1HLO
 
 | | THE CRYSTAL STRUCTURE OF AN INTACT HUMAN MAX-DNA COMPLEX: NEW INSIGHTS INTO MECHANISMS OF TRANSCRIPTIONAL CONTROL | | 分子名称: | DNA (5'-D(*AP*CP*CP*AP*CP*GP*TP*GP*GP*TP*G)-3'), DNA (5'-D(*CP*AP*CP*CP*AP*CP*GP*TP*GP*GP*T)-3'), PROTEIN (TRANSCRIPTION FACTOR MAX) | | 著者 | Brownlie, P, Ceska, T.A, Lamers, M, Romier, C, Theo, H, Suck, D. | | 登録日 | 1997-09-10 | | 公開日 | 1997-10-27 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | The crystal structure of an intact human Max-DNA complex: new insights into mechanisms of transcriptional control.
Structure, 5, 1997
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6CZW
 | | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex | | 分子名称: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, {2-bromo-3-(3-chloro-5-fluorophenoxy)-6-[(difluoromethyl)sulfonyl]phenyl}methanol | | 著者 | Du, X. | | 登録日 | 2018-04-09 | | 公開日 | 2018-10-31 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6D09
 | | Crystal structure of PT2440 bound to HIF2a-B*:ARNT-B* complex | | 分子名称: | 3-{[(3R)-4-(difluoromethyl)-2,2-difluoro-3-hydroxy-1,1-dioxo-2,3-dihydro-1H-1-benzothiophen-5-yl]oxy}-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | 著者 | Du, X. | | 登録日 | 2018-04-10 | | 公開日 | 2018-10-31 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6D0B
 | | Crystal structure of PT1614 bound to HIF2a-B*:ARNT-B* complex | | 分子名称: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, N-(3-chloro-5-fluorophenyl)-2-nitro-4-[(trifluoromethyl)sulfonyl]aniline | | 著者 | Du, X. | | 登録日 | 2018-04-10 | | 公開日 | 2018-10-31 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Crystal structure of PT1614 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6D0C
 | | Crystal structure of HIF2a-B*:ARNT-B* complex | | 分子名称: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | 著者 | Du, X. | | 登録日 | 2018-04-10 | | 公開日 | 2018-10-31 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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2KWF
 | | The structure of E-protein activation domain 1 bound to the KIX domain of CBP/p300 elucidates leukemia induction by E2A-PBX1 | | 分子名称: | CREB-binding protein, Transcription factor 4 | | 著者 | Denis, C.M, Chitayat, S, Plevin, M.J, Liu, S, Spencer, H.L, Ikura, M, LeBrun, D.P, Smith, S.P. | | 登録日 | 2010-04-08 | | 公開日 | 2011-07-20 | | 最終更新日 | 2024-05-01 | | 実験手法 | SOLUTION NMR | | 主引用文献 | The structure of E-protein activation domain 1 bound to the KIX domain of CBP/p300 elucidates leukemia induction by E2A-PBX1
To be Published
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4XT2
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist | | 分子名称: | (5S,7R)-5,7-bis(3-bromophenyl)-4,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidine, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | 著者 | Scheuermann, T.H, Gardner, K.H. | | 登録日 | 2015-01-22 | | 公開日 | 2015-12-09 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.698 Å) | | 主引用文献 | Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2.
J.Med.Chem., 58, 2015
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4GHI
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a benzoxadiazole antagonist | | 分子名称: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, N-(3-chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine | | 著者 | Scheuermann, T.H, Key, J, Tambar, U.K, Bruick, R.K, Gardner, K.H. | | 登録日 | 2012-08-07 | | 公開日 | 2013-02-27 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Allosteric inhibition of hypoxia inducible factor-2 with small molecules.
Nat.Chem.Biol., 9, 2013
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5I4V
 | | Discovery of novel, orally efficacious Liver X Receptor (LXR) beta agonists | | 分子名称: | Oxysterols receptor LXR-beta,Nuclear receptor coactivator 2, Retinoic acid receptor RXR-beta,Nuclear receptor coactivator 2, {2-[(2R)-4-[4-(hydroxymethyl)-3-(methylsulfonyl)phenyl]-2-(propan-2-yl)piperazin-1-yl]-4-(trifluoromethyl)pyrimidin-5-yl}methanol | | 著者 | Chen, G, McKeever, B.M. | | 登録日 | 2016-02-12 | | 公開日 | 2016-06-29 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.61 Å) | | 主引用文献 | Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) beta Agonist.
