3HZF
 
 | | Structure of TR-alfa bound to selective thyromimetic GC-1 in C2 space group | | 分子名称: | Thyroid hormone receptor, alpha isoform 1 variant, {4-[4-hydroxy-3-(1-methylethyl)benzyl]-3,5-dimethylphenoxy}acetic acid | | 著者 | Aparicio, R, Bleicher, L, Polikarpov, I. | | 登録日 | 2009-06-23 | | 公開日 | 2009-07-21 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Structural basis of GC-1 selectivity for thyroid hormone receptor isoforms.
Bmc Struct.Biol., 8, 2008
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3HVL
 | | Tethered PXR-LBD/SRC-1p complexed with SR-12813 | | 分子名称: | Pregnane X receptor, Linker, Steroid receptor coactivator 1, ... | | 著者 | Lesburg, C.A, Wang, W, Prosise, W.W, Chen, J, Taremi, S.S, Le, H.V, Madison, V, Cui, X, Thomas, A, Cheng, K.C. | | 登録日 | 2009-06-16 | | 公開日 | 2009-08-04 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Construction and characterization of a fully active PXR/SRC-1 tethered protein with increased stability
Protein Eng.Des.Sel., 21, 2008
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3HQ5
 | | Progesterone Receptor bound to an Alkylpyrrolidine ligand. | | 分子名称: | 2-chloro-4-{[(3S)-1-methylpyrrolidin-3-yl][2-(trifluoromethyl)benzyl]amino}benzonitrile, GLYCEROL, Progesterone receptor, ... | | 著者 | Madauss, K.P, Williams, S.P, Washburn, D.G. | | 登録日 | 2009-06-05 | | 公開日 | 2010-03-02 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Bioorg.Med.Chem.Lett., 19, 2009
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3HOD
 | | Crystal structure of the PPARgamma-LBD complexed with a new aryloxy-3phenylpropanoic acid | | 分子名称: | (2S)-2-(4-benzylphenoxy)-3-phenylpropanoic acid, Peroxisome proliferator-activated receptor gamma | | 著者 | Pochetti, G, Montanari, R, Mazza, F, Loiodice, F, Fracchiolla, G, Laghezza, A, Lavecchia, A, Novellino, E. | | 登録日 | 2009-06-02 | | 公開日 | 2009-10-27 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | New 2-Aryloxy-3-phenyl-propanoic Acids As Peroxisome Proliferator-Activated Receptors alpha/gamma Dual Agonists with Improved Potency and Reduced Adverse Effects on Skeletal Muscle Function
J.Med.Chem., 52, 2009
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3HO0
 | | Crystal structure of the PPARgamma-LBD complexed with a new aryloxy-3phenylpropanoic acid | | 分子名称: | (2S)-2-(4-phenethylphenoxy)-3-phenyl-propanoic acid, Peroxisome proliferator-activated receptor gamma | | 著者 | Pochetti, G, Montanari, R, Mazza, F, Loiodice, F, Fracchiolla, G, Laghezza, A, Lavecchia, A, Novellino, E. | | 登録日 | 2009-06-01 | | 公開日 | 2009-10-27 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | New 2-Aryloxy-3-phenyl-propanoic Acids As Peroxisome Proliferator-Activated Receptors alpha/gamma Dual Agonists with Improved Potency and Reduced Adverse Effects on Skeletal Muscle Function
J.Med.Chem., 52, 2009
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3HM1
 | | Crystal structure of human Estrogen Receptor Alpha Ligand-Binding Domain in complex with a Glucocorticoid Receptor Interacting Protein 1 Nr Box II Peptide and estrone ((8R,9S,13S,14S)-3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one) | | 分子名称: | (9beta,13alpha)-3-hydroxyestra-1,3,5(10)-trien-17-one, Estrogen receptor, Nuclear receptor coactivator 2 | | 著者 | Rajan, S.S, Kim, Y, Vanek, K, Liwanag, M, Joachimiak, A, Greene, G.L. | | 登録日 | 2009-05-28 | | 公開日 | 2010-06-02 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | | 主引用文献 | Crystal structure of human Estrogen Receptor Alpha Ligand-Binding Domain in complex with a Glucocorticoid Receptor Interacting Protein 1 Nr Box II Peptide and estrone ((8R,9S,13S,14S)-3-hydroxy-13-methyl-7,8,9,11,12,14,15, 16-octahydro-6H-cyclopenta[a]phenanthren-17-one)
