6KKB
| A novel agonist of THRb | Descriptor: | 2-[(1-methyl-4-oxidanyl-7-phenoxy-isoquinolin-3-yl)carbonylamino]ethanoic acid, SRC2-3, Thyroid hormone receptor beta | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2019-07-24 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Revealing a Mutant-Induced Receptor Allosteric Mechanism for the Thyroid Hormone Resistance. Iscience, 20, 2019
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2NLL
| RETINOID X RECEPTOR-THYROID HORMONE RECEPTOR DNA-BINDING DOMAIN HETERODIMER BOUND TO THYROID RESPONSE ELEMENT DNA | Descriptor: | DNA (5'-D(*CP*AP*GP*GP*TP*CP*AP*TP*TP*(5IU)P*CP*AP*GP*GP*TP*CP*AP*G)-3'), DNA (5'-D(*CP*TP*GP*AP*CP*CP*TP*GP*AP*AP*AP*TP*GP*AP*CP*CP*T P*G)-3'), PROTEIN (RETINOIC ACID RECEPTOR), ... | Authors: | Rastinejad, F, Perlmann, T, Evans, R.M, Sigler, P.B. | Deposit date: | 1996-11-20 | Release date: | 1997-03-12 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structural determinants of nuclear receptor assembly on DNA direct repeats. Nature, 375, 1995
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7WMH
| A novel chemical derivative(56) of THRB agonist | Descriptor: | 2-[[1-methoxy-4-oxidanyl-7-(4-phenylphenoxy)isoquinolin-3-yl]carbonylamino]ethanoic acid, Isoform Beta-2 of Thyroid hormone receptor beta, Nuclear receptor coactivator 2 | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2022-01-14 | Release date: | 2022-05-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (1.97 Å) | Cite: | Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor beta Agonist. J.Med.Chem., 65, 2022
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3D57
| TR Variant D355R | Descriptor: | SULFATE ION, Thyroid hormone receptor beta, [4-(4-HYDROXY-3-IODO-PHENOXY)-3,5-DIIODO-PHENYL]-ACETIC ACID | Authors: | Jouravel, N. | Deposit date: | 2008-05-15 | Release date: | 2008-10-14 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Molecular basis for dimer formation of TRbeta variant D355R. Proteins, 75, 2008
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2J4A
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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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3GWS
| Crystal Structure of T3-Bound Thyroid Hormone Receptor | Descriptor: | 3,5,3'TRIIODOTHYRONINE, Thyroid hormone receptor beta | Authors: | Nascimento, A.S, Dias, S.M.G, Nunes, F.M, Aparicio, R, Polikarpov, I, Baxter, J.D, Webb, P. | Deposit date: | 2009-04-01 | Release date: | 2009-04-28 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | 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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2PIN
| Thyroid receptor beta in complex with inhibitor | Descriptor: | 1-(4-HEXYLPHENYL)PROP-2-EN-1-ONE, SULFATE ION, Thyroid hormone receptor beta-1, ... | Authors: | Estebanez-Perpina, E, Jouravel, N, Baxter, J.D, Guy, L.R, Webb, P, Fletterick, R.J. | Deposit date: | 2007-04-13 | Release date: | 2008-02-26 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor. Mol.Endocrinol., 21, 2007
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7WLX
| A novel chemical derivative(53) of THRB agonist | Descriptor: | 2-[[1-methoxy-4-oxidanyl-7-[4-(phenylmethyl)phenoxy]isoquinolin-3-yl]carbonylamino]ethanoic acid, Isoform Beta-2 of Thyroid hormone receptor beta, Nuclear receptor coactivator 2 | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2022-01-14 | Release date: | 2022-05-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.39 Å) | Cite: | Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor beta Agonist. J.Med.Chem., 65, 2022
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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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1NQ2
| Two RTH Mutants with Impaired Hormone Binding | Descriptor: | ARSENIC, SODIUM ION, Thyroid hormone receptor beta-1, ... | 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: | 2003-01-21 | Release date: | 2003-04-15 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Two resistance to thyroid hormone mutants with impaired hormone binding Mol.Endocrinol., 17, 2003
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1XZX
| Thyroxine-Thyroid Hormone Receptor Interactions | Descriptor: | 3,5,3'TRIIODOTHYRONINE, 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: | 2004-11-12 | Release date: | 2004-12-07 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Thyroxine-thyroid hormone receptor interactions. J.Biol.Chem., 279, 2004
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3JZC
| Crystal Structure of TR-beta bound to the selective thyromimetic TRIAC | Descriptor: | Thyroid hormone receptor beta, [4-(4-HYDROXY-3-IODO-PHENOXY)-3,5-DIIODO-PHENYL]-ACETIC ACID | Authors: | Nascimento, A.S, Dias, S.G.M, Nunes, F.M, Aparicio, R. | Deposit date: | 2009-09-23 | Release date: | 2009-12-08 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Gaining ligand selectivity in thyroid hormone receptors via entropy. Proc.Natl.Acad.Sci.USA, 106, 2009
