1ERE
 
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6FZY
 | | PPAR mutant | | Descriptor: | Peroxisome proliferator-activated receptor gamma | | Authors: | Rochel, N. | | Deposit date: | 2018-03-15 | | Release date: | 2019-02-13 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Recurrent activating mutations of PPAR gamma associated with luminal bladder tumors.
Nat Commun, 10, 2019
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3E00
 | | Intact PPAR gamma - RXR alpha Nuclear Receptor Complex on DNA bound with GW9662, 9-cis Retinoic Acid and NCOA2 Peptide | | Descriptor: | (9cis)-retinoic acid, 2-chloro-5-nitro-N-phenylbenzamide, DNA (5'-D(*DCP*DAP*DAP*DAP*DCP*DTP*DAP*DGP*DGP*DTP*DCP*DAP*DAP*DAP*DGP*DGP*DTP*DCP*DAP*DG)-3'), ... | | Authors: | Chandra, V, Huang, P, Hamuro, Y, Raghuram, S, Wang, Y, Burris, T.P, Rastinejad, F. | | Deposit date: | 2008-07-30 | | Release date: | 2008-10-28 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA.
Nature, 456, 2008
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7WNH
 | | Crystal structure of Nurr1 binding to NBRE | | Descriptor: | DNA (5'-D(*CP*CP*GP*AP*AP*AP*AP*GP*GP*TP*CP*AP*TP*GP*CP*G)-3'), DNA (5'-D(*CP*GP*CP*AP*TP*GP*AP*CP*CP*TP*TP*TP*TP*CP*GP*G)-3'), Nuclear receptor subfamily 4 group A member 2, ... | | Authors: | Zhao, M, Xu, T, Wang, N, Guo, Y, Liu, J. | | Deposit date: | 2022-01-18 | | Release date: | 2023-01-25 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Integrative analysis reveals structural basis for transcription activation of Nurr1 and Nurr1-RXR alpha heterodimer.
Proc.Natl.Acad.Sci.USA, 119, 2022
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3DZY
 | | Intact PPAR gamma - RXR alpha Nuclear Receptor Complex on DNA bound with Rosiglitazone, 9-cis Retinoic Acid and NCOA2 Peptide | | Descriptor: | (9cis)-retinoic acid, 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), ... | | Authors: | Chandra, V, Huang, P, Hamuro, Y, Raghuram, S, Wang, Y, Burris, T.P, Rastinejad, F. | | Deposit date: | 2008-07-30 | | Release date: | 2008-10-28 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA.
Nature, 456, 2008
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3RVF
 | | FXR with SRC1 and GSK2034 | | Descriptor: | 5-(4-{[3-(2,6-dichlorophenyl)-5-(propan-2-yl)-1,2-oxazol-4-yl]methoxy}phenyl)-1H-indole-2-carboxylic acid, Bile acid receptor, Nuclear receptor coactivator 1, ... | | Authors: | Williams, S.P, Madauss, K.P. | | Deposit date: | 2011-05-06 | | Release date: | 2011-09-21 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene.
Bioorg.Med.Chem.Lett., 21, 2011
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1NUO
 | | Two RTH Mutants with Impaired Hormone Binding | | Descriptor: | Thyroid hormone receptor beta-1, [4-(4-HYDROXY-3-IODO-PHENOXY)-3,5-DIIODO-PHENYL]-ACETIC ACID | | Authors: | Huber, B.R, Sandler, B, West, B.L, Cunha-Lima, S.T, Nguyen, H.T, Apriletti, J.W, Baxter, J.D, Fletterick, R.J. | | Deposit date: | 2003-01-31 | | Release date: | 2003-04-15 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Two resistance to thyroid hormone mutants with impaired hormone binding
Mol.Endocrinol., 17, 2003
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6DGO
 | | Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Troglitazone | | Descriptor: | (5S)-5-[(4-{[(2R)-6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-2-yl]methoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione, Peroxisome proliferator-activated receptor gamma | | Authors: | Shang, J, Kojetin, D.J. | | Deposit date: | 2018-05-17 | | Release date: | 2019-05-22 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Quantitative structural assessment of graded receptor agonism.
