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PDB: 59 件
4UDD
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BU of 4udd by Molmil
GR in complex with desisobutyrylciclesonide
分子名称: 1,2-ETHANEDIOL, 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, DESISOBUYTYRYL CICLESONIDE, ...
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 (1.8 Å)
主引用文献Ligand Binding Mechanism in Steroid Receptors: From Conserved Plasticity to Differential Evolutionary Constraints.
Structure, 23, 2015
5E69
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BU of 5e69 by Molmil
Glucocorticoid receptor DNA binding domain - IL8 NF-kB response element complex
分子名称: DNA (5'-D(*AP*TP*CP*GP*TP*GP*GP*AP*AP*TP*TP*TP*CP*CP*TP*C)-3'), DNA (5'-D(*GP*AP*GP*GP*AP*AP*AP*TP*TP*CP*CP*AP*CP*GP*AP*T)-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 (1.85 Å)
主引用文献Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
4HN5
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BU of 4hn5 by Molmil
GR DNA Binding Domain - 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 (1.902 Å)
主引用文献The structural basis of direct glucocorticoid-mediated transrepression.
Nat.Struct.Mol.Biol., 20, 2013
4P6W
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BU of 4p6w by Molmil
Crystal Structure of mometasone furoate-bound glucocorticoid receptor ligand binding domain
分子名称: Glucocorticoid receptor, MOMETASONE FUROATE, 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 (1.951 Å)
主引用文献Structures and mechanism for the design of highly potent glucocorticoids.
Cell Res., 24, 2014
8A9G
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BU of 8a9g by Molmil
Binary complex of 14-3-3 zeta Glucocorticoid Receptor (GR) pT524 peptide stabilised by (R)-para chloropyrrolidone1
分子名称: 14-3-3 protein zeta/delta, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 5-[(2~{R})-3-(4-chlorophenyl)carbonyl-2-(4-nitrophenyl)-4-oxidanyl-5-oxidanylidene-2~{H}-pyrrol-1-yl]-2-oxidanyl-benzoic acid, ...
著者Munier, C.C, Edman, K, Perry, M.W.D, Ottmann, C.
登録日2022-06-28
公開日2022-12-28
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.961 Å)
主引用文献Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3-3 Protein-Protein Interaction.
J.Med.Chem., 65, 2022
5CBY
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BU of 5cby by Molmil
AncGR2 DNA Binding Domain - (+)GRE Complex
分子名称: AncGR2 DNA Binding Domain, 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'), ...
著者Hudson, W.H, 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 (1.997 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
5CBX
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BU of 5cbx by Molmil
AncGR DNA Binding Domain - (+)GRE Complex
分子名称: AncGR DNA Binding Domain, 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'), ...
著者Hudson, W.H, 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 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
6X6E
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BU of 6x6e by Molmil
Glucocorticoid Receptor DNA binding domain in complex with methylated precursor for a modern recognition element (methylated pre-GBS)
分子名称: DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*GP*GP*AP*GP*(5CM)P*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*TP*CP*AP*GP*AP*AP*CP*GP*CP*TP*CP*(5CM)P*GP*TP*TP*CP*TP*G)-3'), Glucocorticoid receptor, ...
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 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
5UC3
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BU of 5uc3 by Molmil
Structure of the dominant negative mutant Glucocorticoid Receptor alpha (L733K/N734P) complexed with RU-486
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Min, J, Cidlowski, J.A, Pedersen, L.C.
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 (2.009 Å)
主引用文献Nuclear receptor
To Be Published
6YMO
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BU of 6ymo by Molmil
Binary complex of 14-3-3 zeta with Glucocorticoid Receptor (GR) pS617 peptide
分子名称: 14-3-3 protein zeta/delta, 2-HYDROXYBENZOIC ACID, Glucocorticoid receptor, ...
著者Munier, C.C, Edman, K, Perry, M.W.D, Ottmann, C.
登録日2020-04-09
公開日2021-03-24
最終更新日2024-01-24
実験手法X-RAY DIFFRACTION (2.02 Å)
主引用文献Glucocorticoid receptor Thr524 phosphorylation by MINK1 induces interactions with 14-3-3 protein regulators.
