3g8i

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[[Image:3g8i.png|left|200px]]
 
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{{STRUCTURE_3g8i| PDB=3g8i | SCENE= }}
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==Aleglitazar, a new, potent, and balanced PPAR alpha/gamma agonist for the treatment of type II diabetes==
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<StructureSection load='3g8i' size='340' side='right'caption='[[3g8i]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3g8i]] is a 2 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=3G8I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3G8I FirstGlance]. <br>
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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]] 2.2&#8491;</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=RO7:(2S)-2-METHOXY-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]-1-BENZOTHIOPHEN-7-YL}PROPANOIC+ACID'>RO7</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=3g8i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3g8i OCA], [https://pdbe.org/3g8i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3g8i RCSB], [https://www.ebi.ac.uk/pdbsum/3g8i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3g8i ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/g8/3g8i_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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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=3g8i ConSurf].
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<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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Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPARalphagamma coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.
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===Aleglitazar, a new, potent, and balanced PPAR alpha/gamma agonist for the treatment of type II diabetes===
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Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.,Benardeau A, Benz J, Binggeli A, Blum D, Boehringer M, Grether U, Hilpert H, Kuhn B, Marki HP, Meyer M, Puntener K, Raab S, Ruf A, Schlatter D, Mohr P Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73. Epub 2009 Mar 14. PMID:19349176<ref>PMID:19349176</ref>
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{{ABSTRACT_PUBMED_19349176}}
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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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==About this Structure==
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<div class="pdbe-citations 3g8i" style="background-color:#fffaf0;"></div>
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[[3g8i]] is a 2 chain structure of [[Peroxisome Proliferator-Activated Receptors]] with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3G8I OCA].
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==See Also==
==See Also==
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*[[Peroxisome Proliferator-Activated Receptors|Peroxisome Proliferator-Activated Receptors]]
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*[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:019349176</ref><references group="xtra"/>
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__TOC__
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[[Category: Histone acetyltransferase]]
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Benz, J.]]
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[[Category: Large Structures]]
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[[Category: Bernardeau, A.]]
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[[Category: Benz J]]
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[[Category: Binggeli, A.]]
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[[Category: Bernardeau A]]
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[[Category: Blum, D.]]
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[[Category: Binggeli A]]
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[[Category: Boehringer, M.]]
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[[Category: Blum D]]
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[[Category: Grether, U.]]
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[[Category: Boehringer M]]
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[[Category: Gsell, B.]]
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[[Category: Grether U]]
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[[Category: Hilpert, H.]]
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[[Category: Gsell B]]
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[[Category: Kuhn, B.]]
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[[Category: Hilpert H]]
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[[Category: Maerki, H P.]]
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[[Category: Kuhn B]]
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[[Category: Meyer, M.]]
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[[Category: Maerki HP]]
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[[Category: Mohr, P.]]
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[[Category: Meyer M]]
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[[Category: Puentener, K.]]
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[[Category: Mohr P]]
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[[Category: Raab, S.]]
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[[Category: Puentener K]]
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[[Category: Ruf, A.]]
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[[Category: Raab S]]
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[[Category: Schlatter, D.]]
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[[Category: Ruf A]]
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[[Category: Stihle, M.]]
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[[Category: Schlatter D]]
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[[Category: Activator]]
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[[Category: Stihle M]]
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[[Category: Acyltransferase]]
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[[Category: Diabetes]]
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[[Category: Dna-binding]]
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[[Category: Metal-binding]]
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[[Category: Nuclear hormone receptor]]
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[[Category: Nucleus]]
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[[Category: Phosphoprotein]]
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[[Category: Proto-oncogene]]
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[[Category: Receptor]]
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[[Category: Transcription]]
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[[Category: Transcription factor]]
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[[Category: Transcription regulation]]
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[[Category: Transcription-transferase complex]]
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[[Category: Transferase]]
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[[Category: Zinc-finger]]
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Current revision

Aleglitazar, a new, potent, and balanced PPAR alpha/gamma agonist for the treatment of type II diabetes

PDB ID 3g8i

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