J.Med.Chem., 59, 2016
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4J5W
 | | Crystal Structure of the apo-PXR/RXRalpha LBD Heterotetramer Complex | | 分子名称: | MAGNESIUM ION, Nuclear receptor subfamily 1 group I member 2, Nuclear receptor coactivator 1, ... | | 著者 | Wallace, B.D, Betts, L, Redinbo, M.R. | | 登録日 | 2013-02-10 | | 公開日 | 2013-08-21 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structural and Functional Analysis of the Human Nuclear Xenobiotic Receptor PXR in Complex with RXRalpha.
J.Mol.Biol., 425, 2013
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4J5X
 | | Crystal Structure of the SR12813-bound PXR/RXRalpha LBD Heterotetramer Complex | | 分子名称: | Nuclear receptor subfamily 1 group I member 2, Nuclear receptor coactivator 1, Retinoic acid receptor RXR-alpha, ... | | 著者 | Wallace, B.D, Betts, L, Redinbo, M.R. | | 登録日 | 2013-02-10 | | 公開日 | 2013-08-21 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structural and Functional Analysis of the Human Nuclear Xenobiotic Receptor PXR in Complex with RXRalpha.
J.Mol.Biol., 425, 2013
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4PKY
 | | ARNT/HIF transcription factor/coactivator complex | | 分子名称: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, SULFATE ION, ... | | 著者 | Tomchick, D.R, Partch, C.L, Gardner, K.H. | | 登録日 | 2014-05-15 | | 公開日 | 2015-02-11 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Coiled-coil Coactivators Play a Structural Role Mediating Interactions in Hypoxia-inducible Factor Heterodimerization.
J.Biol.Chem., 290, 2015
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8G4A
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6GEV
 | | Mineralocorticoid receptor in complex with (s)-13 | | 分子名称: | 6-[[(3~{S})-7-fluoranyl-3-(2-methylpropyl)-2,3-dihydro-1,4-benzoxazin-4-yl]carbonyl]-4~{H}-1,4-benzoxazin-3-one, GLYCEROL, Mineralocorticoid receptor, ... | | 著者 | Edman, K, Aagaard, A, Tangefjord, S. | | 登録日 | 2018-04-27 | | 公開日 | 2019-01-09 | | 最終更新日 | 2024-05-15 | | 実験手法 | X-RAY DIFFRACTION (1.54 Å) | | 主引用文献 | Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection.
J.Med.Chem., 62, 2019
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6GG8
 | | Mineralocorticoid receptor in complex with (s)-13 | | 分子名称: | (4S)-2-METHYL-2,4-PENTANEDIOL, Mineralocorticoid receptor, Nuclear receptor coactivator 1, ... | | 著者 | Edman, K, Aagaard, A, Tangefjord, S. | | 登録日 | 2018-05-03 | | 公開日 | 2019-01-09 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection.
J.Med.Chem., 62, 2019
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7T2X
 | | Estrogen Receptor Alpha Ligand Binding Domain Y537S in Complex with 2-chloro-4-((4-hydroxybenzyl)amino)-5-phenylthieno[2,3-d]pyrimidin-6-ol and GRIP Peptide | | 分子名称: | Estrogen receptor, Nuclear receptor coactivator 2, S-(2-chloro-6-{[(4-hydroxyphenyl)methyl]amino}pyrimidin-4-yl) phenylethanethioate | | 著者 | Joiner, C, Sammeta, V.K.R, Norris, J.D, McDonnell, D.P, Wilson, T.M, Fanning, S.W. | | 登録日 | 2021-12-06 | | 公開日 | 2022-06-22 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3- d ]pyrimidine Core.
