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PDB: 59 件
4CSJ
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The discovery of potent selective glucocorticoid receptor modulators, suitable for inhalation
分子名称: 1,2-ETHANEDIOL, GLUCOCORTICOID RECEPTOR, N-[(2S)-1-[[1-(4-fluorophenyl)indazol-4-yl]amino]propan-2-yl]-2,4,6-trimethyl-benzenesulfonamide, ...
著者Edman, K, Ahlgren, R, Bengtsson, M, Bladh, H, Backstrom, S, Dahmen, J, Henriksson, K, Hillertz, P, Hulikal, V, Jerre, A, Kinchin, L, Kase, C, Lepisto, M, Mile, I, Nilsson, S, Smailagic, A, Taylor, J, Tjornebo, A, Wissler, L, Hansson, T.
登録日2014-03-07
公開日2014-05-07
最終更新日2023-12-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The Discovery of Potent and Selective Non-Steroidal Glucocorticoid Receptor Modulators, Suitable for Inhalation.
Bioorg.Med.Chem.Lett., 24, 2014
1NHZ
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Crystal Structure of the Antagonist Form of Glucocorticoid Receptor
分子名称: 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
著者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.
登録日2002-12-20
公開日2003-05-06
最終更新日2024-02-14
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献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
5NFT
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Glucocorticoid Receptor in complex with AZD5423
分子名称: 1,2-ETHANEDIOL, 2,2,2-tris(fluoranyl)-~{N}-[(1~{R},2~{S})-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]ethanamide, Glucocorticoid receptor, ...
著者Edman, K, Wissler, L.
登録日2017-03-15
公開日2017-10-04
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
J. Med. Chem., 60, 2017
5EMC
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Transcription factor GRDBD and smGRE complex
分子名称: DNA (5'-D(*CP*CP*AP*GP*AP*AP*(5CM)P*AP*TP*CP*AP*TP*GP*TP*TP*(5CM)P*TP*G)-3'), DNA (5'-D(*CP*CP*AP*GP*AP*AP*(5CM)P*AP*TP*GP*AP*TP*GP*TP*TP*(5CM)P*TP*G)-3'), Glucocorticoid receptor, ...
著者Su, X.D, Lian, T, Jin, J.
登録日2015-11-06
公開日2016-06-29
最終更新日2024-03-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The effects of cytosine methylation on general transcription factors
To Be Published
5EMP
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Transcription factor GRDBD and mmGRE complex
分子名称: DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*TP*GP*AP*TP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(P*CP*CP*AP*GP*AP*AP*CP*AP*TP*(5CM)P*AP*TP*GP*TP*TP*CP*TP*G)-3'), Glucocorticoid receptor, ...
著者Lian, T, Jin, J, Su, X.
登録日2015-11-06
公開日2016-06-29
最終更新日2024-03-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The effects of cytosine methylation on general transcription factors
To Be Published
5EMQ
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Transcription factor GRDBD and GRE complex
分子名称: DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*TP*CP*AP*TP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*TP*GP*AP*TP*GP*TP*TP*CP*TP*G)-3'), Glucocorticoid receptor, ...
著者Lian, T, Jin, J, Su, X.
登録日2015-11-06
公開日2016-06-29
最終更新日2024-03-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The effects of cytosine methylation on general transcription factors
To Be Published
5CC1
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S425G Glucocorticoid receptor DNA binding domain - (+)GRE complex
分子名称: DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*GP*AP*GP*TP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*TP*CP*AP*GP*AP*AP*CP*AP*CP*TP*CP*TP*GP*TP*TP*CP*TP*G)-3'), Glucocorticoid receptor, ...
著者Hudson, W.H, Weikum, E.A, Ortlund, E.A.
登録日2015-07-01
公開日2015-12-23
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.302 Å)
主引用文献Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space.
