1K74
 
 | | The 2.3 Angstrom resolution crystal structure of the heterodimer of the human PPARgamma and RXRalpha ligand binding domains respectively bound with GW409544 and 9-cis retinoic acid and co-activator peptides. | | Descriptor: | (9cis)-retinoic acid, 2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, Peroxisome proliferator activated receptor gamma, ... | | Authors: | Xu, H.E, Lambert, M.H, Montana, V.G, Moore, L.B, Collins, J.L, Oplinger, J.A, Kliewer, S.A, Gampe Jr, R.T, McKee, D.D, Moore, J.T, Willson, T.M. | | Deposit date: | 2001-10-18 | | Release date: | 2001-12-05 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proc.Natl.Acad.Sci.USA, 98, 2001
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1K7L
 | | The 2.5 Angstrom resolution crystal structure of the human PPARalpha ligand binding domain bound with GW409544 and a co-activator peptide. | | Descriptor: | 2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, Peroxisome proliferator activated receptor alpha, YTTRIUM (III) ION, ... | | Authors: | Xu, H.E, Lambert, M.H, Montana, V.G, Moore, L.B, Collins, J.L, Oplinger, J.A, Kliewer, S.A, Gampe Jr, R.T, McKee, D.D, Moore, J.T, Willson, T.M. | | Deposit date: | 2001-10-19 | | Release date: | 2001-12-05 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proc.Natl.Acad.Sci.USA, 98, 2001
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1KKQ
 | | Crystal structure of the human PPAR-alpha ligand-binding domain in complex with an antagonist GW6471 and a SMRT corepressor motif | | Descriptor: | N-((2S)-2-({(1Z)-1-METHYL-3-OXO-3-[4-(TRIFLUOROMETHYL) PHENYL]PROP-1-ENYL}AMINO)-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]PHENYL}PROPYL)PROPANAMIDE, NUCLEAR RECEPTOR CO-REPRESSOR 2, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR | | Authors: | Xu, H.E, Stanley, T.B, Montana, V.G, Lambert, M.H, Shearer, B.G, Cobb, J.E, McKee, D.D, Galardi, C.M, Nolte, R.T, Parks, D.J. | | Deposit date: | 2001-12-10 | | Release date: | 2002-02-20 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha.
Nature, 415, 2002
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1KNU
 | | LIGAND BINDING DOMAIN OF THE HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA IN COMPLEX WITH A SYNTHETIC AGONIST | | Descriptor: | (S)-3-(4-(2-CARBAZOL-9-YL-ETHOXY)-PHENYL)-2-ETHOXY-PROPIONIC ACID, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA | | Authors: | Svensson, L.A, Mortensen, S.B, Fleckner, J, Woeldike, H.F. | | Deposit date: | 2001-12-19 | | Release date: | 2002-12-19 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity
J.MED.CHEM., 45, 2002
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1GS4
 | | Structural basis for the glucocorticoid response in a mutant human androgen receptor (ARccr) derived from an androgen-independent prostate cancer | | Descriptor: | 9ALPHA-FLUOROCORTISOL, ANDROGEN RECEPTOR, PHOSPHATE ION | | Authors: | Matias, P.M, Carrondo, M.A, Coelho, R, Thomaz, M, Zhao, X.-Y, Wegg, A, Crusius, K, Egner, U, Donner, P. | | Deposit date: | 2001-12-27 | | Release date: | 2003-01-16 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structural Basis for the Glucocorticoid Response in a Mutant Human Androgen Receptor (Ar(Ccr)) Derived from an Androgen-Independent Prostate Cancer
J.Med.Chem., 45, 2002
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1KV6
 | | X-ray structure of the orphan nuclear receptor ERR3 ligand-binding domain in the constitutively active conformation | | Descriptor: | ESTROGEN-RELATED RECEPTOR GAMMA, steroid receptor coactivator 1 | | Authors: | Greschik, H, Wurtz, J.-M, Sanglier, S, Bourguet, W, van Dorsselaer, A, Moras, D, Renaud, J.-P, Structural Proteomics in Europe (SPINE) | | Deposit date: | 2002-01-25 | | Release date: | 2003-01-25 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Structural and Functional Evidence for Ligand-Independent Transcriptional Activation by the Estrogen-Related Receptor 3
Mol.Cell, 9, 2002
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1L2J
 | | Human Estrogen Receptor beta Ligand-binding Domain in Complex with (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol | | Descriptor: | (R,R)-5,11-CIS-DIETHYL-5,6,11,12-TETRAHYDROCHRYSENE-2,8-DIOL, ESTROGEN RECEPTOR BETA | | Authors: | Shiau, A.K, Barstad, D, Radek, J.T, Meyers, M.J, Nettles, K.W, Katzenellenbogen, B.S, Katzenellenbogen, J.A, Agard, D.A, Greene, G.L. | | Deposit date: | 2002-02-21 | | Release date: | 2002-05-01 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.95 Å) | | Cite: | Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.
