6fx0

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==Structure-based design of Trifarotene (CD5789), a potent and selective RAR gamma agonist for the treatment of acne==
==Structure-based design of Trifarotene (CD5789), a potent and selective RAR gamma agonist for the treatment of acne==
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<StructureSection load='6fx0' size='340' side='right' caption='[[6fx0]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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<StructureSection load='6fx0' size='340' side='right'caption='[[6fx0]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6fx0]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6FX0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6FX0 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6fx0]] is a 1 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=6FX0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6FX0 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=E9T:6-[3-(1-adamantyl)-4-oxidanyl-phenyl]naphthalene-2-carboxylic+acid'>E9T</scene>, <scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</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]] 1.9&#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=6fx0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6fx0 OCA], [http://pdbe.org/6fx0 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6fx0 RCSB], [http://www.ebi.ac.uk/pdbsum/6fx0 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6fx0 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=E9T:6-[3-(1-adamantyl)-4-oxidanyl-phenyl]naphthalene-2-carboxylic+acid'>E9T</scene>, <scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</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=6fx0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6fx0 OCA], [https://pdbe.org/6fx0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6fx0 RCSB], [https://www.ebi.ac.uk/pdbsum/6fx0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6fx0 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/RARG_HUMAN RARG_HUMAN]] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. Required for limb bud development. In concert with RARA or RARB, required for skeletal growth, matrix homeostasis and growth plate function (By similarity).
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[https://www.uniprot.org/uniprot/RARG_HUMAN RARG_HUMAN] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. Required for limb bud development. In concert with RARA or RARB, required for skeletal growth, matrix homeostasis and growth plate function (By similarity).
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 6fx0" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 6fx0" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Retinoic acid receptor 3D structures|Retinoic acid receptor 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Chantalat, L]]
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[[Category: Homo sapiens]]
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[[Category: Thoreau, E]]
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[[Category: Large Structures]]
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[[Category: Agonist]]
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[[Category: Chantalat L]]
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[[Category: Drug design]]
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[[Category: Thoreau E]]
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[[Category: Retinoic ligand complex]]
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[[Category: Selectivity]]
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[[Category: Signaling protein]]
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Current revision

Structure-based design of Trifarotene (CD5789), a potent and selective RAR gamma agonist for the treatment of acne

PDB ID 6fx0

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