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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
3G0W
| |
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
|
|
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
|
|
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
|
|
3FS1
| |
3FLI
| Discovery of XL335, a Highly Potent, Selective and Orally-Active Agonist of the Farnesoid X Receptor (FXR) | 分子名称: | 1-methylethyl 3-[(3,4-difluorophenyl)carbonyl]-1,1-dimethyl-1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate, Bile acid receptor | 著者 | Foster, P.G, Stout, T.J. | 登録日 | 2008-12-18 | 公開日 | 2009-12-22 | 最終更新日 | 2024-02-21 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR). J.Med.Chem., 52, 2009
|
|
3FEJ
| Design and biological evaluation of novel, balanced dual PPARa/g agonists | 分子名称: | (2S)-3-(4-{[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methoxy}-2-methylphenyl)-2-ethoxypropanoic acid, Peroxisome proliferator-activated receptor gamma, peptide motif 3 of Nuclear receptor coactivator 1 | 著者 | Benz, J, Grether, U, Gsell, B, Binggeli, A, Hilpert, H, Kuhn, B, Maerki, H.P, Mohr, P, Ruf, A, Stihle, M. | 登録日 | 2008-11-30 | 公開日 | 2009-10-20 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | 主引用文献 | Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists Chemmedchem, 4, 2009
|
|
3FEI
| Design and biological evaluation of novel, balanced dual PPARa/g agonists | 分子名称: | (2S)-3-(4-{[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methoxy}-2-methylphenyl)-2-ethoxypropanoic acid, Peptide motif 5 of Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor alpha | 著者 | Benz, J, Grether, U, Gsell, B, Binggeli, A, Hilpert, H, Maerki, H.P, Mohr, P, Ruf, A, Stihle, M, Schlatter, D. | 登録日 | 2008-11-30 | 公開日 | 2009-10-20 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists Chemmedchem, 4, 2009
|
|
3FC6
| hRXRalpha & mLXRalpha with an indole Pharmacophore, SB786875 | 分子名称: | Nr1h3 protein, RETINOIC ACID, Retinoic acid receptor RXR-alpha, ... | 著者 | Washburn, D.G, Hoang, T.H, Campobasso, N, Smallwood, A, Parks, D.J, Webb, C.L, Frank, K, Nord, M, Duraiswami, C, Evans, C, Jaye, M, Thompson, S.K. | 登録日 | 2008-11-21 | 公開日 | 2009-02-10 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.063 Å) | 主引用文献 | Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. Bioorg.Med.Chem.Lett., 19, 2009
|
|
3FAL
| humanRXR alpha & mouse LXR alpha complexed with Retenoic acid and GSK2186 | 分子名称: | 2-{4-[butyl(3-chloro-4,5-dimethoxybenzyl)amino]phenyl}-1,1,1,3,3,3-hexafluoropropan-2-ol, Oxysterols receptor LXR-alpha, RETINOIC ACID, ... | 著者 | Chao, E.Y, Caravella, J.A, Watson, M.A, Campobasso, N, Ghisletti, S, Billin, A.N, Galardi, C, Willson, T.M, Zuercher, W.J, Collins, J.L. | 登録日 | 2008-11-17 | 公開日 | 2009-04-14 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.36 Å) | 主引用文献 | Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. J.Med.Chem., 51, 2008
|
|
3F7D
| SF-1 LBD bound by phosphatidylcholine | 分子名称: | (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate, Peroxisome proliferator-activated receptor gamma coactivator 1-alpha, nuclear receptor SF-1 | 著者 | Sablin, E.P, Fletterick, R.J. | 登録日 | 2008-11-07 | 公開日 | 2008-12-09 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | Structure of SF-1 bound by different phospholipids: evidence for regulatory ligands. Mol.Endocrinol., 23, 2009
|
|
3F5C
| Structure of Dax-1:LRH-1 complex | 分子名称: | Nuclear receptor subfamily 0 group B member 1, Nuclear receptor subfamily 5 group A member 2 | 著者 | Fletterick, R.J, Sablin, E.P. | 登録日 | 2008-11-03 | 公開日 | 2008-12-23 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (3 Å) | 主引用文献 | The structure of corepressor Dax-1 bound to its target nuclear receptor LRH-1. Proc.Natl.Acad.Sci.USA, 105, 2008
|
|