5uc1: Difference between revisions

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'''Unreleased structure'''


The entry 5uc1 is ON HOLD
==Structural Analysis of Glucocorticoid Receptor beta Ligand Binding Domain Complexed with Glucocorticoid Antagonist RU-486: Implication of Helix 12 in Antagonism==
<StructureSection load='5uc1' size='340' side='right'caption='[[5uc1]], [[Resolution|resolution]] 2.35&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5uc1]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Heterocephalus_glaber Heterocephalus glaber]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5UC1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5UC1 FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.351&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=486:11-(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'>486</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=CPS:3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE'>CPS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=MPD:(4S)-2-METHYL-2,4-PENTANEDIOL'>MPD</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5uc1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5uc1 OCA], [https://pdbe.org/5uc1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5uc1 RCSB], [https://www.ebi.ac.uk/pdbsum/5uc1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5uc1 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/G5AQS2_HETGA G5AQS2_HETGA]
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Glucocorticoid receptor beta (GRbeta) is associated with glucocorticoid resistance via dominant negative regulation of GRalpha. To better understand how GRbeta functions as a dominant negative inhibitor of GRalpha at a molecular level, we determined the crystal structure of the ligand binding domain of GRbeta complexed with antagonist RU-486. The structure reveals that RU-486 binds in the same ligand binding pocket as in GRalpha and the unique C-terminal amino acids of GRbeta are mostly disordered. Binding energy analysis suggests that these C-terminal residues of GRbeta do not contribute to RU-486 binding. Intriguingly, the GRbeta/RU-486 complex binds corepressor peptide with similar affinity as GRalpha/RU-486 complex, despite the lack of helix 12. Our biophysical and biochemical analysis reveals that in the presence of RU-486, GRbeta is found in a conformation that favors corepressor binding, potentially antagonizing GRalpha function. This study thus presents an unexpected molecular mechanism by which GRbeta could repress transcription.


Authors: Pedersen, L.C., Min, J.
Probing Dominant Negative Behavior of Glucocorticoid Receptor beta through a Hybrid Structural and Biochemical Approach.,Min J, Perera L, Krahn JM, Jewell CM, Moon AF, Cidlowski JA, Pedersen LC Mol Cell Biol. 2018 Feb 5. pii: MCB.00453-17. doi: 10.1128/MCB.00453-17. PMID:29437838<ref>PMID:29437838</ref>


Description: Nuclear receptor
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[Category: Unreleased Structures]]
</div>
[[Category: Min, J]]
<div class="pdbe-citations 5uc1" style="background-color:#fffaf0;"></div>
[[Category: Pedersen, L.C]]
 
==See Also==
*[[Glucocorticoid receptor 3D structures|Glucocorticoid receptor 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Heterocephalus glaber]]
[[Category: Large Structures]]
[[Category: Min J]]
[[Category: Pedersen LC]]
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