7WGO
 
 | | X-ray structure of human PPAR gamma ligand binding domain-bezafibrate co-rystals obtained by co-crystallization | | Descriptor: | 15-meric peptide from Nuclear receptor coactivator 1, 2-[P-[2-P-CHLOROBENZAMIDO)ETHYL]PHENOXY]-2-METHYLPROPIONIC ACID, Isoform 1 of Peroxisome proliferator-activated receptor gamma | | Authors: | Kamata, S, Honda, A, Akahane, M, Machida, Y, Uchii, K, Shiiyama, Y, Masuda, R, Oyama, T, Ishii, I. | | Deposit date: | 2021-12-28 | | Release date: | 2022-05-25 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.36 Å) | | Cite: | Functional and Structural Insights into Human PPAR alpha / delta / gamma Subtype Selectivity of Bezafibrate, Fenofibric Acid, and Pemafibrate.
Int J Mol Sci, 23, 2022
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7WGL
 | | X-ray structure of human PPAR delta ligand binding domain-bezafibrate co-crystals obtained by co-crystallization | | Descriptor: | 2-[P-[2-P-CHLOROBENZAMIDO)ETHYL]PHENOXY]-2-METHYLPROPIONIC ACID, Peroxisome proliferator-activated receptor delta, octyl beta-D-glucopyranoside | | Authors: | Kamata, S, Honda, A, Machida, Y, Uchii, K, Shiiyama, Y, Masuda, R, Oyama, T, Ishii, I. | | Deposit date: | 2021-12-28 | | Release date: | 2022-05-25 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.091 Å) | | Cite: | Functional and Structural Insights into Human PPAR alpha / delta / gamma Subtype Selectivity of Bezafibrate, Fenofibric Acid, and Pemafibrate.
Int J Mol Sci, 23, 2022
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7UJC
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7UJ8
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7UJF
 | | Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Methylated Lasofoxifene Derivative with Selective Estrogen Receptor Degrader Properties | | Descriptor: | (5R,6S)-5-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor | | Authors: | Hosfield, D.J, Greene, G.L, Fanning, S.W. | | Deposit date: | 2022-03-30 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | 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
 | | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Possesses Selective Estrogen Receptor Degrader Activities | | Descriptor: | (5R,6S)-5-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor | | Authors: | Hosfield, D.J, Greene, G.L, Fanning, S.W. | | Deposit date: | 2022-03-31 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | 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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7UJM
 | | Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Methylated Lasofoxifene Derivative That Increases Receptor Resonance Time in the Nucleus of Breast Cancer Cells | | Descriptor: | (5R,6S)-5-(4-{2-[(2R)-2-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor | | Authors: | Hosfield, D.J, Greene, G.L, Fanning, S.W. | | Deposit date: | 2022-03-31 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | 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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7UJO
 | | Estrogen Receptor Alpha Ligand Binding Domain in Complex with RU39411 | | Descriptor: | (9beta,11beta,17beta)-11-{4-[2-(dimethylamino)ethoxy]phenyl}estra-1,3,5(10)-triene-3,17-diol, Estrogen receptor, MAGNESIUM ION | | Authors: | Hosfield, D.J, Greene, G.L, Fanning, S.W. | | Deposit date: | 2022-03-31 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.449 Å) | | Cite: | 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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7UJY
 | | Estrogen receptor alpha ligand binding domain Y537S mutant in complex with a methylated lasofoxifene derivative that enhances estrogen receptor alpha nuclear resonance time | | Descriptor: | (5R,6S)-5-(4-{2-[(2R)-2-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor | | Authors: | Hosfield, D.J, Greene, G.L, Fanning, S.W. | | Deposit date: | 2022-03-31 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | 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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6TSG
 | | Crystal structure of Peroxisome proliferator-activated receptor gamma (PPARG) in complex with TETRAC | | Descriptor: | 3,3',5,5'-TETRAIODOTHYROACETIC ACID, Peroxisome proliferator-activated receptor gamma | | Authors: | Chaikuad, A, Gellrich, L, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Merk, D, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2019-12-20 | | Release date: | 2020-07-22 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.98 Å) | | Cite: | l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR gamma.