J.Biol.Chem., 296, 2021
6YO8
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BU of 6yo8 by Molmil
Binary complex of 14-3-3 zeta with Glucocorticoid Receptor (GR) pT524 peptide
分子名称: 14-3-3 protein zeta/delta, Glucocorticoid receptor
著者Munier, C.C, Edman, K, Perry, M.W.D, Ottmann, C.
登録日2020-04-14
公開日2021-03-24
最終更新日2024-01-24
実験手法X-RAY DIFFRACTION (2.09 Å)
主引用文献Glucocorticoid receptor Thr524 phosphorylation by MINK1 induces interactions with 14-3-3 protein regulators.
J.Biol.Chem., 296, 2021
3K22
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BU of 3k22 by Molmil
Glucocorticoid Receptor with Bound alaninamide 10 with TIF2 peptide
分子名称: Glucocorticoid receptor, N-[(1R)-2-amino-1-methyl-2-oxoethyl]-3-(6-methyl-4-{[3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl]amino}-1H-indazol-1-yl)benzamide, Transcriptional Intermediary Factor 2, ...
著者Biggadike, K.B, McLay, I.M, Madauss, K.P, Williams, S.P, Bledsoe, R.K.
登録日2009-09-29
公開日2010-08-11
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.
Proc.Natl.Acad.Sci.USA, 106, 2009
5NFP
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BU of 5nfp by Molmil
Glucocorticoid Receptor in complex with budesonide
分子名称: (1~{S},2~{S},4~{R},6~{R},8~{S},9~{S},11~{S},12~{S},13~{R})-9,13-dimethyl-11-oxidanyl-8-(2-oxidanylethanoyl)-6-propyl-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-16-one, 1,2-ETHANEDIOL, 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, ...
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 (2.1 Å)
主引用文献Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
J. Med. Chem., 60, 2017
8VKZ
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BU of 8vkz by Molmil
Crystal structure of Glucocorticoid Receptor in complex with an inhibitor
分子名称: (4aR,4bS,5R,6aS,6bS,8R,9aR,10aR,10bR)-8-{4-[(3-aminophenyl)methyl]phenyl}-5-hydroxy-6b-(hydroxyacetyl)-4a,6a-dimethyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H,8H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-2-one, Glucocorticoid receptor, Nuclear receptor coactivator 2
著者Judge, R.A, Hobson, A.D.
登録日2024-01-10
公開日2024-01-24
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (2.133 Å)
主引用文献Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties.
Rsc Med Chem, 15, 2024
3E7C
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BU of 3e7c by Molmil
Glucocorticoid Receptor LBD bound to GSK866
分子名称: 5-amino-N-[(2S)-2-({[(2,6-dichlorophenyl)carbonyl](ethyl)amino}methyl)-3,3,3-trifluoro-2-hydroxypropyl]-1-(4-fluorophenyl)-1H-pyrazole-4-carboxamide, GLYCEROL, Glucocorticoid receptor, ...
著者Madauss, K.P, Williams, S.P, Mclay, I, Stewart, E.L, Bledsoe, R.K.
登録日2008-08-18
公開日2008-11-25
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.15 Å)
主引用文献The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Bioorg.Med.Chem.Lett., 18, 2008
5VA7
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BU of 5va7 by Molmil
Glucocorticoid Receptor DNA Binding Domain - IL11 AP-1 recognition element Complex
分子名称: DNA (5'-D(*AP*GP*GP*GP*TP*GP*AP*GP*TP*CP*AP*GP*GP*AP*TP*G)-3'), DNA (5'-D(*CP*AP*TP*CP*CP*TP*GP*AP*CP*TP*CP*AP*CP*CP*CP*T)-3'), Glucocorticoid receptor, ...
著者Weikum, E.R, Ortlund, E.A.
登録日2017-03-24
公開日2017-08-09
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.153 Å)
主引用文献Tethering not required: the glucocorticoid receptor binds directly to activator protein-1 recognition motifs to repress inflammatory genes.
Nucleic Acids Res., 45, 2017
6EL7
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BU of 6el7 by Molmil
Glucocorticoid Receptor in complex with compound 31
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 (2.18 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
6EL9
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BU of 6el9 by Molmil
Glucocorticoid Receptor in complex with AZD9567
分子名称: 1,2-ETHANEDIOL, 2,2-bis(fluoranyl)-~{N}-[(1~{R},2~{S})-3-methyl-1-[1-(1-methyl-6-oxidanylidene-pyridin-3-yl)indazol-5-yl]oxy-1-phenyl-butan-2-yl]propanamide, Glucocorticoid receptor, ...
