3gz9

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Current revision (09:57, 21 February 2024) (edit) (undo)
 
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<StructureSection load='3gz9' size='340' side='right'caption='[[3gz9]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
<StructureSection load='3gz9' size='340' side='right'caption='[[3gz9]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3gz9]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3GZ9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3GZ9 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3gz9]] 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=3GZ9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3GZ9 FirstGlance]. <br>
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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=B7G:HEPTYL-BETA-D-GLUCOPYRANOSIDE'>B7G</scene>, <scene name='pdbligand=D32:(2,3-DIMETHYL-4-{[2-(PROP-2-YN-1-YLOXY)-4-{[4-(TRIFLUOROMETHYL)PHENOXY]METHYL}PHENYL]SULFANYL}PHENOXY)ACETIC+ACID'>D32</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]] 2&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PPARD, NR1C2, PPARB ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=B7G:HEPTYL-BETA-D-GLUCOPYRANOSIDE'>B7G</scene>, <scene name='pdbligand=D32:(2,3-DIMETHYL-4-{[2-(PROP-2-YN-1-YLOXY)-4-{[4-(TRIFLUOROMETHYL)PHENOXY]METHYL}PHENYL]SULFANYL}PHENOXY)ACETIC+ACID'>D32</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=3gz9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3gz9 OCA], [https://pdbe.org/3gz9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3gz9 RCSB], [https://www.ebi.ac.uk/pdbsum/3gz9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3gz9 ProSAT]</span></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=3gz9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3gz9 OCA], [https://pdbe.org/3gz9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3gz9 RCSB], [https://www.ebi.ac.uk/pdbsum/3gz9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3gz9 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[https://www.uniprot.org/uniprot/PPARD_HUMAN 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.<ref>PMID:1333051</ref> <ref>PMID:15604518</ref>
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[https://www.uniprot.org/uniprot/PPARD_HUMAN 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.<ref>PMID:1333051</ref> <ref>PMID:15604518</ref>
== Evolutionary Conservation ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3gz9 ConSurf].
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3gz9 ConSurf].
<div style="clear:both"></div>
<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
 
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== Publication Abstract from PubMed ==
 
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The discovery and optimization of a series of potent PPARdelta full agonists with partial agonistic activity against PPARgamma is described.
 
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Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.,Connors RV, Wang Z, Harrison M, Zhang A, Wanska M, Hiscock S, Fox B, Dore M, Labelle M, Sudom A, Johnstone S, Liu J, Walker NP, Chai A, Siegler K, Li Y, Coward P Bioorg Med Chem Lett. 2009 Jul 1;19(13):3550-4. Epub 2009 May 9. PMID:19464171<ref>PMID:19464171</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 3gz9" style="background-color:#fffaf0;"></div>
 
==See Also==
==See Also==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Sudom, A]]
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[[Category: Sudom A]]
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[[Category: Walker, N P]]
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[[Category: Walker NP]]
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[[Category: Wang, Z]]
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[[Category: Wang Z]]
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[[Category: Activator]]
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[[Category: Alternative splicing]]
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[[Category: Complex]]
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[[Category: Dna-binding]]
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[[Category: Growth factor receptor]]
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[[Category: Hormone]]
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[[Category: Metal-binding]]
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[[Category: Nuclear receptor fold]]
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[[Category: Nucleus]]
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[[Category: Ppar]]
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[[Category: Ppar delta]]
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[[Category: Receptor]]
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[[Category: Transcription]]
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[[Category: Transcription regulation]]
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[[Category: Zinc]]
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[[Category: Zinc-finger]]
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Current revision

Crystal Structure of Peroxisome Proliferator-Activated Receptor Delta (PPARd) in Complex with a Full Agonist

PDB ID 3gz9

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