Proc.Natl.Acad.Sci.USA, 116, 2019
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1Y0X
 | | Thyroxine-Thyroid Hormone Receptor Interactions | | Descriptor: | 3,5,3',5'-TETRAIODO-L-THYRONINE, CACODYLATE ION, Thyroid hormone receptor beta-1 | | Authors: | Sandler, B, Webb, P, Apriletti, J.W, Huber, B.R, Togashi, M, Cunha Lima, S.T, Juric, S, Nilsson, S, Wagner, R, Fletterick, R.J, Baxter, J.D. | | Deposit date: | 2004-11-16 | | Release date: | 2004-12-07 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Thyroxine-thyroid hormone receptor interactions.
J.Biol.Chem., 279, 2004
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5VQK
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6DGP
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4NQA
 | | Crystal structure of liganded hRXR-alpha/hLXR-beta heterodimer on DNA | | Descriptor: | (9cis)-retinoic acid, 5'-D(*TP*AP*AP*GP*GP*TP*CP*AP*CP*TP*TP*CP*AP*GP*GP*TP*CP*A)-3', 5'-D(*TP*AP*TP*GP*AP*CP*CP*TP*GP*AP*AP*GP*TP*GP*AP*CP*CP*T)-3', ... | | Authors: | Lou, X.H, Toresson, G, Benod, C, Suh, J.H, Phillips, K.J, Webb, P, Gustafsson, J.A. | | Deposit date: | 2013-11-24 | | Release date: | 2014-02-26 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.102 Å) | | Cite: | Structure of the retinoid X receptor alpha-liver X receptor beta (RXR alpha-LXR beta ) heterodimer on DNA.
Nat.Struct.Mol.Biol., 21, 2014
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4S0T
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2XYW
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6CHT
 | | HNF4alpha in complex with the corepressor EBP1 fragment | | Descriptor: | Hepatocyte nuclear factor 4-alpha, LAURIC ACID, Proliferation-associated protein 2G4 | | Authors: | Chi, Y.I, Singh, P, Lee, I.K. | | Deposit date: | 2018-02-22 | | Release date: | 2019-02-27 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.174 Å) | | Cite: | ErbB3-binding protein 1 (EBP1) represses HNF4 alpha-mediated transcription and insulin secretion in pancreatic beta-cells.
J.Biol.Chem., 294, 2019
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6B31
 | | Structure of RORgt in complex with a novel inverse agonist 2 | | Descriptor: | (3S)-N~1~-(3-chloro-4-cyanophenyl)-N~5~-(1,3-diethyl-2,4-dioxo-1,2,3,4-tetrahydroquinazolin-6-yl)-3-methylpentanediamide, Nuclear receptor ROR-gamma | | Authors: | Skene, R.J, Hoffman, I. | | Deposit date: | 2017-09-20 | | Release date: | 2018-08-01 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (3.18 Å) | | Cite: | Identification of novel quinazolinedione derivatives as ROR gamma t inverse agonist.
Bioorg. Med. Chem., 26, 2018
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3WWR
 | | Crystal structure of the human vitamin D receptor ligand binding domain complexed with 1-((((1S,2R,6R,Z)-2,6-dihydroxy-4-((E)-2-((1R,3aS,7aR)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methylhexahydro-1H-inden-4(2H)-ylidene)ethylidene)-3-methylenecyclohexyl)oxy)methyl)cyclopropanecarbonitrile | | Descriptor: | 1-({[(1R,2S,3R,5Z,7E,14beta,17alpha)-1,3,25-trihydroxy-9,10-secocholesta-5,7,10-trien-2-yl]oxy}methyl)cyclopropanecarbonitrile, Vitamin D3 receptor | | Authors: | Kakuda, S, Takimoto-Kamimura, M. | | Deposit date: | 2014-06-27 | | Release date: | 2014-12-31 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (3.18 Å) | | Cite: | Synthesis and biological activities of vitamin D3 derivatives with cyanoalkyl side chain at C-2 position.
J.Steroid Biochem.Mol.Biol., 148, 2015
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6BR2
 | | Structure of RORgt in complex with a novel isoquinoline inverse agonist. | | Descriptor: | (1R)-N-(4-tert-butyl-3-fluorophenyl)-6-methoxy-2-[(3-oxo-2,3-dihydro-1,2-oxazol-5-yl)acetyl]-1,2,3,4-tetrahydroisoquinoline-1-carboxamide, (4S)-2-METHYL-2,4-PENTANEDIOL, Nuclear receptor ROR-gamma | | Authors: | Skene, R.J, Hoffman, I. | | Deposit date: | 2017-11-29 | | Release date: | 2018-03-21 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (3.18 Å) | | Cite: | Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor gamma t Inverse Agonist.
