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5azt
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 5azt is ON HOLD Authors: Egawa, D., Itoh, T., Yamamoto, K. Description: Ternary complex of hPPARalpha ligand binding domain, 17-oxoDHA and a SRC1 p...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Ternary complex of hPPARalpha ligand binding domain, 17-oxoDHA and a SRC1 peptide== | |
| + | <StructureSection load='5azt' size='340' side='right'caption='[[5azt]], [[Resolution|resolution]] 3.45Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5azt]] is a 3 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=5AZT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AZT FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=4M5:(4~{Z},7~{Z},10~{Z},13~{Z},19~{Z})-17-OXIDANYLIDENEDOCOSA-4,7,10,13,19-PENTAENOIC+ACID'>4M5</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=5azt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5azt OCA], [https://pdbe.org/5azt PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5azt RCSB], [https://www.ebi.ac.uk/pdbsum/5azt PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5azt ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/PPARA_HUMAN PPARA_HUMAN] Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety (By similarity). Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2.<ref>PMID:7684926</ref> <ref>PMID:7629123</ref> <ref>PMID:9556573</ref> <ref>PMID:10195690</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 17-Hydroxy docosahexaenoic acid (17-HDHA) is an oxidized form of docosahexaenoic acid (DHA) and known as a specialized proresolving mediator. We found that a further oxidized product, 17-oxodocosahexaenoic acid (17-oxoDHA), activates peroxisome proliferator-activated receptors gamma (PPARgamma) and PPARalpha in transcriptional assays and thus can be classified as an alpha/gamma dual agonist. ESI mass spectroscopy and X-ray crystallographic analysis showed that 17-oxoDHA binds to PPARgamma and PPARalpha covalently, making 17-oxoDHA the first of a novel class of PPAR agonists, the PPARalpha/gamma dual covalent agonist. Furthermore, the covalent binding sites were identified as Cys285 for PPARgamma and Cys275 for PPARalpha. | ||
| - | + | 17-OxoDHA Is a PPARalpha/gamma Dual Covalent Modifier and Agonist.,Egawa D, Itoh T, Akiyama Y, Saito T, Yamamoto K ACS Chem Biol. 2016 Jul 1. PMID:27337155<ref>PMID:27337155</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: Egawa | + | <div class="pdbe-citations 5azt" style="background-color:#fffaf0;"></div> |
| - | [[Category: | + | |
| - | [[Category: | + | ==See Also== |
| + | *[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Egawa D]] | ||
| + | [[Category: Itoh T]] | ||
| + | [[Category: Yamamoto K]] | ||
Current revision
Ternary complex of hPPARalpha ligand binding domain, 17-oxoDHA and a SRC1 peptide
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