To be Published
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3HLV
 | | Crystal structure of human Estrogen Receptor Alpha Ligand-Binding Domain in complex with a Glucocorticoid Receptor Interacting Protein 1 Nr Box II Peptide and 16-alpha-hydroxy-estrone ((8S,9R,13S,14R,16R)-3,16-dihydroxy-13-methyl-7,8,9,11,12,14,15, 16-octahydro-6H-cyclopenta[a]phenanthren-17-one | | 分子名称: | (9beta,13alpha,16beta)-3,16-dihydroxyestra-1,3,5(10)-trien-17-one, Estrogen receptor, Nuclear receptor coactivator 2 | | 著者 | Rajan, S.S, Kim, Y, Vanek, K, Joachimiak, A, Greene, G.L. | | 登録日 | 2009-05-28 | | 公開日 | 2010-06-02 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Crystal structure of human alphaER-LBD in complex with GRIP peptide and 16alpha-hydroxyestrone
To be Published
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3HC6
 | | FXR with SRC1 and GSK088 | | 分子名称: | 3-[(5-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}-1H-indol-1-yl)methyl]benzoic acid, Bile acid receptor, Nuclear receptor coactivator 1, ... | | 著者 | Williams, S.P, Madauss, K.P. | | 登録日 | 2009-05-05 | | 公開日 | 2009-07-21 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | FXR agonist activity of conformationally constrained analogs of GW 4064.
Bioorg.Med.Chem.Lett., 19, 2009
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3HC5
 | | FXR with SRC1 and GSK826 | | 分子名称: | 3-(6-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}-1-benzothiophen-2-yl)benzoic acid, Bile acid receptor, Nuclear receptor coactivator 1, ... | | 著者 | Williams, S.P, Madauss, K.P. | | 登録日 | 2009-05-05 | | 公開日 | 2009-07-21 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | FXR agonist activity of conformationally constrained analogs of GW 4064.
Bioorg.Med.Chem.Lett., 19, 2009
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3H52
 | | Crystal structure of the antagonist form of human glucocorticoid receptor | | 分子名称: | 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, GLYCEROL, Glucocorticoid receptor, ... | | 著者 | Schoch, G.A, Benz, J, D'Arcy, B, Stihle, M, Burger, D, Thoma, R, Ruf, A. | | 登録日 | 2009-04-21 | | 公開日 | 2009-12-01 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Molecular switch in the glucocorticoid receptor: active and passive antagonist conformations
J.Mol.Biol., 395, 2010
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3H0A
 | | Crystal Structure of Peroxisome Proliferator-Activated Receptor Gamma (PPARg) and Retinoic Acid Receptor Alpha (RXRa) in Complex with 9-cis Retinoic Acid, Co-activator Peptide, and a Partial Agonist | | 分子名称: | 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl]benzoic acid, Nuclear receptor coactivator 1, Co-activator Peptide, ... | | 著者 | Wang, Z, Sudom, A, Walker, N.P. | | 登録日 | 2009-04-08 | | 公開日 | 2009-06-09 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Bioorg.Med.Chem.Lett., 19, 2009
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3GZ9
