3peq: Difference between revisions
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[[ | ==PPARd complexed with a phenoxyacetic acid partial agonist== | ||
<StructureSection load='3peq' size='340' side='right' caption='[[3peq]], [[Resolution|resolution]] 2.40Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[3peq]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PEQ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PEQ FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3EQ:[(4-{BUTYL[2-METHYL-4-(METHYLSULFANYL)BIPHENYL-3-YL]SULFAMOYL}NAPHTHALEN-1-YL)OXY]ACETIC+ACID'>3EQ</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene>, <scene name='pdbligand=JZR:HEXYL+BETA-D-GLUCOPYRANOSIDE'>JZR</scene></td></tr> | |||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">NR1C2, PPARB, PPARD ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3peq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3peq OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3peq RCSB], [http://www.ebi.ac.uk/pdbsum/3peq PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
A series of phenoxyacetic acids as subtype selective and potent hPPARdelta partial agonists is described. Many analogues were readily accessible via a single solution-phase synthetic route which resulted in the rapid identification of key structure-activity relationships (SAR), and the discovery of two potent exemplars which were further evaluated in vivo. Details of the SAR, optimization, and in vivo efficacy of this series are presented herein. | |||
Phenoxyacetic acids as PPARdelta partial agonists: synthesis, optimization, and in vivo efficacy.,Evans KA, Shearer BG, Wisnoski DD, Shi D, Sparks SM, Sternbach DD, Winegar DA, Billin AN, Britt C, Way JM, Epperly AH, Leesnitzer LM, Merrihew RV, Xu RX, Lambert MH, Jin J Bioorg Med Chem Lett. 2011 Apr 15;21(8):2345-50. Epub 2011 Mar 15. PMID:21414782<ref>PMID:21414782</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
==See Also== | ==See Also== | ||
*[[Peroxisome Proliferator-Activated Receptors|Peroxisome Proliferator-Activated Receptors]] | *[[Peroxisome Proliferator-Activated Receptors|Peroxisome Proliferator-Activated Receptors]] | ||
== References == | |||
== | <references/> | ||
< | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: Human]] | |||
[[Category: Billin, A N.]] | [[Category: Billin, A N.]] | ||
[[Category: Britt, C.]] | [[Category: Britt, C.]] | ||
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[[Category: Way, J M.]] | [[Category: Way, J M.]] | ||
[[Category: Winegar, D A.]] | [[Category: Winegar, D A.]] | ||
[[Category: Wisnoski, D D]] | [[Category: Wisnoski, D D.]] | ||
[[Category: Ppar nuclear receptor]] | [[Category: Ppar nuclear receptor]] | ||
[[Category: Transcription-transcription agonist complex]] | [[Category: Transcription-transcription agonist complex]] |