4eo8
From Proteopedia
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| - | [[ | + | ==HCV NS5B polymerase inhibitors: Tri-substituted acylhydrazines as tertiary amide bioisosteres== |
| + | <StructureSection load='4eo8' size='340' side='right' caption='[[4eo8]], [[Resolution|resolution]] 1.80Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4eo8]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Viruses Viruses]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EO8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4EO8 FirstGlance]. <br> | ||
| + | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0S3:5-(3,3-DIMETHYLBUT-1-YN-1-YL)-3-{2,2-DIMETHYL-1-[(TRANS-4-METHYLCYCLOHEXYL)CARBONYL]HYDRAZINYL}THIOPHENE-2-CARBOXYLIC+ACID'>0S3</scene><br> | ||
| + | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4eo6|4eo6]]</td></tr> | ||
| + | <tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">NS5B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10239 Viruses])</td></tr> | ||
| + | <tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/RNA-directed_RNA_polymerase RNA-directed RNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.48 2.7.7.48] </span></td></tr> | ||
| + | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4eo8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4eo8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4eo8 RCSB], [http://www.ebi.ac.uk/pdbsum/4eo8 PDBsum]</span></td></tr> | ||
| + | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The use of a tri-substituted acylhydrazine as an isostere of a tertiary amide was explored in a series of HCV NS5B thumb site II inhibitors. Direct replacement generated an analog with similar conformational and physicochemical properties. The series was extended to produce compounds with potent binding affinities and encouraging levels of cellular potency. | ||
| - | + | Tri-substituted acylhydrazines as tertiary amide bioisosteres: HCV NS5B polymerase inhibitors.,Canales E, Carlson JS, Appleby T, Fenaux M, Lee J, Tian Y, Tirunagari N, Wong M, Watkins WJ Bioorg Med Chem Lett. 2012 Jul 1;22(13):4288-92. Epub 2012 May 17. PMID:22664130<ref>PMID:22664130</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| - | + | ==See Also== | |
| - | + | *[[RNA polymerase|RNA polymerase]] | |
| - | == | + | == References == |
| - | [[ | + | <references/> |
| - | + | __TOC__ | |
| - | == | + | </StructureSection> |
| - | < | + | |
[[Category: RNA-directed RNA polymerase]] | [[Category: RNA-directed RNA polymerase]] | ||
[[Category: Viruses]] | [[Category: Viruses]] | ||
Revision as of 07:46, 5 June 2014
HCV NS5B polymerase inhibitors: Tri-substituted acylhydrazines as tertiary amide bioisosteres
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