Nat.Struct.Biol., 9, 2002
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1L2I
 | | Human Estrogen Receptor alpha Ligand-binding Domain in Complex with (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol and a Glucocorticoid Receptor Interacting Protein 1 NR box II Peptide | | Descriptor: | (R,R)-5,11-CIS-DIETHYL-5,6,11,12-TETRAHYDROCHRYSENE-2,8-DIOL, CHLORIDE ION, ESTROGEN RECEPTOR, ... | | Authors: | Shiau, A.K, Barstad, D, Radek, J.T, Meyers, M.J, Nettles, K.W, Katzenellenbogen, B.S, Katzenellenbogen, J.A, Agard, D.A, Greene, G.L. | | Deposit date: | 2002-02-21 | | Release date: | 2002-05-01 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.
Nat.Struct.Biol., 9, 2002
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1GWQ
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1GWR
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1LV2
 | | Hepatocyte Nuclear Factor 4 is a Transcription Factor that Constitutively Binds Fatty Acids | | Descriptor: | Hepatocyte nuclear factor 4-gamma, PALMITIC ACID | | Authors: | Wisely, B, Miller, A.B, Davis, R.G, Spitzer, T, Shearer, B, Moore, J.T, Johnson, R, Sefler, A, Willson, T.M, Williams, S.P. | | Deposit date: | 2002-05-24 | | Release date: | 2002-12-18 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Hepatocyte Nuclear Factor 4 Is a Transcription Factor
that Constitutively Binds Fatty Acids.
Structure, 10, 2002
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1M13
 | | Crystal Structure of the Human Pregane X Receptor Ligand Binding Domain in Complex with Hyperforin, a Constituent of St. John's Wort | | Descriptor: | 4-HYDROXY-5-ISOBUTYRYL-6-METHYL-1,3,7-TRIS-(3-METHYL-BUT-2-ENYL)-6-(4-METHYL-PENT-3-ENYL)-BICYCLO[3.3.1]NON-3-ENE-2,9-DIONE, Orphan Nuclear Receptor PXR | | Authors: | Watkins, R.E, Maglich, J.M, Moore, L.B, Wisely, G.B, Noble, S.M, Davis-Searles, P.R, Lambert, M.H, Kliewer, S.A, Redinbo, M.R. | | Deposit date: | 2002-06-17 | | Release date: | 2003-03-04 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | 2.1 A Crystal Structure of Human PXR in Complex with the St. John's Wort Compound Hyperforin
Biochemistry, 42, 2003
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1M2Z
 | | Crystal structure of a dimer complex of the human glucocorticoid receptor ligand-binding domain bound to dexamethasone and a TIF2 coactivator motif | | Descriptor: | DEXAMETHASONE, glucocorticoid receptor, nuclear receptor coactivator 2, ... | | Authors: | Bledsoe, R.B, Montana, V.G, Stanley, T.B, Delves, C.J, Apolito, C.J, Mckee, D.D, Consler, T.G, Parks, D.J, Stewart, E.L, Willson, T.M, Lambert, M.H, Moore, J.T, Pearce, K.H, Xu, H.E. | | Deposit date: | 2002-06-26 | | Release date: | 2003-07-15 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Reveals a Novel Mode of Receptor Dimerization and Coactivator Recognition
Cell(Cambridge,Mass.), 110, 2002
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1M7W
 | | HNF4a ligand binding domain with bound fatty acid | | Descriptor: | Hepatocyte nuclear factor 4-alpha, LAURIC ACID | | Authors: | Dhe-Paganon, S, Duda, K, Iwamoto, M, Chi, Y.I, Shoelson, S.E. | | Deposit date: | 2002-07-22 | | Release date: | 2003-07-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal structure of the HNF4 alpha ligand binding domain in complex with endogenous fatty acid ligand
J.Biol.Chem., 277, 2002
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1MVC
 | | Crystal structure of the human RXR alpha ligand binding domain bound to the synthetic agonist compound BMS 649 and a coactivator peptide | | Descriptor: | 4-[2-(5,5,8,8-TETRAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-[1,3]DIOXOLAN-2-YL]-BENZOIC ACID, Nuclear receptor coactivator 2, RXR retinoid X receptor | | Authors: | Egea, P.F, Mitschler, A, Moras, D. | | Deposit date: | 2002-09-24 | | Release date: | 2002-10-16 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Molecular Recognition of Agonist Ligands by RXRs
MOL.ENDOCRINOL., 16, 2002
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1MV9
