3g8i
From Proteopedia
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==Aleglitazar, a new, potent, and balanced PPAR alpha/gamma agonist for the treatment of type II diabetes== | ==Aleglitazar, a new, potent, and balanced PPAR alpha/gamma agonist for the treatment of type II diabetes== | ||
- | <StructureSection load='3g8i' size='340' side='right' caption='[[3g8i]], [[Resolution|resolution]] 2.20Å' scene=''> | + | <StructureSection load='3g8i' size='340' side='right'caption='[[3g8i]], [[Resolution|resolution]] 2.20Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
- | <table><tr><td colspan='2'>[[3g8i]] is a 2 chain structure with sequence from [ | + | <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> |
- | </td></tr><tr id=' | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.2Å</td></tr> |
- | + | <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> | |
- | <tr id=' | + | <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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- | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
- | == Disease == | ||
- | [[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children. | ||
== Function == | == 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> |
== Evolutionary Conservation == | == Evolutionary Conservation == | ||
[[Image:Consurf_key_small.gif|200px|right]] | [[Image:Consurf_key_small.gif|200px|right]] | ||
Check<jmol> | Check<jmol> | ||
<jmolCheckbox> | <jmolCheckbox> | ||
- | <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/g8/3g8i_consurf.spt"</scriptWhenChecked> | + | <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/g8/3g8i_consurf.spt"</scriptWhenChecked> |
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
<text>to colour the structure by Evolutionary Conservation</text> | <text>to colour the structure by Evolutionary Conservation</text> | ||
</jmolCheckbox> | </jmolCheckbox> | ||
- | </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/ | + | </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]. |
<div style="clear:both"></div> | <div style="clear:both"></div> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
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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 3g8i" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
- | *[[Peroxisome | + | *[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]] |
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
- | [[Category: Histone acetyltransferase]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
- | [[Category: Benz | + | [[Category: Large Structures]] |
- | [[Category: Bernardeau | + | [[Category: Benz J]] |
- | [[Category: Binggeli | + | [[Category: Bernardeau A]] |
- | [[Category: Blum | + | [[Category: Binggeli A]] |
- | [[Category: Boehringer | + | [[Category: Blum D]] |
- | [[Category: Grether | + | [[Category: Boehringer M]] |
- | [[Category: Gsell | + | [[Category: Grether U]] |
- | [[Category: Hilpert | + | [[Category: Gsell B]] |
- | [[Category: Kuhn | + | [[Category: Hilpert H]] |
- | [[Category: Maerki | + | [[Category: Kuhn B]] |
- | [[Category: Meyer | + | [[Category: Maerki HP]] |
- | [[Category: Mohr | + | [[Category: Meyer M]] |
- | [[Category: Puentener | + | [[Category: Mohr P]] |
- | [[Category: Raab | + | [[Category: Puentener K]] |
- | [[Category: Ruf | + | [[Category: Raab S]] |
- | [[Category: Schlatter | + | [[Category: Ruf A]] |
- | [[Category: Stihle | + | [[Category: Schlatter D]] |
- | + | [[Category: Stihle M]] | |
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Current revision
Aleglitazar, a new, potent, and balanced PPAR alpha/gamma agonist for the treatment of type II diabetes
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Categories: Homo sapiens | Large Structures | Benz J | Bernardeau A | Binggeli A | Blum D | Boehringer M | Grether U | Gsell B | Hilpert H | Kuhn B | Maerki HP | Meyer M | Mohr P | Puentener K | Raab S | Ruf A | Schlatter D | Stihle M