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==
==Crystal Structure of the Glucocorticoid Receptor Bound to a Non-steroidal Antagonist Reveals Repositioning and Partial Disordering of Activation Function Helix 12==
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<StructureSection load='4mdd' size='340' side='right' caption='[[4mdd]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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<StructureSection load='4mdd' size='340' side='right'caption='[[4mdd]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4mdd]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MDD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4MDD FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4mdd]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MDD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4MDD FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=29M:N-[2-{[BENZYL(METHYL)AMINO]METHYL}-3-(4-FLUORO-2-METHOXYPHENYL)-5-(PROPAN-2-YL)-1H-INDOL-7-YL]METHANESULFONAMIDE'>29M</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4&#8491;</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4mdd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mdd OCA], [http://pdbe.org/4mdd PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4mdd RCSB], [http://www.ebi.ac.uk/pdbsum/4mdd PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4mdd ProSAT]</span></td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=29M:N-[2-{[BENZYL(METHYL)AMINO]METHYL}-3-(4-FLUORO-2-METHOXYPHENYL)-5-(PROPAN-2-YL)-1H-INDOL-7-YL]METHANESULFONAMIDE'>29M</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4mdd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mdd OCA], [https://pdbe.org/4mdd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4mdd RCSB], [https://www.ebi.ac.uk/pdbsum/4mdd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4mdd ProSAT]</span></td></tr>
</table>
</table>
== Disease ==
== Disease ==
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[[http://www.uniprot.org/uniprot/GCR_HUMAN GCR_HUMAN]] Defects in NR3C1 are a cause of glucocorticoid resistance (GCRES) [MIM:[http://omim.org/entry/138040 138040]]; also known as cortisol resistance. It is a hypertensive, hyperandrogenic disorder characterized by increased serum cortisol concentrations. Inheritance is autosomal dominant.<ref>PMID:12050230</ref> <ref>PMID:1704018</ref> <ref>PMID:7683692</ref> <ref>PMID:11589680</ref> <ref>PMID:11701741</ref>
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[https://www.uniprot.org/uniprot/GCR_HUMAN GCR_HUMAN] Defects in NR3C1 are a cause of glucocorticoid resistance (GCRES) [MIM:[https://omim.org/entry/138040 138040]; also known as cortisol resistance. It is a hypertensive, hyperandrogenic disorder characterized by increased serum cortisol concentrations. Inheritance is autosomal dominant.<ref>PMID:12050230</ref> <ref>PMID:1704018</ref> <ref>PMID:7683692</ref> <ref>PMID:11589680</ref> <ref>PMID:11701741</ref>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/GCR_HUMAN GCR_HUMAN]] Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth. Involved in chromatin remodeling. Plays a significant role in transactivation.<ref>PMID:21664385</ref> [[http://www.uniprot.org/uniprot/NCOR1_HUMAN NCOR1_HUMAN]] Mediates transcriptional repression by certain nuclear receptors. Part of a complex which promotes histone deacetylation and the formation of repressive chromatin structures which may impede the access of basal transcription factors.<ref>PMID:14527417</ref>
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[https://www.uniprot.org/uniprot/GCR_HUMAN GCR_HUMAN] Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth. Involved in chromatin remodeling. Plays a significant role in transactivation.<ref>PMID:21664385</ref>
==See Also==
==See Also==
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*[[Glucocorticoid receptor|Glucocorticoid receptor]]
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*[[Glucocorticoid receptor 3D structures|Glucocorticoid receptor 3D structures]]
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*[[Nuclear receptor corepressor|Nuclear receptor corepressor]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Coghlan, M J]]
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[[Category: Homo sapiens]]
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[[Category: Luz, J G]]
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[[Category: Large Structures]]
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[[Category: Nuclear hormone receptor ligand binding domain]]
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[[Category: Coghlan MJ]]
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[[Category: Protein binding]]
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[[Category: Luz JG]]

Current revision

Crystal Structure of the Glucocorticoid Receptor Bound to a Non-steroidal Antagonist Reveals Repositioning and Partial Disordering of Activation Function Helix 12

PDB ID 4mdd

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