3oz0: Difference between revisions
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==PPAR Delta in complex with azppard02== | ==PPAR Delta in complex with azppard02== | ||
<StructureSection load='3oz0' size='340' side='right' caption='[[3oz0]], [[Resolution|resolution]] 3.00Å' scene=''> | <StructureSection load='3oz0' size='340' side='right' caption='[[3oz0]], [[Resolution|resolution]] 3.00Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[3oz0]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/ | <table><tr><td colspan='2'>[[3oz0]] is a 1 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=3OZ0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3OZ0 FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3OZ:[4-({(1S)-1-[(2,4-DICHLOROPHENYL)CARBAMOYL]-1,3-DIHYDRO-2H-ISOINDOL-2-YL}METHYL)-2-METHYLPHENOXY]ACETIC+ACID'>3OZ</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3OZ:[4-({(1S)-1-[(2,4-DICHLOROPHENYL)CARBAMOYL]-1,3-DIHYDRO-2H-ISOINDOL-2-YL}METHYL)-2-METHYLPHENOXY]ACETIC+ACID'>3OZ</scene></td></tr> | ||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PPARD, NR1C2, PPARB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PPARD, NR1C2, PPARB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3oz0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3oz0 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3oz0 RCSB], [http://www.ebi.ac.uk/pdbsum/3oz0 PDBsum]</span></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=3oz0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3oz0 OCA], [http://pdbe.org/3oz0 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3oz0 RCSB], [http://www.ebi.ac.uk/pdbsum/3oz0 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3oz0 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 3oz0" style="background-color:#fffaf0;"></div> | |||
==See Also== | ==See Also== | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Human]] | ||
[[Category: Ogg, D]] | [[Category: Ogg, D]] | ||
[[Category: Nuclear receptor fold]] | [[Category: Nuclear receptor fold]] | ||
Revision as of 11:09, 5 August 2016
PPAR Delta in complex with azppard02PPAR Delta in complex with azppard02
Structural highlights
Function[PPARD_HUMAN] Ligand-activated transcription factor. Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Has a preference for poly-unsaturated fatty acids, such as gamma-linoleic acid and eicosapentanoic acid. Once activated by a ligand, the receptor binds to promoter elements of target genes. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the acyl-CoA oxidase gene. Decreases expression of NPC1L1 once activated by a ligand.[1] [2] Publication Abstract from PubMedSmall molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor delta (PPARdelta. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation, with upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) in human primary myotubes. Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARdelta agonists.,Luckhurst CA, Stein LA, Furber M, Webb N, Ratcliffe MJ, Allenby G, Botterell S, Tomlinson W, Martin B, Walding A Bioorg Med Chem Lett. 2011 Jan 1;21(1):492-6. Epub 2010 Oct 27. PMID:21094606[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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