Proc.Natl.Acad.Sci.USA, 113, 2016
4LSJ
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Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Bound to a Dibenzoxapine Sulfonamide
分子名称: D30 peptide, Glucocorticoid receptor, N-{3-[(1Z)-1-(10-methoxydibenzo[b,e]oxepin-11(6H)-ylidene)propyl]phenyl}methanesulfonamide
著者Carson, M, Luz, J.G, Clawson, D, Coghlan, M.
登録日2013-07-22
公開日2014-01-29
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.35 Å)
主引用文献Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
J.Med.Chem., 57, 2014
5UC1
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Structural Analysis of Glucocorticoid Receptor beta Ligand Binding Domain Complexed with Glucocorticoid Antagonist RU-486: Implication of Helix 12 in Antagonism
分子名称: (4S)-2-METHYL-2,4-PENTANEDIOL, 1,2-ETHANEDIOL, 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, ...
著者Pedersen, L.C, Min, J.
登録日2016-12-21
公開日2017-12-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.351 Å)
主引用文献Probing Dominant Negative Behavior of Glucocorticoid Receptor beta through a Hybrid Structural and Biochemical Approach.
Mol. Cell. Biol., 2018
4MDD
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Crystal Structure of the Glucocorticoid Receptor Bound to a Non-steroidal Antagonist Reveals Repositioning and Partial Disordering of Activation Function Helix 12
分子名称: Glucocorticoid receptor, N-[2-{[benzyl(methyl)amino]methyl}-3-(4-fluoro-2-methoxyphenyl)-5-(propan-2-yl)-1H-indol-7-yl]methanesulfonamide, Nuclear receptor corepressor 1
著者Coghlan, M.J, Luz, J.G.
登録日2013-08-22
公開日2014-12-03
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Crystal Structure of the Glucocorticoid Receptor Bound to a Non-steroidal Antagonist Reveals Repositioning and Partial Disordering of Activation Function Helix 12
To be Published
5G3J
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Discovery of New Selective Glucocorticoid Receptor Agonist Leads
分子名称: 1,2-ETHANEDIOL, 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, 5-[[(1S,2R,4R)-4-ethyl-6,7-bis(fluoranyl)-2,5-bis(oxidanyl)-2-(trifluoromethyl)-3,4-dihydro-1H-naphthalen-1-yl]amino]-1H-quinolin-2-one, ...
著者Berger, M, Edman, K, Wissler, L, Neuhaus, R, Rehwinkel, H, Schacke, H, Jaroch, S.
登録日2016-04-27
公開日2017-02-15
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Discovery of New Selective Glucocorticoid Receptor Agonist Leads.
Bioorg.Med.Chem.Lett., 27, 2017
6BSF
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Human GR (418-507) in complex with monomeric DNA binding site
分子名称: DNA (5'-D(P*AP*AP*GP*CP*TP*AP*GP*TP*AP*CP*AP*TP*TP*TP*GP*C)-3'), DNA (5'-D(P*TP*GP*CP*AP*AP*AP*TP*GP*TP*AP*CP*TP*AP*GP*CP*T)-3'), Glucocorticoid receptor, ...
著者Pufall, M.A.
登録日2017-12-02
公開日2018-12-05
最終更新日2024-05-22
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献General and sequence-specific roles for DNA in glucocorticoid receptor DNA-binding stoichiometry
To Be Published
5E6D
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Glucocorticoid receptor DNA binding domain - ICAM1 NF-kB response element complex
分子名称: DNA (5'-D(*GP*CP*TP*CP*CP*GP*GP*AP*AP*TP*TP*TP*CP*CP*AP*A)-3'), DNA (5'-D(*TP*TP*GP*GP*AP*AP*AP*TP*TP*CP*CP*GP*GP*AP*GP*C)-3'), Glucocorticoid receptor, ...
著者Hudson, W.H, Rye, E.A, Herbst, A.G, Ortlund, E.A.