Acs Med.Chem.Lett., 13, 2022
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6BNS
 | | STRUCTURE OF HUMAN PREGNANE X RECEPTOR LIGAND BINDING DOMAIN BOUND TETHERED WITH SRC co-activator peptide and Compound 25a AKA BICYCLIC HEXAFLUOROISOPROPYL 2 ALCOHOL SULFONAMIDES | | 分子名称: | 2-[(2S)-4-[(4-fluorophenyl)sulfonyl]-7-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-3,4-dihydro-2H-1,4-benzothiazin-2-yl]-N-(2-hydroxy-2-methylpropyl)acetamide, Nuclear receptor subfamily 1 group I member 2,Nuclear receptor coactivator 1 Chimera | | 著者 | DHAR, T.G, GONG, H, WEINSTEIN, D.S, LU, Z, DUAN, J.J.W, STACHURA, S, HAQUE, L, KARMAKAR, A, HEMAGIRI, H, RAUT, D.K, GUPTA, A.K, KHAN, J.A, SACK, J.S, CAMAC, D.M, PUDZIANOWSKI, A.A, WU, D.R, YARDE, M, SHEN, D.R, BOROWSKI, V, XIE, J.H, SUN, H, ARIENZO, C.D, DABROS, M, GALELLA, M.A, WANG, F, WEIGELT, C.A, ZHAO, Q, FOSTER, W, SOMERVILLE, J.E, SALTER-CID, L.M, BARRISH, J.C, CARTER, P.H. | | 登録日 | 2017-11-17 | | 公開日 | 2017-12-20 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.56 Å) | | 主引用文献 | Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR gamma /RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bioorg. Med. Chem. Lett., 28, 2018
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2LFH
 | | Solution NMR Structure of the Helix-loop-Helix Domain of Human ID3 Protein, Northeast Structural Genomics Consortium Target HR3111A | | 分子名称: | DNA-binding protein inhibitor ID-3 | | 著者 | Eletsky, A, Wang, D, Kohan, E, Janjua, H, Acton, T.B, Xiao, R, Everett, J.K, Montelione, G.T, Szyperski, T, Northeast Structural Genomics Consortium (NESG) | | 登録日 | 2011-06-30 | | 公開日 | 2011-07-27 | | 最終更新日 | 2024-05-15 | | 実験手法 | SOLUTION NMR | | 主引用文献 | Solution NMR Structure of the Helix-loop-Helix Domain of Human ID3 Protein, Northeast Structural Genomics Consortium Target HR3111A
To be Published
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6HTY
 | | PXR in complex with P2X4 inhibitor compound 25 | | 分子名称: | (2~{R})-~{N}-[4-(3-chloranylphenoxy)-3-sulfamoyl-phenyl]-2-phenyl-propanamide, DIMETHYL SULFOXIDE, GLYCEROL, ... | | 著者 | Hillig, R.C, Puetter, V, Werner, S, Mesch, S, Laux-Biehlmann, A, Braeuer, N, Dahloef, H, Klint, J, ter Laak, A, Pook, E, Neagoe, I, Nubbemeyer, R, Schulz, S. | | 登録日 | 2018-10-05 | | 公開日 | 2019-12-04 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.22 Å) | | 主引用文献 | Discovery and Characterization of the Potent and Selective P2X4 InhibitorN-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile.
J.Med.Chem., 62, 2019
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8E1D
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3H7W
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains with the artificial ligand THS017 | | 分子名称: | 2-nitro-N-(thiophen-3-ylmethyl)-4-(trifluoromethyl)aniline, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | 著者 | Key, J.M, Scheuermann, T.H, Anderson, P.C, Daggett, V, Gardner, K.H. | | 登録日 | 2009-04-28 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Principles of ligand binding within a completely buried cavity in HIF2alpha PAS-B
J.Am.Chem.Soc., 131, 2009
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3H82
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains with the artificial ligand THS020 | | 分子名称: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, N-(furan-2-ylmethyl)-2-nitro-4-(trifluoromethyl)aniline | | 著者 | Key, J.M, Scheuermann, T.H, Anderson, P.C, Daggett, V, Gardner, K.H. | | 登録日 | 2009-04-28 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Principles of ligand binding within a completely buried cavity in HIF2alpha PAS-B
J.Am.Chem.Soc., 131, 2009
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2MH0
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5UFP
 | | Crystal structure of PT2399 bound to HIF2a-B*:ARNT-B* complex | | 分子名称: | 3-({(1S)-7-[(difluoromethyl)sulfonyl]-2,2-difluoro-1-hydroxy-2,3-dihydro-1H-inden-4-yl}oxy)-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | 著者 | Du, X. | | 登録日 | 2017-01-05 | | 公開日 | 2017-01-25 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | On-target efficacy of a HIF-2 alpha antagonist in preclinical kidney cancer models.
Nature, 539, 2016
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5TBM
 | | Crystal structure of PT2385 bound to HIF2a-B*:ARNT-B* complex | | 分子名称: | 3-{[(1S)-2,2-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | 著者 | Du, X. | | 登録日 | 2016-09-12 | | 公開日 | 2016-09-21 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | A Small-Molecule Antagonist of HIF2 alpha Is Efficacious in Preclinical Models of Renal Cell Carcinoma.
Cancer Res., 76, 2016
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