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3fej

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{{Seed}}
 
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[[Image:3fej.jpg|left|200px]]
 
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==Design and biological evaluation of novel, balanced dual PPARa/g agonists==
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The line below this paragraph, containing "STRUCTURE_3fej", creates the "Structure Box" on the page.
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<StructureSection load='3fej' size='340' side='right'caption='[[3fej]], [[Resolution|resolution]] 2.01&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3fej]] 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=3FEJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FEJ FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 2.01&#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=CTM:(2S)-3-(4-{[2-(4-CHLOROPHENYL)-1,3-THIAZOL-4-YL]METHOXY}-2-METHYLPHENYL)-2-ETHOXYPROPANOIC+ACID'>CTM</scene></td></tr>
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{{STRUCTURE_3fej| PDB=3fej | SCENE= }}
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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=3fej FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fej OCA], [https://pdbe.org/3fej PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3fej RCSB], [https://www.ebi.ac.uk/pdbsum/3fej PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3fej ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/PPARG_HUMAN PPARG_HUMAN] Note=Defects in PPARG can lead to type 2 insulin-resistant diabetes and hyptertension. PPARG mutations may be associated with colon cancer. Defects in PPARG may be associated with susceptibility to obesity (OBESITY) [MIM:[https://omim.org/entry/601665 601665]. It is a condition characterized by an increase of body weight beyond the limitation of skeletal and physical requirements, as the result of excessive accumulation of body fat.<ref>PMID:9753710</ref> Defects in PPARG are the cause of familial partial lipodystrophy type 3 (FPLD3) [MIM:[https://omim.org/entry/604367 604367]. Familial partial lipodystrophies (FPLD) are a heterogeneous group of genetic disorders characterized by marked loss of subcutaneous (sc) fat from the extremities. Affected individuals show an increased preponderance of insulin resistance, diabetes mellitus and dyslipidemia.<ref>PMID:12453919</ref> <ref>PMID:11788685</ref> Genetic variations in PPARG can be associated with susceptibility to glioma type 1 (GLM1) [MIM:[https://omim.org/entry/137800 137800]. Gliomas are central nervous system neoplasms derived from glial cells and comprise astrocytomas, glioblastoma multiforme, oligodendrogliomas, and ependymomas. Note=Polymorphic PPARG alleles have been found to be significantly over-represented among a cohort of American patients with sporadic glioblastoma multiforme suggesting a possible contribution to disease susceptibility.
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== Function ==
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[https://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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== 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/fe/3fej_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=3fej 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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An X-ray-guided design approach led to the identification of a novel, balanced class of alpha-ethoxy-phenylpropionic acid-derived dual PPARalpha/gamma agonists. The series shows a wide range of PPARalpha/gamma ratios within a rather narrow structural space. Advanced compounds possess favorable physicochemical and pharmacokinetic profiles and show a high efficacy in T2D and dyslipidemia animal models.
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===Design and biological evaluation of novel, balanced dual PPARa/g agonists===
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Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists.,Grether U, Benardeau A, Benz J, Binggeli A, Blum D, Hilpert H, Kuhn B, Marki HP, Meyer M, Mohr P, Puntener K, Raab S, Ruf A, Schlatter D ChemMedChem. 2009 Jun;4(6):951-6. PMID:19326383<ref>PMID:19326383</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 3fej" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_19326383}}, adds the Publication Abstract to the page
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*[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 19326383 is the PubMed ID number.
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== References ==
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-->
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<references/>
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{{ABSTRACT_PUBMED_19326383}}
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__TOC__
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</StructureSection>
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==About this Structure==
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3FEJ is a 2 chains structure of sequences 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=3FEJ OCA].
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==Reference==
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<ref group="xtra">PMID:19326383</ref><references group="xtra"/>
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[[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: Binggeli, A.]]
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[[Category: Benz J]]
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[[Category: Grether, U.]]
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[[Category: Binggeli A]]
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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: Mohr, P.]]
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[[Category: Maerki HP]]
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[[Category: Ruf, A.]]
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[[Category: Mohr P]]
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[[Category: Stihle, M.]]
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[[Category: Ruf A]]
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[[Category: Activator]]
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[[Category: Stihle M]]
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[[Category: Alternative splicing]]
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[[Category: Diabetes]]
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[[Category: Diabetes mellitus]]
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[[Category: Disease mutation]]
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[[Category: Dna-binding]]
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[[Category: Metal-binding]]
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[[Category: Nuclear recpetor]]
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[[Category: Nucleus]]
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[[Category: Obesity]]
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[[Category: Phosphoprotein]]
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[[Category: Polymorphism]]
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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: Zinc]]
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[[Category: Zinc-finger]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Oct 21 10:21:39 2009''
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Current revision

Design and biological evaluation of novel, balanced dual PPARa/g agonists

PDB ID 3fej

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