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3MNE
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CRYSTAL STRUCTURE OF THE AGONIST FORM OF MOUSE GLUCOCORTICOID RECEPTOR STABILIZED BY F608S MUTATION AT 1.96A
Descriptor:Glucocorticoid receptor, Nuclear receptor coactivator 2 peptide, GLYCEROL, ...
Authors:Schoch, G.A., Seitz, T., Benz, J., Banner, D., Stihle, M., D'Arcy, B., Thoma, R., Sterner, R., Hennig, M., Ruf, A.
Deposit date:2010-04-21
Release date:2010-09-15
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.96 Å)
Cite:Enhancing the stability and solubility of the glucocorticoid receptor ligand-binding domain by high-throughput library screening.
J.Mol.Biol., 403, 2010
3MNO
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CRYSTAL STRUCTURE OF THE AGONIST FORM OF MOUSE GLUCOCORTICOID RECEPTOR STABILIZED BY (A611V, F608S) MUTATIONS AT 1.55A
Descriptor:Glucocorticoid receptor, Nuclear receptor coactivator 2 peptide, GLYCEROL, ...
Authors:Schoch, G.A., Seitz, T., Benz, J., Banner, D., Stihle, M., D'Arcy, B., Thoma, R., Sterner, R., Hennig, M., Ruf, A.
Deposit date:2010-04-22
Release date:2010-09-15
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.55 Å)
Cite:Enhancing the stability and solubility of the glucocorticoid receptor ligand-binding domain by high-throughput library screening.
J.Mol.Biol., 403, 2010
3MNP
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CRYSTAL STRUCTURE OF THE AGONIST FORM OF MOUSE GLUCOCORTICOID RECEPTOR STABILIZED BY (A611V, V708A, E711G) MUTATIONS AT 1.50A
Descriptor:Glucocorticoid receptor, Nuclear receptor coactivator 2 peptide, GLYCEROL, ...
Authors:Schoch, G.A., Seitz, T., Benz, J., Banner, D., Stihle, M., D'Arcy, B., Thoma, R., Sterner, R., Hennig, M., Ruf, A.
Deposit date:2010-04-22
Release date:2010-09-15
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.5 Å)
Cite:Enhancing the stability and solubility of the glucocorticoid receptor ligand-binding domain by high-throughput library screening.
J.Mol.Biol., 403, 2010
5CC1
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S425G GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN - (+)GRE COMPLEX
Descriptor:Glucocorticoid receptor, 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'), ...
Authors:Hudson, W.H., Weikum, E.A., Ortlund, E.A.
Deposit date:2015-07-01
Release date:2015-12-23
Last modified:2017-09-20
Method:X-RAY DIFFRACTION (2.302 Å)
Cite:Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space.
Proc.Natl.Acad.Sci.USA, 113, 2016
5E69
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GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN - IL8 NF-KB RESPONSE ELEMENT COMPLEX
Descriptor:Glucocorticoid receptor, DNA (5'-D(*GP*AP*GP*GP*AP*AP*AP*TP*TP*CP*CP*AP*CP*GP*AP*T)-3'), DNA (5'-D(*AP*TP*CP*GP*TP*GP*GP*AP*AP*TP*TP*TP*CP*CP*TP*C)-3'), ...
Authors:Hudson, W.H., Rye, E.A., Herbst, A.G., Ortlund, E.A.
Deposit date:2015-10-09
Release date:2017-02-08
Last modified:2018-10-24
Method:X-RAY DIFFRACTION (1.85 Å)
Cite:Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
5E6A
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GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN - PLAU NF-KB RESPONSE ELEMENT COMPLEX
Descriptor:Glucocorticoid receptor, DNA (5'-D(*CP*TP*GP*GP*GP*AP*AP*TP*TP*TP*CP*CP*TP*GP*AP*T)-3'), DNA (5'-D(*AP*TP*CP*AP*GP*GP*AP*AP*AP*TP*TP*CP*CP*CP*AP*G)-3'), ...
Authors:Hudson, W.H., Rye, E.A., Herbst, A.G., Ortlund, E.A.
Deposit date:2015-10-09
Release date:2017-02-08
Last modified:2018-10-24
Method:X-RAY DIFFRACTION (2.197 Å)
Cite:Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
5E6B
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GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN - RELB NF-KB RESPONSE ELEMENT COMPLEX
Descriptor:Glucocorticoid receptor, DNA (5'-D(*CP*GP*GP*CP*GP*GP*AP*AP*TP*TP*CP*CP*CP*CP*GP*G)-3'), DNA (5'-D(*CP*CP*GP*GP*GP*GP*AP*AP*TP*TP*CP*CP*GP*CP*CP*G)-3'), ...
Authors:Hudson, W.H., Rye, E.A., Herbst, A.G., Ortlund, E.A.
Deposit date:2015-10-09
Release date:2017-02-08
Last modified:2018-10-24
Method:X-RAY DIFFRACTION (2.25 Å)
Cite:Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
5E6C
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GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN - CCL2 NF-KB RESPONSE ELEMENT COMPLEX
Descriptor:Glucocorticoid receptor, 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'), ...
