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{{STRUCTURE_4lsj|  PDB=4lsj  |  SCENE=  }}
===Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Bound to a Dibenzoxapine Sulfonamide===
{{ABSTRACT_PUBMED_24446728}}


==Disease==
==Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Bound to a Dibenzoxapine Sulfonamide==
[[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>
<StructureSection load='4lsj' size='340' side='right'caption='[[4lsj]], [[Resolution|resolution]] 2.35&Aring;' scene=''>
 
== Structural highlights ==
==Function==
<table><tr><td colspan='2'>[[4lsj]] is a 2 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=4LSJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4LSJ FirstGlance]. <br>
[[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>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.35&#8491;</td></tr>
 
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LSJ:N-{3-[(1Z)-1-(10-METHOXYDIBENZO[B,E]OXEPIN-11(6H)-YLIDENE)PROPYL]PHENYL}METHANESULFONAMIDE'>LSJ</scene></td></tr>
==About this Structure==
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4lsj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lsj OCA], [https://pdbe.org/4lsj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4lsj RCSB], [https://www.ebi.ac.uk/pdbsum/4lsj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4lsj ProSAT]</span></td></tr>
[[4lsj]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LSJ OCA].
</table>
== Disease ==
[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 ==
[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==
*[[Glucocorticoid receptor|Glucocorticoid receptor]]
*[[Glucocorticoid receptor 3D structures|Glucocorticoid receptor 3D structures]]
 
== References ==
==Reference==
<references/>
<ref group="xtra">PMID:024446728</ref><references group="xtra"/><references/>
__TOC__
[[Category: Carson, M.]]
</StructureSection>
[[Category: Clawson, D.]]
[[Category: Homo sapiens]]
[[Category: Coghlan, M.]]
[[Category: Large Structures]]
[[Category: Luz, J G.]]
[[Category: Carson M]]
[[Category: Nuclear hormone receptor]]
[[Category: Clawson D]]
[[Category: Transcription]]
[[Category: Coghlan M]]
[[Category: Luz JG]]

Latest revision as of 12:21, 1 March 2024

Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Bound to a Dibenzoxapine Sulfonamide

4lsj, resolution 2.35Å

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