登録日2015-10-09
公開日2017-02-08
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
6EL6
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Glucocorticoid Receptor in complex with compound 4
分子名称: 1,2-ETHANEDIOL, Glucocorticoid receptor, Nuclear receptor coactivator 2, ...
著者Edman, K, Wissler, L.
登録日2017-09-28
公開日2018-02-21
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
J. Med. Chem., 61, 2018
6X6D
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BU of 6x6d by Molmil
Glucocorticoid Receptor DNA binding domain in complex with unmodified precursor for a modern recognition element (pre-GBS)
分子名称: CACODYLATE ION, DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*GP*GP*AP*GP*CP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*TP*CP*AP*GP*AP*AP*CP*GP*CP*TP*CP*CP*GP*TP*TP*CP*TP*G)-3'), ...
著者Liu, X, Ortlund, E.A.
登録日2020-05-28
公開日2021-06-02
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.48 Å)
主引用文献Structural basis for glucocorticoid receptor recognition of both unmodified and methylated binding sites, precursors of a modern recognition element.
Nucleic Acids Res., 49, 2021
3BQD
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Doubling the Size of the Glucocorticoid Receptor Ligand Binding Pocket by Deacylcortivazol
分子名称: 1-[(1R,2R,3aS,3bS,10aR,10bS,11S,12aS)-1,11-dihydroxy-2,5,10a,12a-tetramethyl-7-phenyl-1,2,3,3a,3b,7,10,10a,10b,11,12,12a-dodecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]-2-hydroxyethanone, Glucocorticoid receptor, Nuclear receptor coactivator 1
著者Xu, H.E.
登録日2007-12-20
公開日2008-01-15
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Doubling the size of the glucocorticoid receptor ligand binding pocket by deacylcortivazol.
Mol.Cell.Biol., 28, 2008
1M2Z
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Crystal structure of a dimer complex of the human glucocorticoid receptor ligand-binding domain bound to dexamethasone and a TIF2 coactivator motif
分子名称: DEXAMETHASONE, glucocorticoid receptor, nuclear receptor coactivator 2, ...
著者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.
登録日2002-06-26
公開日2003-07-15
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Reveals a Novel Mode of Receptor Dimerization and Coactivator Recognition
Cell(Cambridge,Mass.), 110, 2002
6CFN
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BU of 6cfn by Molmil
Crystal Structure of the DNA-free Glucocorticoid Receptor DNA Binding Domain
分子名称: Glucocorticoid receptor, ZINC ION
著者Frank, F, Okafor, C.D, Ortlund, E.A.
登録日2018-02-15
公開日2018-09-26
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献The first crystal structure of a DNA-free nuclear receptor DNA binding domain sheds light on DNA-driven allostery in the glucocorticoid receptor.
Sci Rep, 8, 2018
6BQU
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BU of 6bqu by Molmil
Human GR (418-507) in complex with monomeric DNA binding site
分子名称: DNA (5'-D(P*AP*AP*GP*CP*TP*AP*GP*TP*AP*CP*AP*TP*TP*TP*GP*C)-3'), DNA (5'-D(P*TP*GP*CP*AP*AP*AP*TP*GP*TP*AP*CP*TP*AP*GP*CP*T)-3'), Glucocorticoid receptor, ...
著者Pufall, M.A.
登録日2017-11-28
公開日2018-12-05
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献General and sequence-specific roles for DNA in glucocorticoid receptor DNA-binding stoichiometry
To Be Published
4P6X
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Crystal Structure of cortisol-bound glucocorticoid receptor ligand binding domain
分子名称: (11alpha,14beta)-11,17,21-trihydroxypregn-4-ene-3,20-dione, Glucocorticoid receptor, Nuclear receptor coactivator 2
著者He, Y, Zhou, X.E, Tolbert, W.D, Powell, K, Melcher, K, Xu, H.E.
登録日2014-03-25
公開日2014-04-16
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Structures and mechanism for the design of highly potent glucocorticoids.