 | | Crystal Structure of Peroxisome Proliferator-Activated Receptor Delta (PPARd) in Complex with a Full Agonist | | 分子名称: | (2,3-dimethyl-4-{[2-(prop-2-yn-1-yloxy)-4-{[4-(trifluoromethyl)phenoxy]methyl}phenyl]sulfanyl}phenoxy)acetic acid, Peroxisome proliferator-activated receptor delta, heptyl beta-D-glucopyranoside | | 著者 | Wang, Z, Sudom, A, Walker, N.P. | | 登録日 | 2009-04-06 | | 公開日 | 2009-06-30 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Bioorg.Med.Chem.Lett., 19, 2009
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3GYU
 | | Nuclear receptor DAF-12 from parasitic nematode Strongyloides stercoralis in complex with its physiological ligand dafachronic acid delta 7 | | 分子名称: | (5beta,14beta,17alpha,25R)-3-oxocholest-7-en-26-oic acid, Nuclear hormone receptor of the steroid/thyroid hormone receptors superfamily, SRC1 | | 著者 | Zhou, X.E, Wang, Z, Suino-Powell, K, Motola, D.L, Conneely, A, Ogata, C, Sharma, K.K, Auchus, R.J, Kliewer, S.A, Xu, H.E, Mangelsdorf, D.J. | | 登録日 | 2009-04-05 | | 公開日 | 2009-07-07 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Identification of the nuclear receptor DAF-12 as a therapeutic target in parasitic nematodes.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3GYT
 | | Nuclear receptor DAF-12 from parasitic nematode Strongyloides stercoralis in complex with its physiological ligand dafachronic acid delta 4 | | 分子名称: | (14beta,17alpha,25R)-3-oxocholest-4-en-26-oic acid, Nuclear hormone receptor of the steroid/thyroid hormone receptors superfamily, SRC1 | | 著者 | Zhou, X.E, Wang, Z, Suino-Powell, K, Motola, D.L, Conneely, A, Ogata, C, Sharma, K.K, Auchus, R.J, Kliewer, S.A, Xu, H.E, Mangelsdorf, D.J. | | 登録日 | 2009-04-05 | | 公開日 | 2009-07-07 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Identification of the nuclear receptor DAF-12 as a therapeutic target in parasitic nematodes.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3GWX
 | | MOLECULAR RECOGNITION OF FATTY ACIDS BY PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS | | 分子名称: | 5,8,11,14,17-EICOSAPENTAENOIC ACID, PROTEIN (PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR (PPAR-DELTA)) | | 著者 | Xu, H.E, Lambert, M.H, Montana, V.G, Parks, D.J, Blanchard, S.G, Brown, P.J, Sternbach, D.D, Lehmann, J.M, Wisely, G.B, Willson, T.M, Kliewer, S.A, Milburn, M.V. | | 登録日 | 1999-04-26 | | 公開日 | 2000-04-26 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Molecular recognition of fatty acids by peroxisome proliferator-activated receptors.
Mol.Cell, 3, 1999
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3GWS
 | | Crystal Structure of T3-Bound Thyroid Hormone Receptor | | 分子名称: | 3,5,3'TRIIODOTHYRONINE, Thyroid hormone receptor beta | | 著者 | Nascimento, A.S, Dias, S.M.G, Nunes, F.M, Aparicio, R, Polikarpov, I, Baxter, J.D, Webb, P. | | 登録日 | 2009-04-01 | | 公開日 | 2009-04-28 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structural rearrangements in the thyroid hormone receptor hinge domain and their putative role in the receptor function
J.Mol.Biol., 360, 2006
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3GD2
 | | isoxazole ligand bound to farnesoid X receptor (FXR) | | 分子名称: | 3-[(E)-2-(2-chloro-4-{[3-{[(R)-(2,6-dichlorophenyl)(hydroxy)-lambda~4~-sulfanyl]methyl}-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid, Bile acid receptor, activator peptide | | 著者 | Madauss, K.P, Williams, S.P, Deaton, D.N, Wisely, G.B, Mcfadyen, R.B. | | 登録日 | 2009-02-23 | | 公開日 | 2009-07-07 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.