 | | Crystal Structure of the human RXR alpha ligand binding domain bound to the eicosanoid DHA (Docosa Hexaenoic Acid) and a coactivator peptide | | Descriptor: | DOCOSA-4,7,10,13,16,19-HEXAENOIC ACID, Nuclear receptor coactivator 2, RXR retinoid X receptor | | Authors: | Egea, P.F, Mitschler, A, Moras, D. | | Deposit date: | 2002-09-24 | | Release date: | 2002-10-16 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Molecular Recognition of Agonist Ligands by RXRs
MOL.ENDOCRINOL., 16, 2002
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1MZN
 | | CRYSTAL STRUCTURE at 1.9 ANGSTROEMS RESOLUTION OF THE HOMODIMER OF HUMAN RXR ALPHA LIGAND BINDING DOMAIN BOUND TO THE SYNTHETIC AGONIST COMPOUND BMS 649 AND A COACTIVATOR PEPTIDE | | Descriptor: | 4-[2-(5,5,8,8-TETRAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-[1,3]DIOXOLAN-2-YL]-BENZOIC ACID, Nuclear receptor coactivator 2, RXR retinoid X receptor | | Authors: | Egea, P.F, Mitschler, A, Moras, D. | | Deposit date: | 2002-10-09 | | Release date: | 2002-10-23 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Molecular Recognition of Agonist Ligands by RXRs
MOL.ENDOCRINOL., 16, 2002
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1N46
 | | CRYSTAL STRUCTURE OF HUMAN TR BETA LIGAND-BINDING DOMAIN COMPLEXED WITH A POTENT SUBTYPE-SELECTIVE THYROMIMETIC | | Descriptor: | Thyroid hormone receptor Beta-1, [4-(4-HYDROXY-3-ISOPROPYL-PHENOXY)-3,5-DIMETHYL-PHENYL]-6-AZAURACIL | | Authors: | Dow, R.L, Schneider, S.R, Paight, E.S, Hank, R.F, Chiang, P, Cornelius, P, Lee, E, Newsome, W.P, Swick, A.G, Spitzer, J, Hargrove, D.M, Patterson, T.A, Pandit, J, Chrunyk, B.A, LeMotte, P.K, Danley, D.E, Rosner, M.H, Ammirati, M.J, Simons, S.P, Schulte, G.K, Tate, B.F, DaSilva-Jardine, P. | | Deposit date: | 2002-10-30 | | Release date: | 2003-04-22 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Discovery of a Novel Series of 6-Azauracil-Based Thyroid Hormone Receptor Ligands:
Potent, TRbeta Subtype-Selective Thyromimetics
Bioorg.Med.Chem.Lett., 13, 2003
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1N4H
 | | Characterization of ligands for the orphan nuclear receptor RORbeta | | Descriptor: | Nuclear Receptor ROR-beta, RETINOIC ACID, Steroid Receptor Coactivator-1 | | Authors: | Stehlin-Gaon, C, Willmann, D, Sanglier, S, Van Dorsselaer, A, Renaud, J.-P, Moras, D, Schuele, R. | | Deposit date: | 2002-10-31 | | Release date: | 2003-09-23 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | All-trans retinoic acid is a ligand for the orphan nuclear receptor RORbeta
Nat.Struct.Biol., 10, 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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1NAV
 | | Thyroid Receptor Alpha in complex with an agonist selective for Thyroid Receptor Beta1 | | Descriptor: | SULFATE ION, hormone receptor alpha 1, THRA1, ... | | 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 (2.5 Å) | | Cite: | Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.
J.Med.Chem., 46, 2003
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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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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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1NHZ
 | | Crystal Structure of the Antagonist Form of Glucocorticoid Receptor | | Descriptor: | 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, GLUCOCORTICOID RECEPTOR, HEXANE-1,6-DIOL | | Authors: | Kauppi, B, Jakob, C, Farnegardh, M, Yang, J, Ahola, H, Alarcon, M, Calles, K, Engstrom, O, Harlan, J, Muchmore, S, Ramqvist, A.-K, Thorell, S, Ohman, L, Greer, J, Gustafsson, J.-A, Carlstedt-Duke, J, Carlquist, M. | | Deposit date: | 2002-12-20 | | Release date: | 2003-05-06 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | The Three-dimensional Structures of Antagonistic and Agonistic Forms of the Glucocorticoid Receptor Ligand-binding Domain:
RU-486 INDUCES A TRANSCONFORMATION THAT LEADS TO ACTIVE ANTAGONISM.
J.Biol.Chem., 278, 2003
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1NQ0
 | | 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 (2.4 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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