Cell Res., 24, 2014
4UDC
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BU of 4udc by Molmil
GR in complex with dexamethasone
分子名称: 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, DEXAMETHASONE, GLUCOCORTICOID RECEPTOR, ...
著者Edman, K, Hogner, A, Hussein, A, Bjursell, M, Aagaard, A, Backstrom, S, Bodin, C, Wissler, L, Jellesmark-Jensen, T, Cavallin, A, Karlsson, U, Nilsson, E, Lecina, D, Takahashi, R, Grebner, C, Lepisto, M, Guallar, V.
登録日2014-12-09
公開日2015-11-25
最終更新日2023-12-20
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Ligand Binding Mechanism in Steroid Receptors: From Conserved Plasticity to Differential Evolutionary Constraints.
Structure, 23, 2015
7PRW
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BU of 7prw by Molmil
The glucocorticoid receptor in complex with velsecorat, a PGC1a coactivator fragment and sgk 23bp
分子名称: 1,2-ETHANEDIOL, DNA (5'-D(*GP*TP*AP*CP*AP*GP*AP*AP*CP*AP*TP*TP*TP*TP*GP*TP*CP*CP*GP*TP*CP*GP*A)-3'), DNA (5'-D(*TP*CP*GP*AP*CP*GP*GP*AP*CP*AP*AP*AP*AP*TP*GP*TP*TP*CP*TP*GP*TP*AP*C)-3'), ...
著者Postel, S, Edman, K, Wissler, L.
登録日2021-09-22
公開日2023-02-08
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.502 Å)
主引用文献Quaternary glucocorticoid receptor structure highlights allosteric interdomain communication.
Nat.Struct.Mol.Biol., 30, 2023
4HN6
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GR DNA Binding Domain R460D/D462R - TSLP nGRE Complex
分子名称: DNA (5'-D(*AP*GP*CP*TP*CP*TP*CP*CP*CP*GP*GP*AP*GP*GP*CP*G)-3'), DNA (5'-D(*CP*GP*CP*CP*TP*CP*CP*GP*GP*GP*AP*GP*AP*GP*CP*T)-3'), Glucocorticoid receptor, ...
著者Hudson, W.H, Youn, C.E, Ortlund, E.A.
登録日2012-10-18
公開日2012-12-12
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.549 Å)
主引用文献The structural basis of direct glucocorticoid-mediated transrepression.
Nat.Struct.Mol.Biol., 20, 2013
7KRJ
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The GR-Maturation Complex: Glucocorticoid Receptor in complex with Hsp90 and co-chaperone p23
分子名称: ADENOSINE-5'-TRIPHOSPHATE, DEXAMETHASONE, Glucocorticoid receptor, ...
著者Noddings, C.M, Wang, Y.-R, Agard, D.A.
登録日2020-11-20
公開日2022-01-12
最終更新日2024-05-29
実験手法ELECTRON MICROSCOPY (2.56 Å)
主引用文献Structure of Hsp90-p23-GR reveals the Hsp90 client-remodelling mechanism.
Nature, 601, 2021
7PRV
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The glucocorticoid receptor in complex with fluticasone furoate, a PGC1a coactivator fragment and sgk 23bp
分子名称: (6alpha,11alpha,14beta,16alpha,17alpha)-6,9-difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoan drosta-1,4-dien-17-yl furan-2-carboxylate, 1,2-ETHANEDIOL, DNA (5'-D(*TP*AP*CP*AP*GP*AP*AP*CP*AP*TP*TP*TP*TP*GP*TP*CP*CP*GP*TP*CP*GP*A)-3'), ...
著者Postel, S, Edman, K, Wissler, L.
登録日2021-09-22
公開日2023-02-08
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Quaternary glucocorticoid receptor structure highlights allosteric interdomain communication.
Nat.Struct.Mol.Biol., 30, 2023

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