Bioorg.Med.Chem.Lett., 19, 2009
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3GBK
 | | Crystal Structure of Human PPAR-gamma Ligand Binding Domain Complexed with a Potent and Selective Agonist | | 分子名称: | 2-[(1-{3-[4-(biphenyl-4-ylcarbonyl)-2-propylphenoxy]propyl}-1,2,3,4-tetrahydroquinolin-5-yl)oxy]-2-methylpropanoic acid, Peroxisome proliferator-activated receptor gamma | | 著者 | Peng, Y.-H, Lin, C.-H, Hsieh, H.-P, Wu, S.-Y. | | 登録日 | 2009-02-19 | | 公開日 | 2009-12-29 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists
J.Med.Chem., 52, 2009
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3G9E
 | | Aleglitaar. a new. potent, and balanced dual ppara/g agonist for the treatment of type II diabetes | | 分子名称: | (2S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}propanoic acid, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma | | 著者 | Ruf, A, Benz, J, Bernardeau, A, Binggeli, A, Blum, D, Boehringer, M, Grether, U, Hilpert, H, Kuhn, B, Maerki, H.P, Meyer, M, Puenterner, K, Raab, S, Schlatter, D, Gsell, B, Stihle, M, Mohr, P. | | 登録日 | 2009-02-13 | | 公開日 | 2009-06-02 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
Bioorg.Med.Chem.Lett., 19, 2009
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3G8O
 | | Progesterone Receptor with bound Pyrrolidine 1 | | 分子名称: | N~2~-[4-cyano-3-(trifluoromethyl)phenyl]-N,N-dimethyl-N~2~-(2,2,2-trifluoroethyl)-L-alaninamide, Progesterone receptor, SULFATE ION | | 著者 | Thompson, S.K, Washburn, D.G, Madauss, K.P, Williams, S.P, Stewart, E.L. | | 登録日 | 2009-02-12 | | 公開日 | 2010-02-16 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Bioorg.Med.Chem.Lett., 19, 2009
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3G8I
 | | Aleglitazar, a new, potent, and balanced PPAR alpha/gamma agonist for the treatment of type II diabetes | | 分子名称: | (2S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}propanoic acid, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor alpha | | 著者 | Benz, J, Bernardeau, A, Binggeli, A, Blum, D, Boehringer, M, Grether, U, Hilpert, H, Kuhn, B, Maerki, H.P, Meyer, M, Puentener, K, Raab, S, Ruf, A, Schlatter, D, Gsell, B, Stihle, M, Mohr, P. | | 登録日 | 2009-02-12 | | 公開日 | 2009-06-02 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
Bioorg.Med.Chem.Lett., 19, 2009
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3G0W
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3FXV
 | | Identification of an N-oxide pyridine GW4064 analogue as a potent FXR agonist | | 分子名称: | 12-meric peptide from Nuclear receptor coactivator 1, 6-(4-{[3-(3,5-dichloropyridin-4-yl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}-2-methylphenyl)-1-methyl-1H-indole-3-carbox ylic acid, NR1H4 protein | | 著者 | Feng, S, Yang, M, He, Y, Chen, L, Zhang, Z, Wang, Z, Hong, D, Richter, H, Benson, G.M, Bleicher, K, Grether, U, Martin, R, Plancher, J.-M, Kuhn, B, Rudolph, M.G. | | 登録日 | 2009-01-21 | | 公開日 | 2009-04-14 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.26 Å) | | 主引用文献 | Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist
Bioorg.Med.Chem.Lett., 19, 2009
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3FUR
 | | Crystal Structure of PPARg in complex with INT131 | | 分子名称: | 2,4-dichloro-N-[3,5-dichloro-4-(quinolin-3-yloxy)phenyl]benzenesulfonamide, CHLORIDE ION, Nuclear receptor coactivator 1, ... | | 著者 | Wang, Z, Liu, J, Walker, N. | | 登録日 | 2009-01-14 | | 公開日 | 2009-06-09 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | INT131: a selective modulator of PPAR gamma.
J.Mol.Biol., 386, 2009
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3FUG
 | | Crystal Structure of the Retinoid X Receptor Ligand Binding Domain Bound to the Synthetic Agonist 3-[4-Hydroxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-phenyl]acrylic Acid | | 分子名称: | (2E)-3-[4-hydroxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]prop-2-enoic acid, Nuclear receptor coactivator 2, Retinoic acid receptor RXR-alpha | | 著者 | Bourguet, W. | | 登録日 | 2009-01-14 | | 公開日 | 2009-05-12 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Modulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers.
J.Med.Chem., 52, 2009
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