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 (2.19 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
5E6A
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BU of 5e6a by Molmil
Glucocorticoid receptor DNA binding domain - PLAU NF-kB response element complex
分子名称: DNA (5'-D(*AP*TP*CP*AP*GP*GP*AP*AP*AP*TP*TP*CP*CP*CP*AP*G)-3'), DNA (5'-D(*CP*TP*GP*GP*GP*AP*AP*TP*TP*TP*CP*CP*TP*GP*AP*T)-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 (2.197 Å)
主引用文献Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
5CBZ
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BU of 5cbz by Molmil
AncMR DNA Binding Domain - (+)GRE Complex
分子名称: AncMR DNA Binding Domain, DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*CP*TP*CP*TP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*TP*CP*AP*GP*AP*AP*CP*AP*GP*AP*GP*TP*GP*TP*TP*CP*TP*G)-3'), ...
著者Hudson, W.H, 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 (2.2 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
5G5W
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BU of 5g5w by Molmil
Structure guided design and discovery of Indazole ethers as highly potent, non-steroidal Glucocorticoid receptor modulators
分子名称: 1,2-ETHANEDIOL, 2,2,2-trifluoro-N-[(1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-phenylpropan-2-yl]acetamide, GLUCOCORTICOID RECEPTOR, ...
著者Hemmerling, M, Edman, K, Lepisto, M, Eriksson, A, Ivanova, S, Dahmen, J, Rehwinkel, H, Berger, M, Hendrickx, R, Dearman, M, Jellesmark-Jensen, T, Wissler, L, Hansson, T.
登録日2016-06-08
公開日2017-02-15
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Discovery of Indazole Ethers as Novel, Potent, Non-Steroidal Glucocorticoid Receptor Modulators.
Bioorg.Med.Chem.Lett., 26, 2017
5E6C
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BU of 5e6c by Molmil
Glucocorticoid receptor DNA binding domain - CCL2 NF-kB response element complex
分子名称: DNA (5'-D(*AP*GP*TP*GP*GP*AP*AP*AP*TP*TP*CP*CP*CP*AP*CP*T)-3'), DNA (5'-D(*AP*GP*TP*GP*GP*GP*AP*AP*TP*TP*TP*CP*CP*AP*CP*T)-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 (2.2 Å)
主引用文献Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
7PRX
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BU of 7prx by Molmil
wildtype ligand binding domain of the glucocorticoid receptor complexed with velsecorat and a PGC1a coactivator fragment
分子名称: Glucocorticoid receptor, Peroxisome proliferator-activated receptor gamma coactivator 1-alpha, Velsecorat
著者Edman, K, Wissler, L, Koehler, C, Postel, S.
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 (2.2 Å)
主引用文献Quaternary glucocorticoid receptor structure highlights allosteric interdomain communication.
Nat.Struct.Mol.Biol., 30, 2023
5E6B
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BU of 5e6b by Molmil
Glucocorticoid receptor DNA binding domain - RELB NF-kB response element complex
分子名称: DNA (5'-D(*CP*CP*GP*GP*GP*GP*AP*AP*TP*TP*CP*CP*GP*CP*CP*G)-3'), DNA (5'-D(*CP*GP*GP*CP*GP*GP*AP*AP*TP*TP*CP*CP*CP*CP*GP*G)-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 (2.25 Å)
主引用文献Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
5VA0
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BU of 5va0 by Molmil
Glucocorticoid Receptor DNA Binding Domain in complex with AP-1 response element from VCAM-1 Promoter
分子名称: DNA (5'-D(*CP*GP*GP*CP*TP*GP*AP*CP*TP*CP*AP*TP*CP*AP*AP*G)-3'), DNA (5'-D(*CP*TP*TP*GP*AP*TP*GP*AP*GP*TP*CP*AP*GP*CP*CP*G)-3'), Glucocorticoid receptor, ...
著者Weikum, E.R, Ortlund, E.A.
登録日2017-03-24
公開日2017-08-09
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.295 Å)
主引用文献Tethering not required: the glucocorticoid receptor binds directly to activator protein-1 recognition motifs to repress inflammatory genes.
Nucleic Acids Res., 45, 2017

 

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