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3IMY
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7WMO
| A novel chemical derivative(92) of THRB agonist | Descriptor: | 2-[[1-ethoxy-7-[4-(3-fluoranyl-5-methoxy-phenyl)carbonyl-2,6-dimethyl-phenoxy]-4-oxidanyl-isoquinolin-3-yl]carbonylamino]ethanoic acid, Isoform Beta-2 of Thyroid hormone receptor beta, Nuclear receptor coactivator 2 | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2022-01-15 | Release date: | 2022-05-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.56 Å) | Cite: | Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor beta Agonist. J.Med.Chem., 65, 2022
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7WMN
| A novel chemical derivative(89) of THRB agonist | Descriptor: | 2-[[7-[2,6-dimethyl-4-(3-methylphenyl)carbonyl-phenoxy]-1-methoxy-4-oxidanyl-isoquinolin-3-yl]carbonylamino]ethanoic acid, Isoform Beta-2 of Thyroid hormone receptor beta, Nuclear receptor coactivator 2 | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2022-01-15 | Release date: | 2022-05-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.57 Å) | Cite: | Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor beta Agonist. J.Med.Chem., 65, 2022
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6KKE
| THRb mutation with a novel agonist | Descriptor: | 2-[(1-methyl-4-oxidanyl-7-phenoxy-isoquinolin-3-yl)carbonylamino]ethanoic acid, SRC2-3, Thyroid hormone receptor beta | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2019-07-25 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.577 Å) | Cite: | Revealing a Mutant-Induced Receptor Allosteric Mechanism for the Thyroid Hormone Resistance. Iscience, 20, 2019
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6KNW
| THRb mutation with a novel agonist | Descriptor: | 2-[(1-methyl-4-oxidanyl-7-phenoxy-isoquinolin-3-yl)carbonylamino]ethanoic acid, Nuclear receptor coactivator 2, Thyroid hormone receptor beta | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2019-08-07 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.67 Å) | Cite: | Revealing a Mutant-Induced Receptor Allosteric Mechanism for the Thyroid Hormone Resistance. Iscience, 20, 2019
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7WML
| A novel chemical derivative(85) of THRB agonist | Descriptor: | 2-[[7-[4-(3,5-dimethylphenyl)carbonyl-2,6-dimethyl-phenoxy]-1-ethoxy-4-oxidanyl-isoquinolin-3-yl]carbonylamino]ethanoic acid, Isoform Beta-2 of Thyroid hormone receptor beta, Nuclear receptor coactivator 2 | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2022-01-15 | Release date: | 2022-05-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.67 Å) | Cite: | Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor beta Agonist. J.Med.Chem., 65, 2022
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6KNU
| THRb mutation with a novel agonist | Descriptor: | 2-[(1-methyl-4-oxidanyl-7-phenoxy-isoquinolin-3-yl)carbonylamino]ethanoic acid, Nuclear receptor coactivator 2, Thyroid hormone receptor beta | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2019-08-07 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Revealing a Mutant-Induced Receptor Allosteric Mechanism for the Thyroid Hormone Resistance. Iscience, 20, 2019
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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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6KNV
| THRb mutation with a novel agonist | Descriptor: | 2-[(1-methyl-4-oxidanyl-7-phenoxy-isoquinolin-3-yl)carbonylamino]ethanoic acid, Nuclear receptor coactivator 2, Thyroid hormone receptor beta | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2019-08-07 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Revealing a Mutant-Induced Receptor Allosteric Mechanism for the Thyroid Hormone Resistance. Iscience, 20, 2019
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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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7WMJ
| A novel chemical derivative(71) of THRB agonist | Descriptor: | 2-[[7-[2,6-dimethyl-4-(phenylcarbonyl)phenoxy]-1-methoxy-4-oxidanyl-isoquinolin-3-yl]carbonylamino]ethanoic acid, Isoform Beta-2 of Thyroid hormone receptor beta, Nuclear receptor coactivator 2 | Authors: | Yao, B.Q, Li, Y. | Deposit date: | 2022-01-14 | Release date: | 2022-05-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.81 Å) | Cite: | Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor beta Agonist. J.Med.Chem., 65, 2022
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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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