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3ow6
From Proteopedia
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| - | [[ | + | ==Crystal Structure of HSP90 with N-Aryl-benzimidazolone I== |
| + | <StructureSection load='3ow6' size='340' side='right' caption='[[3ow6]], [[Resolution|resolution]] 1.80Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3ow6]] is a 1 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=3OW6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3OW6 FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MEX:1-(2,4-DIHYDROXYPHENYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE'>MEX</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3owb|3owb]], [[3owd|3owd]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">HSP90AA1, HSP90A, HSPC1, HSPCA ([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=3ow6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ow6 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ow6 RCSB], [http://www.ebi.ac.uk/pdbsum/3ow6 PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | We describe the development of a novel series of N-aryl-benzimidazolone HSP90 inhibitors (9) targeting the N-terminal ATP-ase site. SAR development was influenced by structure-based design based around X-ray structures of ligand bound HSP90 complexes. Lead compounds exhibited high binding affinities, ATP-ase inhibition and cellular client protein degradation. | ||
| - | + | N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.,Bruncko M, Tahir SK, Song X, Chen J, Ding H, Huth JR, Jin S, Judge RA, Madar DJ, Park CH, Park CM, Petros AM, Tse C, Rosenberg SH, Elmore SW Bioorg Med Chem Lett. 2010 Dec 15;20(24):7503-6. Epub 2010 Oct 12. PMID:21106457<ref>PMID:21106457</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
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==See Also== | ==See Also== | ||
*[[Heat Shock Proteins|Heat Shock Proteins]] | *[[Heat Shock Proteins|Heat Shock Proteins]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: Park, C H | + | [[Category: Park, C H]] |
[[Category: Chaperone]] | [[Category: Chaperone]] | ||
[[Category: Hsp90]] | [[Category: Hsp90]] | ||
Revision as of 12:24, 9 December 2014
Crystal Structure of HSP90 with N-Aryl-benzimidazolone I
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