Authors:Hudson, W.H., Rye, E.A., Herbst, A.G., Ortlund, E.A.
Deposit date:2015-10-09
Release date:2017-02-08
Last modified:2018-10-24
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
5E6D
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GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN - ICAM1 NF-KB RESPONSE ELEMENT COMPLEX
Descriptor: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, ...
Authors:Hudson, W.H., Rye, E.A., Herbst, A.G., Ortlund, E.A.
Deposit date:2015-10-09
Release date:2017-02-08
Last modified:2018-10-24
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:Cryptic glucocorticoid receptor-binding sites pervade genomic NF-kappa B response elements.
Nat Commun, 9, 2018
5VA0
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GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN IN COMPLEX WITH AP-1 RESPONSE ELEMENT FROM VCAM-1 PROMOTER
Descriptor:Glucocorticoid receptor, 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'), ...
Authors:Weikum, E.R., Ortlund, E.A.
Deposit date:2017-03-24
Release date:2017-08-09
Last modified:2017-09-13
Method:X-RAY DIFFRACTION (2.295 Å)
Cite:Tethering not required: the glucocorticoid receptor binds directly to activator protein-1 recognition motifs to repress inflammatory genes.
Nucleic Acids Res., 45, 2017
5VA7
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GLUCOCORTICOID RECEPTOR DNA BINDING DOMAIN - IL11 AP-1 RECOGNITION ELEMENT COMPLEX
Descriptor:Glucocorticoid receptor, 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'), ...
Authors:Weikum, E.R., Ortlund, E.A.
Deposit date:2017-03-24
Release date:2017-08-09
Last modified:2017-09-13
Method:X-RAY DIFFRACTION (2.153 Å)
Cite:Tethering not required: the glucocorticoid receptor binds directly to activator protein-1 recognition motifs to repress inflammatory genes.
Nucleic Acids Res., 45, 2017
6DXK
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GLUCOCORTICOID RECEPTOR IN COMPLEX WITH COMPOUND 11
Descriptor:Glucocorticoid receptor, (8S,11R,13S,14S,17S)-11-[4-(dimethylamino)phenyl]-17-(3,3-dimethylbut-1-yn-1-yl)-17-hydroxy-13-methyl-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one (non-preferred name)
Authors:Rew, Y., Du, X., Eksterowicz, J., Zhou, H., Jahchan, N., Zhu, L., Yan, X., Kawai, H., McGee, L.R., Medina, J.C., Huang, T., Chen, C., Zavorotinskaya, T., Sutimantanapi, D., Waszczuk, J., Jackson, E., Huang, E., Ye, Q., Fantin, V.R., Daqing, S.
Deposit date:2018-06-29
Release date:2018-10-03
Method:X-RAY DIFFRACTION (3.05 Å)
Cite:Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
J. Med. Chem., 61, 2018
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
Descriptor:glucocorticoid receptor, nuclear receptor coactivator 2, B-OCTYLGLUCOSIDE, ...
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:2017-10-11
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
1NHZ
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CRYSTAL STRUCTURE OF THE ANTAGONIST FORM OF GLUCOCORTICOID RECEPTOR
Descriptor:GLUCOCORTICOID RECEPTOR, 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, 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:2011-07-13
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
1P93
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CRYSTAL STRUCTURE OF THE AGONIST FORM OF GLUCOCORTICOID RECEPTOR
Descriptor:Glucocorticoid receptor, Nuclear receptor coactivator 2, DEXAMETHASONE
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:2003-05-09
Release date:2003-07-08
Last modified:2018-01-31
Method:X-RAY DIFFRACTION (2.7 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
3BQD
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DOUBLING THE SIZE OF THE GLUCOCORTICOID RECEPTOR LIGAND BINDING POCKET BY DEACYLCORTIVAZOL
Descriptor:Glucocorticoid receptor, Nuclear receptor coactivator 1, 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
Authors:Xu, H.E.
Deposit date:2007-12-20
Release date:2008-01-15
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Doubling the size of the glucocorticoid receptor ligand binding pocket by deacylcortivazol.
Mol.Cell.Biol., 28, 2008
3CLD
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LIGAND BINDING DOMAIN OF THE GLUCOCORTICOID RECEPTOR COMPLEXED WITH FLUTICAZONE FUROATE
Descriptor:Glucocorticoid receptor, Tif2 coactivator motif, (6alpha,11alpha,14beta,16alpha,17alpha)-6,9-difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl furan-2-carboxylate
Authors:Shewchuk, L.M., McLay, I., Stewart, E., Biggadike, K.B., Hassell, A.M., Bledsoe, R.K.
Deposit date:2008-03-18
Release date:2008-06-24
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.84 Å)
Cite:X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain.
J.Med.Chem., 51, 2008
3E7C
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GLUCOCORTICOID RECEPTOR LBD BOUND TO GSK866
Descriptor:Glucocorticoid receptor, Nuclear receptor coactivator 2, 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, ...