J.Med.Chem., 63, 2020
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6T1V
 | | Structure of PPARg H494Y mutant in complex with GW1929 | | Descriptor: | (2~{S})-3-[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]-2-[[2-(phenylcarbonyl)phenyl]amino]propanoic acid, Peroxisome proliferator-activated receptor gamma, Peroxisome proliferator-activated receptor gamma coactivator 1-alpha | | Authors: | Rochel, N. | | Deposit date: | 2019-10-06 | | Release date: | 2021-04-14 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.21 Å) | | Cite: | Structure of a PPARg mutant complex
To Be Published
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3IMY
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1NQ1
 | | TR Receptor Mutations Conferring Hormone Resistance and Reduced Corepressor Release Exhibit Decreased Stability in the Nterminal LBD | | Descriptor: | ARSENIC, Thyroid hormone receptor beta-1, [4-(4-HYDROXY-3-IODO-PHENOXY)-3,5-DIIODO-PHENYL]-ACETIC ACID | | Authors: | Huber, B.R, Desclozeaux, M, West, B.L, Cunha-Lima, S.T, Nguyen, H.T, Baxter, J.D, Ingraham, H.A, Fletterick, R.J. | | Deposit date: | 2003-01-20 | | Release date: | 2003-04-15 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Thyroid hormone receptor-beta mutations conferring hormone resistance and reduced corepressor release exhibit decreased stability in the N-terminal ligand-binding domain
Mol.Endocrinol., 17, 2003
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1OSV
 | | STRUCTURAL BASIS FOR BILE ACID BINDING AND ACTIVATION OF THE NUCLEAR RECEPTOR FXR | | Descriptor: | 6-ETHYL-CHENODEOXYCHOLIC ACID, Bile acid receptor, Nuclear receptor coactivator 2 | | Authors: | Mi, L.Z, Devarakonda, S, Harp, J.M, Han, Q, Pellicciari, R, Willson, T.M, Khorasanizadeh, S, Rastinejad, F. | | Deposit date: | 2003-03-20 | | Release date: | 2004-03-23 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structural Basis for Bile Acid Binding and Activation of the Nuclear Receptor FXR
Mol.Cell, 11, 2003
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3IXP
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3IA6
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7VQP
 | | Vitamin D receptor complexed with a lithocholic acid derivative | | Descriptor: | 3-((R)-4-((3R,5R,8R,9S,10S,13R,14S,17R)-3-(2-hydroxy-2-methylpropyl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)propanoic acid, Mediator of RNA polymerase II transcription subunit 1, Vitamin D3 receptor | | Authors: | Kato, K, Numoto, N, Kagechika, H, Tanatani, A, Ito, N. | | Deposit date: | 2021-10-20 | | Release date: | 2022-03-09 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | Lithocholic Acid Amides as Potent Vitamin D Receptor Agonists.
Biomolecules, 12, 2022
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1PK5
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7UJ7
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1Q4X
 | | Crystal Structure of Human Thyroid Hormone Receptor beta LBD in complex with specific agonist GC-24 | | Descriptor: | Thyroid hormone receptor beta-1, [4-(3-BENZYL-4-HYDROXYBENZYL)-3,5-DIMETHYLPHENOXY]ACETIC ACID | | Authors: | Borngraeber, S, Budny, M.J, Chiellini, G, Cunha-Lima, S.T, Togashi, M, Webb, P, Baxter, J.D, Scanlan, T.S, Fletterick, R.J. | | Deposit date: | 2003-08-04 | | Release date: | 2004-02-03 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Ligand selectivity by seeking hydrophobicity in thyroid hormone receptor.
