckelbauer, J. | 登録日 | 2007-09-27 | 公開日 | 2007-11-27 | 最終更新日 | 2024-04-03 | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | 主引用文献 | Discovery of Azetidinone Acids as Conformationally-Constrained Dual (alpha/gamma) PPAR Activators To be Published
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7SQA
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![BU of 7sqa by Molmil](/molmil-images/mine/7sqa) | PPAR gamma LBD bound to SR10221 and SMRT corepressor motif | 分子名称: | (2S)-2-{5-[(5-{[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]-2-chlorophenoxy}propanoic acid, Nuclear receptor corepressor 2, Peroxisome proliferator-activated receptor gamma | 著者 | Frkic, R.L, Pederick, J.L, Bruning, J.B. | 登録日 | 2021-11-05 | 公開日 | 2023-05-10 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2.499 Å) | 主引用文献 | PPAR gamma Corepression Involves Alternate Ligand Conformation and Inflation of H12 Ensembles. Acs Chem.Biol., 18, 2023
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7SQB
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![BU of 7sqb by Molmil](/molmil-images/mine/7sqb) | PPAR gamma LBD bound to Inverse Agonist SR10221 | 分子名称: | (2S)-2-{5-[(5-{[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]-2-chlorophenoxy}propanoic acid, Peroxisome proliferator-activated receptor gamma | 著者 | Frkic, R.L, Pederick, J.L, Bruning, J.B. | 登録日 | 2021-11-05 | 公開日 | 2023-05-10 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | PPAR gamma Corepression Involves Alternate Ligand Conformation and Inflation of H12 Ensembles. Acs Chem.Biol., 18, 2023
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2V0V
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![BU of 2v0v by Molmil](/molmil-images/mine/2v0v) | Crystal Structure of Rev-Erb beta | 分子名称: | ORPHAN NUCLEAR RECEPTOR NR1D2 | 著者 | Woo, E.-J, Jeong, D.G, Lim, M.-Y, Jun Kim, S, Eon Ryu, S. | 登録日 | 2007-05-19 | 公開日 | 2007-10-23 | 最終更新日 | 2024-05-08 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Structural Insight Into the Constitutive Repression Function of the Nuclear Receptor Rev-Erbbeta J.Mol.Biol., 373, 2007
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7TT8
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![BU of 7tt8 by Molmil](/molmil-images/mine/7tt8) | Human LRH-1 LBD bound to agonist 6N-10CA and fragment of Tif2 coactivator | 分子名称: | 10-[(3aR,6S,6aR)-3-phenyl-3a-(1-phenylethenyl)-6-(sulfamoylamino)-1,3a,4,5,6,6a-hexahydropentalen-2-yl]decanoic acid (non-preferred name), Nuclear receptor coactivator 2, Nuclear receptor subfamily 5 group A member 2 | 著者 | Cato, M.L, Ortlund, E.A. | 登録日 | 2022-01-31 | 公開日 | 2022-05-11 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | 主引用文献 | Differential Modulation of Nuclear Receptor LRH-1 through Targeting Buried and Surface Regions of the Binding Pocket. J.Med.Chem., 65, 2022
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7TRB
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![BU of 7trb by Molmil](/molmil-images/mine/7trb) | CRYSTAL STRUCTURE OF FARNESOID X-ACTIVATED RECEPTOR COMPLEXED WITH COMPOUND-32 AKA (1S,3S)-N-({4-[5-(2-FLUOROPR OPAN-2-YL)-1,2,4-OXADIAZOL-3-YL]BICYCLO[2.2.2]OCTAN-1-YL}M ETHYL)-3-HYDROXY-N-[4'-(2-HYDROXYPROPAN-2-YL)-[1,1'-BIPHEN YL]-3-YL]-3-(TRIFLUOROMETHYL)CYCLOBUTANE-1-CARBOXAMIDE | 分子名称: | (1s,3s)-N-({4-[5-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-3-yl]bicyclo[2.2.2]octan-1-yl}methyl)-3-hydroxy-N-[4'-(2-hydroxypropan-2-yl)[1,1'-biphenyl]-3-yl]-3-(trifluoromethyl)cyclobutane-1-carboxamide, Bile acid receptor, co-activator | 著者 | Khan, J.A, Ruzanov, M. | 登録日 | 2022-01-28 | 公開日 | 2022-06-29 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | 主引用文献 | Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis. J.Med.Chem., 65, 2022
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2VV0
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![BU of 2vv0 by Molmil](/molmil-images/mine/2vv0) | hPPARgamma Ligand binding domain in complex with DHA | 分子名称: | DOCOSA-4,7,10,13,16,19-HEXAENOIC ACID, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA | 著者 | Itoh, T, Fairall, L, Schwabe, J.W.R. | 登録日 | 2008-06-02 | 公開日 | 2008-08-19 | 最終更新日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | 主引用文献 | Structural Basis for the Activation of Pparg by Oxidised Fatty Acids Nat.Struct.Mol.Biol., 15, 2008
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2VV3
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![BU of 2vv3 by Molmil](/molmil-images/mine/2vv3) | hPPARgamma Ligand binding domain in complex with 4-oxoDHA | 分子名称: | (6E,10Z,13Z,16Z,19Z)-4-oxodocosa-6,10,13,16,19-pentaenoic acid, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA | 著者 | Itoh, T, Fairall, L, Schwabe, J.W.R. | 登録日 | 2008-06-02 | 公開日 | 2008-08-19 | 最終更新日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | 主引用文献 | Structural Basis for the Activation of Ppargamma by Oxidized Fatty Acids. Nat.Struct.Mol.Biol., 15, 2008
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2VST