J. Med. Chem., 61, 2018
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5UHI
 | | Structure of RORgt bound to | | Descriptor: | (R)-(4-chloro-2-methoxy-3-{[4-(1H-pyrazol-1-yl)phenyl]methyl}quinolin-6-yl)(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methanol, Nuclear receptor ROR-gamma | | Authors: | Spurlino, J, Abad, M. | | Deposit date: | 2017-01-11 | | Release date: | 2017-04-05 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (3.198 Å) | | Cite: | Identification and structure activity relationships of quinoline tertiary alcohol modulators of ROR gamma t.
Bioorg. Med. Chem. Lett., 27, 2017
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2YLY
 | | Sulfonamides as selective Estrogen Receptor beta Agonists. | | Descriptor: | ESTROGEN RECEPTOR BETA, N-cyclopropyl-4-oxidanyl-N-[(2R)-2-oxidanyl-2-phenyl-propyl]benzenesulfonamide, SULFATE ION | | Authors: | Roberts, L.R, Armour, D, Barker, C, Bazin, R, Bess, K, Brown, A, Favor, D, Ellis, D, MacKenny, M, Pullen, N, Stennett, A, Strand, L, Styles, M, Phillips, C. | | Deposit date: | 2011-06-06 | | Release date: | 2012-06-13 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Sulfonamides as Selective Oestrogen Receptor Beta Agonists.
Bioorg.Med.Chem.Lett., 21, 2011
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3GD2
 | | isoxazole ligand bound to farnesoid X receptor (FXR) | | Descriptor: | 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 | | Authors: | Madauss, K.P, Williams, S.P, Deaton, D.N, Wisely, G.B, Mcfadyen, R.B. | | Deposit date: | 2009-02-23 | | Release date: | 2009-07-07 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.
Bioorg.Med.Chem.Lett., 19, 2009
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3DZU
 | | Intact PPAR gamma - RXR alpha Nuclear Receptor Complex on DNA bound with BVT.13, 9-cis Retinoic Acid and NCOA2 Peptide | | Descriptor: | (9cis)-retinoic acid, 2-[(2,4-DICHLOROBENZOYL)AMINO]-5-(PYRIMIDIN-2-YLOXY)BENZOIC ACID, DNA (5'-D(*DCP*DAP*DAP*DAP*DCP*DTP*DAP*DGP*DGP*DTP*DCP*DAP*DAP*DAP*DGP*DGP*DTP*DCP*DAP*DG)-3'), ... | | Authors: | Chandra, V, Huang, P, Hamuro, Y, Raghuram, S, Wang, Y, Burris, T.P, Rastinejad, F. | | Deposit date: | 2008-07-30 | | Release date: | 2008-10-28 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA.
Nature, 456, 2008
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6NWU
 | | RORgamma Ligand Binding Domain | | Descriptor: | 6-[(3,5-dichloropyridin-4-yl)methoxy]-1-{[3-(trifluoromethyl)phenyl]sulfonyl}-2,3-dihydro-1H-indole, Nuclear receptor ROR-gamma | | Authors: | Strutzenberg, T.S, Park, H, Griffin, P.R. | | Deposit date: | 2019-02-07 | | Release date: | 2019-07-10 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | HDX-MS reveals structural determinants for ROR gamma hyperactivation by synthetic agonists.
Elife, 8, 2019
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7WOX
 | | PPARgamma antagonist (MMT-160)- PPARgamma LBD complex | | Descriptor: | N-[[5-(3-phenylprop-2-ynoylamino)-2-propoxy-phenyl]methyl]-4-pyrimidin-2-yl-benzamide, Peroxisome proliferator-activated receptor gamma | | Authors: | Yoshizawa, M, Aoyama, T, Itoh, T, Miyachi, H. | | Deposit date: | 2022-01-22 | | Release date: | 2022-04-13 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Arylalkynyl amide-type peroxisome proliferator-activated receptor gamma (PPAR gamma )-selective antagonists covalently bind to the PPAR gamma ligand binding domain with a unique binding mode.
Bioorg.Med.Chem.Lett., 64, 2022
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7E2O
 | | X-ray Crystal structure of PPARgamma R288H mutant. | | Descriptor: | Peroxisome proliferator-activated receptor gamma | | Authors: | Egawa, D, Itoh, T. | | Deposit date: | 2021-02-06 | | Release date: | 2022-01-19 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Structural Insights into the Loss-of-Function R288H Mutant of Human PPAR gamma.
Biol.Pharm.Bull., 44, 2021
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