Authors:Madauss, K.P., Williams, S.P., Mclay, I., Stewart, E.L., Bledsoe, R.K.
Deposit date:2008-08-18
Release date:2008-11-25
Last modified:2017-10-25
Method:X-RAY DIFFRACTION (2.15 Å)
Cite:The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Bioorg.Med.Chem.Lett., 18, 2008
3H52
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CRYSTAL STRUCTURE OF THE ANTAGONIST FORM OF HUMAN GLUCOCORTICOID RECEPTOR
Descriptor:Glucocorticoid receptor, Nuclear receptor corepressor 1, 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, ...
Authors:Schoch, G.A., Benz, J., D'Arcy, B., Stihle, M., Burger, D., Thoma, R., Ruf, A.
Deposit date:2009-04-21
Release date:2009-12-01
Last modified:2014-02-05
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Molecular switch in the glucocorticoid receptor: active and passive antagonist conformations
J.Mol.Biol., 395, 2010
3K22
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GLUCOCORTICOID RECEPTOR WITH BOUND ALANINAMIDE 10 WITH TIF2 PEPTIDE
Descriptor:Glucocorticoid receptor, Transcriptional Intermediary Factor 2, 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, ...
Authors:Biggadike, K.B., McLay, I.M., Madauss, K.P., Williams, S.P., Bledsoe, R.K.
Deposit date:2009-09-29
Release date:2010-08-11
Last modified:2017-11-01
Method:X-RAY DIFFRACTION (2.1 Å)
Cite: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
3K23
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GLUCOCORTICOID RECEPTOR WITH BOUND D-PROLINAMIDE 11
Descriptor:Glucocorticoid receptor, Nuclear receptor coactivator 2, 1-{[3-(4-{[(2R)-4-(5-fluoro-2-methoxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentyl]amino}-6-methyl-1H-indazol-1-yl)phenyl]carbonyl}-D-prolinamide
Authors:Biggadike, K.B., McLay, I.M., Madauss, K.P., Williams, S.P., Bledsoe, R.K.
Deposit date:2009-09-29
Release date:2009-10-27
Last modified:2017-11-01
Method:X-RAY DIFFRACTION (3 Å)
Cite: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
4CSJ
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THE DISCOVERY OF POTENT SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS, SUITABLE FOR INHALATION
Descriptor:GLUCOCORTICOID RECEPTOR, NUCLEAR RECEPTOR COACTIVATOR 2, 1,2-ETHANEDIOL, ...
Authors: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.
Deposit date:2014-03-07
Release date:2014-05-07
Last modified:2014-05-21
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:The Discovery of Potent and Selective Non-Steroidal Glucocorticoid Receptor Modulators, Suitable for Inhalation.
Bioorg.Med.Chem.Lett., 24, 2014
4HN5
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GR DNA BINDING DOMAIN - TSLP NGRE COMPLEX
Descriptor:Glucocorticoid receptor, DNA (5'-D(*CP*GP*CP*CP*TP*CP*CP*GP*GP*GP*AP*GP*AP*GP*CP*T)-3'), DNA (5'-D(*AP*GP*CP*TP*CP*TP*CP*CP*CP*GP*GP*AP*GP*GP*CP*G)-3'), ...
Authors:Hudson, W.H., Youn, C.E., Ortlund, E.A.
Deposit date:2012-10-18
Release date:2012-12-12
Last modified:2013-01-16
Method:X-RAY DIFFRACTION (1.902 Å)
Cite:The structural basis of direct glucocorticoid-mediated transrepression.
Nat.Struct.Mol.Biol., 20, 2013
4HN6
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GR DNA BINDING DOMAIN R460D/D462R - TSLP NGRE COMPLEX
Descriptor:Glucocorticoid receptor, DNA (5'-D(*CP*GP*CP*CP*TP*CP*CP*GP*GP*GP*AP*GP*AP*GP*CP*T)-3'), DNA (5'-D(*AP*GP*CP*TP*CP*TP*CP*CP*CP*GP*GP*AP*GP*GP*CP*G)-3'), ...
Authors:Hudson, W.H., Youn, C.E., Ortlund, E.A.
Deposit date:2012-10-18
Release date:2012-12-12
Last modified:2018-01-24
Method:X-RAY DIFFRACTION (2.549 Å)
Cite:The structural basis of direct glucocorticoid-mediated transrepression.
Nat.Struct.Mol.Biol., 20, 2013
4LSJ
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CRYSTAL STRUCTURE OF THE GLUCOCORTICOID RECEPTOR LIGAND BINDING DOMAIN BOUND TO A DIBENZOXAPINE SULFONAMIDE
Descriptor:Glucocorticoid receptor, D30 peptide, N-{3-[(1Z)-1-(10-methoxydibenzo[b,e]oxepin-11(6H)-ylidene)propyl]phenyl}methanesulfonamide
Authors:Carson, M., Luz, J.G., Clawson, D., Coghlan, M.
Deposit date:2013-07-22
Release date:2014-01-29
Last modified:2014-03-12
Method:X-RAY DIFFRACTION (2.35 Å)
Cite: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
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