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==Crystal structure of RORgamma complexed with SRC2 and compound 5d==
==Crystal structure of RORgamma complexed with SRC2 and compound 5d==
<StructureSection load='5yp5' size='340' side='right' caption='[[5yp5]], [[Resolution|resolution]] 2.65&Aring;' scene=''>
<StructureSection load='5yp5' size='340' side='right'caption='[[5yp5]], [[Resolution|resolution]] 2.65&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[5yp5]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YP5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5YP5 FirstGlance]. <br>
<table><tr><td colspan='2'>[[5yp5]] 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=5YP5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5YP5 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4CZ:2-[4-(ethylsulfonyl)phenyl]-N-{5-[2-(2-methylpropyl)benzoyl]-4-phenyl-1,3-thiazol-2-yl}acetamide'>4CZ</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.65&#8491;</td></tr>
<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=5yp5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5yp5 OCA], [http://pdbe.org/5yp5 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5yp5 RCSB], [http://www.ebi.ac.uk/pdbsum/5yp5 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5yp5 ProSAT]</span></td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=4CZ:2-[4-(ethylsulfonyl)phenyl]-N-{5-[2-(2-methylpropyl)benzoyl]-4-phenyl-1,3-thiazol-2-yl}acetamide'>4CZ</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=5yp5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5yp5 OCA], [https://pdbe.org/5yp5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5yp5 RCSB], [https://www.ebi.ac.uk/pdbsum/5yp5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5yp5 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/RORG_HUMAN RORG_HUMAN]] Possible nuclear receptor for hydroxycholesterols, the binding of which strongly promotes coactivators recruitment. Essential for thymopoiesis and the development of several secondary lymphoid tissues, including lymph nodes. Involved in lineage specification of uncommitted CD4(+) T-helper cells into Th17 cells. Regulate the expression of several components of the circadian clock.  
[https://www.uniprot.org/uniprot/RORG_HUMAN RORG_HUMAN] Possible nuclear receptor for hydroxycholesterols, the binding of which strongly promotes coactivators recruitment. Essential for thymopoiesis and the development of several secondary lymphoid tissues, including lymph nodes. Involved in lineage specification of uncommitted CD4(+) T-helper cells into Th17 cells. Regulate the expression of several components of the circadian clock.
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Biaryl amides as new RORgammat modulators were discovered. The crystal structure of biaryl amide agonist 6 in complex with RORgammat ligand binding domain (LBD) was resolved, and both "short" and "long" inverse agonists were obtained by removing from 6 or adding to 6 a proper structural moiety. While "short" inverse agonist (8) recruits a corepressor peptide and dispels a coactivator peptide, "long" inverse agonist (9) dispels both. The two types of inverse agonists can be utilized as potential tools to study mechanisms of Th17 transcriptional network inhibition and related disease biology.
 
From RORgammat Agonist to Two Types of RORgammat Inverse Agonists.,Wang Y, Cai W, Tang T, Liu Q, Yang T, Yang L, Ma Y, Zhang G, Huang Y, Song X, Orband-Miller LA, Wu Q, Zhou L, Xiang Z, Xiang JN, Leung S, Shao L, Lin X, Lobera M, Ren F ACS Med Chem Lett. 2018 Jan 22;9(2):120-124. doi: 10.1021/acsmedchemlett.7b00476., eCollection 2018 Feb 8. PMID:29456799<ref>PMID:29456799</ref>
 
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 5yp5" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Cai, W]]
[[Category: Homo sapiens]]
[[Category: Chunwa, C]]
[[Category: Large Structures]]
[[Category: Gao, M]]
[[Category: Cai W]]
[[Category: Complex structure]]
[[Category: Chunwa C]]
[[Category: Nuclear receptor ror]]
[[Category: Gao M]]
[[Category: Transcription factor]]
[[Category: Transcription-inhibitor complex]]
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