6qj5

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<StructureSection load='6qj5' size='340' side='right'caption='[[6qj5]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
<StructureSection load='6qj5' size='340' side='right'caption='[[6qj5]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6qj5]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6QJ5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6QJ5 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6qj5]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6QJ5 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6QJ5 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=H8R:(2~{S})-3-methyl-2-[(4-octoxyphenyl)carbonylamino]butanoic+acid'>H8R</scene></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=H8R:(2~{S})-3-methyl-2-[(4-octoxyphenyl)carbonylamino]butanoic+acid'>H8R</scene></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=6qj5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6qj5 OCA], [http://pdbe.org/6qj5 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6qj5 RCSB], [http://www.ebi.ac.uk/pdbsum/6qj5 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6qj5 ProSAT]</span></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PPARG, NR1C3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6qj5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6qj5 OCA], [http://pdbe.org/6qj5 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6qj5 RCSB], [http://www.ebi.ac.uk/pdbsum/6qj5 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6qj5 ProSAT]</span></td></tr>
</table>
</table>
== Disease ==
== Disease ==
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== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/PPARG_HUMAN PPARG_HUMAN]] Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated proinflammatory responses.<ref>PMID:9065481</ref> <ref>PMID:16150867</ref> <ref>PMID:20829347</ref>
[[http://www.uniprot.org/uniprot/PPARG_HUMAN PPARG_HUMAN]] Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated proinflammatory responses.<ref>PMID:9065481</ref> <ref>PMID:16150867</ref> <ref>PMID:20829347</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A proprietary library of novel N-aryl-substituted amino acid derivatives bearing a hydroxamate head group allowed the identification of compound 3a that possesses weak proadipogenic and peroxisome proliferator-activated receptor gamma (PPARgamma) activating properties. The systematic optimization of 3a, in order to improve its PPARgamma agonist activity, led to the synthesis of compound 7j (N-aryl-substituted valine derivative) that possesses dual PPARgamma/PPARalpha agonistic activity. Structural and kinetic analyses reveal that 7j occupies the typical ligand binding domain of the PPARgamma agonists with, however, a unique high-affinity binding mode. Furthermore, 7j is highly effective in preventing cyclin-dependent kinase 5-mediated phosphorylation of PPARgamma serine 273. Although less proadipogenic than rosiglitazone, 7j significantly increases adipocyte insulin-stimulated glucose uptake and efficiently promotes white-to-brown adipocyte conversion. In addition, 7j prevents oleic acid-induced lipid accumulation in hepatoma cells. The unique biochemical properties and biological activities of compound 7j suggest that it would be a promising candidate for the development of compounds to reduce insulin resistance, obesity, and nonalcoholic fatty liver disease.
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A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor gamma Binding Properties and Biological Activities.,Peiretti F, Montanari R, Capelli D, Bonardo B, Colson C, Amri EZ, Grimaldi M, Balaguer P, Ito K, Roeder RG, Pochetti G, Brunel JM J Med Chem. 2020 Nov 12;63(21):13124-13139. doi: 10.1021/acs.jmedchem.0c01555., Epub 2020 Nov 3. PMID:33142057<ref>PMID:33142057</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 6qj5" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Capelli, D]]
[[Category: Capelli, D]]

Revision as of 07:06, 25 November 2020

X-ray structure of PPARgamma LBD with the ligand NV1380

PDB ID 6qj5

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