3gt9
From Proteopedia
(Difference between revisions)
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| - | [[ | + | ==Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic== |
| + | <StructureSection load='3gt9' size='340' side='right' caption='[[3gt9]], [[Resolution|resolution]] 1.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3gt9]] is a 2 chain structure 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=3GT9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3GT9 FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=516:N-{(1S)-1-CYCLOHEXYL-2-[(2S)-2-(4-NAPHTHALEN-1-YL-1,3-THIAZOL-2-YL)PYRROLIDIN-1-YL]-2-OXOETHYL}-N~2~-METHYL-L-ALANINAMIDE'>516</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3f7h|3f7h]], [[3f7i|3f7i]], [[3f7g|3f7g]], [[2i3h|2i3h]], [[2i3i|2i3i]], [[1tw6|1tw6]], [[3gta|3gta]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BIRC7 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=3gt9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3gt9 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3gt9 RCSB], [http://www.ebi.ac.uk/pdbsum/3gt9 PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Evolutionary Conservation == | ||
| + | [[Image:Consurf_key_small.gif|200px|right]] | ||
| + | Check<jmol> | ||
| + | <jmolCheckbox> | ||
| + | <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/gt/3gt9_consurf.spt"</scriptWhenChecked> | ||
| + | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
| + | <text>to colour the structure by Evolutionary Conservation</text> | ||
| + | </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/chain_selection.php?pdb_ID=2ata ConSurf]. | ||
| + | <div style="clear:both"></div> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compounds, 19a and 33b, were found to have K(i)'s of 20-30 nM against ML-IAP and 50-60 nM against XIAP-BIR3. | ||
| - | + | Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.,Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ Bioorg Med Chem Lett. 2010 Apr 1;20(7):2229-33. Epub 2010 Feb 8. PMID:20189383<ref>PMID:20189383</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| - | + | <references/> | |
| - | + | __TOC__ | |
| - | + | </StructureSection> | |
| - | + | ||
| - | == | + | |
| - | < | + | |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: Cohen, F | + | [[Category: Cohen, F]] |
| - | [[Category: Fairbrother, W J | + | [[Category: Fairbrother, W J]] |
| - | [[Category: Franklin, M C | + | [[Category: Franklin, M C]] |
[[Category: Apoptosis]] | [[Category: Apoptosis]] | ||
[[Category: Apoptosis inhibition]] | [[Category: Apoptosis inhibition]] | ||
Revision as of 09:12, 8 December 2014
Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic
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