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5yp5

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Revision as of 09:24, 21 October 2020

Crystal structure of RORgamma complexed with SRC2 and compound 5d

Structural highlights

5yp5 is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[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.

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^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ 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. From RORgammat Agonist to Two Types of RORgammat Inverse Agonists. ACS Med Chem Lett. 2018 Jan 22;9(2):120-124. doi: 10.1021/acsmedchemlett.7b00476., eCollection 2018 Feb 8. PMID:29456799 doi:http://dx.doi.org/10.1021/acsmedchemlett.7b00476

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/5yp5"

@@ Line 1: / Line 1: @@
 ==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 ==
-<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. 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://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='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'>[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='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/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>
 </table>
 == Function ==
@@ Line 22: / Line 22: @@
 __TOC__
 </StructureSection>
+[[Category: Large Structures]]
 [[Category: Cai, W]]
 [[Category: Chunwa, C]]

5yp5

From Proteopedia

Revision as of 09:24, 21 October 2020

Crystal structure of RORgamma complexed with SRC2 and compound 5d

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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