Proc.Natl.Acad.Sci.USA, 100, 2003
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1PQ9
 | | HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317 COMPLEX | | Descriptor: | 1,1,1,3,3,3-HEXAFLUORO-2-{4-[(2,2,2-TRIFLUOROETHYL)AMINO]PHENYL}PROPAN-2-OL, Oxysterols receptor LXR-beta, benzenesulfonic acid | | Authors: | Farnegardh, M, Bonn, T, Sun, S, Ljunggren, J, Ahola, H, Wilhelmsson, A, Gustafsson, J.-A, Carlquist, M. | | Deposit date: | 2003-06-18 | | Release date: | 2003-09-09 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands.
J.Biol.Chem., 278, 2003
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1N83
 | | Crystal Structure of the complex between the Orphan Nuclear Hormone Receptor ROR(alpha)-LBD and Cholesterol | | Descriptor: | CHOLESTEROL, Nuclear receptor ROR-alpha | | Authors: | Kallen, J.A, Schlaeppi, J.M, Bitsch, F, Geisse, S, Geiser, M, Delhon, I, Fournier, B. | | Deposit date: | 2002-11-19 | | Release date: | 2002-12-11 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | X-ray Structure of hROR(alpha) LBD at 1.63A: Structural and Functional data that Cholesterol or a Cholesterol derivative is the natural ligand of ROR(alpha)
Structure, 10, 2002
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1NAX
 | | Thyroid receptor beta1 in complex with a beta-selective ligand | | Descriptor: | Thyroid hormone receptor beta-1, {3,5-DICHLORO-4-[4-HYDROXY-3-(PROPAN-2-YL)PHENOXY]PHENYL}ACETIC ACID | | Authors: | Ye, L, Li, Y.L, Mellstrom, K, Mellin, C, Bladh, L.G, Koehler, K, Garg, N, Garcia Collazo, A.M, Litten, C, Husman, B, Persson, K, Ljunggren, J, Grover, G, Sleph, P.G, George, R, Malm, J. | | Deposit date: | 2002-11-29 | | Release date: | 2003-06-17 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.
J.Med.Chem., 46, 2003
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6U25
 | | CRYSTAL STRUCTURE OF RAR-RELATED ORPHAN RECEPTOR C (NHIS- RORGT(244-487)-L6-SRC1(678-692)) IN COMPLEX WITH A TRICYCLIC INVERSE AGONIST | | Descriptor: | GLYCEROL, NUCLEAR RECEPTOR COACTIVATOR 1 CHIMERA, trans-4-[(3aR,9bR)-9b-[(4-fluorophenyl)sulfonyl]-7-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)-1,2,3a,4,5,9b-hexahydro-3H-benzo[e]indole-3-carbonyl]cyclohexane-1-carboxylic acid | | Authors: | Sack, J. | | Deposit date: | 2019-08-19 | | Release date: | 2019-11-06 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.61 Å) | | Cite: | Rationally Designed, Conformationally Constrained Inverse Agonists of ROR gamma t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
J.Med.Chem., 62, 2019
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1NDE
 | | Estrogen Receptor beta with Selective Triazine Modulator | | Descriptor: | 4-(2-{[4-{[3-(4-CHLOROPHENYL)PROPYL]SULFANYL}-6-(1-PIPERAZINYL)-1,3,5-TRIAZIN-2-YL]AMINO}ETHYL)PHENOL, Estrogen receptor beta | | Authors: | Henke, B.R, Consler, T.G, Go, N, Hale, R.L, Hohman, D.R, Jones, S.A, Lu, A.T, Moore, L.B, Moore, J.T, Orband-Miller, L.A, Robinett, R.G, Shearin, J, Spearing, P.K, Stewart, E.L, Turnbull, P.S, Weaver, S.L, Williams, S.P, Wisely, G.B, Lambert, M.H. | | Deposit date: | 2002-12-09 | | Release date: | 2002-12-18 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | A New Series of Estrogen Receptor Modulators That Display Selectivity for Estrogen Receptor beta
J.Med.Chem., 45, 2002
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