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![BU of 2vst by Molmil](/molmil-images/mine/2vst) | hPPARgamma Ligand binding domain in complex with 13-(S)-HODE | 分子名称: | (9Z,11E,13S)-13-hydroxyoctadeca-9,11-dienoic acid, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA | 著者 | Itoh, T, Fairall, L, Schwabe, J.W.R. | 登録日 | 2008-04-29 | 公開日 | 2008-08-19 | 最終更新日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | 主引用文献 | Structural Basis for the Activation of Pparg by Oxidised Fatty Acids Nat.Struct.Mol.Biol., 15, 2008
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2VV4
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![BU of 2vv4 by Molmil](/molmil-images/mine/2vv4) | hPPARgamma Ligand binding domain in complex with 6-oxoOTE | 分子名称: | (8E,10S,12Z)-10-hydroxy-6-oxooctadeca-8,12-dienoic acid, (8R,9Z,12Z)-8-hydroxy-6-oxooctadeca-9,12-dienoic acid, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA | 著者 | Itoh, T, Fairall, L, Schwabe, J.W.R. | 登録日 | 2008-06-02 | 公開日 | 2008-08-19 | 最終更新日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | 主引用文献 | Structural Basis for the Activation of Pparg by Oxidised Fatty Acids Nat.Struct.Mol.Biol., 15, 2008
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2VV2
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![BU of 2vv2 by Molmil](/molmil-images/mine/2vv2) | hPPARgamma Ligand binding domain in complex with 5-HEPA | 分子名称: | (5R,6E,8Z,11Z,14Z,17Z)-5-hydroxyicosa-6,8,11,14,17-pentaenoic acid, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA | 著者 | Itoh, T, Fairall, L, Schwabe, J.W.R. | 登録日 | 2008-06-02 | 公開日 | 2008-08-19 | 最終更新日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | 主引用文献 | Structural Basis for the Activation of Pparg by Oxidised Fatty Acids Nat.Struct.Mol.Biol., 15, 2008
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2W8Y
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![BU of 2w8y by Molmil](/molmil-images/mine/2w8y) | RU486 bound to the progesterone receptor in a destabilized agonistic conformation | 分子名称: | (14beta,17alpha)-17-ethynyl-17-hydroxyestr-4-en-3-one, 1,2-ETHANEDIOL, 11-(4-DIMETHYLAMINO-PHENYL)-17-HYDROXY-13-METHYL-17-PROP-1-YNYL-1,2,6,7,8,11,12,13,14,15,16,17-DODEC AHYDRO-CYCLOPENTA[A]PHENANTHREN-3-ONE, ... | 著者 | Raaijmakers, H.C.A, Versteeg, J, Uitdehaag, J.C.M. | 登録日 | 2009-01-20 | 公開日 | 2009-04-28 | 最終更新日 | 2024-05-08 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | The X-Ray Structure of Ru486 Bound to the Progesterone Receptor in a Destabilized Agonistic Conformation. J.Biol.Chem., 284, 2009
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2VSR
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![BU of 2vsr by Molmil](/molmil-images/mine/2vsr) | hPPARgamma Ligand binding domain in complex with 9-(S)-HODE | 分子名称: | (9S,10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA | 著者 | Itoh, T, Fairall, L, Schwabe, J.W.R. | 登録日 | 2008-04-29 | 公開日 | 2008-08-19 | 最終更新日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | 主引用文献 | Structural Basis for the Activation of Pparg by Oxidised Fatty Acids Nat.Struct.Mol.Biol., 15, 2008
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7UJ7
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![BU of 7uj7 by Molmil](/molmil-images/mine/7uj7) | |
7UJ8
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![BU of 7uj8 by Molmil](/molmil-images/mine/7uj8) | |
7UJY
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![BU of 7ujy by Molmil](/molmil-images/mine/7ujy) | Estrogen receptor alpha ligand binding domain Y537S mutant in complex with a methylated lasofoxifene derivative that enhances estrogen receptor alpha nuclear resonance time | 分子名称: | (5R,6S)-5-(4-{2-[(2R)-2-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor | 著者 | Hosfield, D.J, Greene, G.L, Fanning, S.W. | 登録日 | 2022-03-31 | 公開日 | 2022-06-15 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells. Elife, 11, 2022
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7UJW
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![BU of 7ujw by Molmil](/molmil-images/mine/7ujw) | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Possesses Selective Estrogen Receptor Degrader Activities | 分子名称: | (5R,6S)-5-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor | 著者 | Hosfield, D.J, Greene, G.L, Fanning, S.W. | 登録日 | 2022-03-31 | 公開日 | 2022-06-15 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells. Elife, 11, 2022
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7UJC
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![BU of 7ujc by Molmil](/molmil-images/mine/7ujc) | |
7UJO
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![BU of 7ujo by Molmil](/molmil-images/mine/7ujo) | Estrogen Receptor Alpha Ligand Binding Domain in Complex with RU39411 | 分子名称: | (9beta,11beta,17beta)-11-{4-[2-(dimethylamino)ethoxy]phenyl}estra-1,3,5(10)-triene-3,17-diol, Estrogen receptor, MAGNESIUM ION | 著者 | Hosfield, D.J, Greene, G.L, Fanning, S.W. | 登録日 | 2022-03-31 | 公開日 | 2022-06-15 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (1.449 Å) | 主引用文献 | Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells. Elife, 11, 2022
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