3ttz
From Proteopedia
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| - | [[ | + | ==Crystal structure of a topoisomerase ATPase inhibitor== |
| + | <StructureSection load='3ttz' size='340' side='right' caption='[[3ttz]], [[Resolution|resolution]] 1.63Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3ttz]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3TTZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3TTZ FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=07N:2-[(3S,4R)-4-{[(3,4-DICHLORO-5-METHYL-1H-PYRROL-2-YL)CARBONYL]AMINO}-3-FLUOROPIPERIDIN-1-YL]-1,3-THIAZOLE-5-CARBOXYLIC+ACID'>07N</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3u2d|3u2d]], [[3u2k|3u2k]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">gyrB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=1280 Staphylococcus aureus])</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/DNA_topoisomerase_(ATP-hydrolyzing) DNA topoisomerase (ATP-hydrolyzing)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=5.99.1.3 5.99.1.3] </span></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=3ttz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ttz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ttz RCSB], [http://www.ebi.ac.uk/pdbsum/3ttz PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The pyrrolamides are a new class of antibacterial agents targeting DNA gyrase, an essential enzyme across bacterial species and inhibition results in the disruption of DNA synthesis and subsequently, cell death. The optimization of biochemical activity and other drug-like properties through substitutions to the pyrrole, piperidine, and heterocycle portions of the molecule resulted in pyrrolamides with improved cellular activity and in vivo efficacy. | ||
| - | + | Pyrrolamide DNA gyrase inhibitors: Optimization of antibacterial activity and efficacy.,Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT 3rd, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, Degrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE Bioorg Med Chem Lett. 2011 Oct 12. PMID:22041057<ref>PMID:22041057</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
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==See Also== | ==See Also== | ||
*[[Gyrase|Gyrase]] | *[[Gyrase|Gyrase]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Staphylococcus aureus]] | [[Category: Staphylococcus aureus]] | ||
| - | [[Category: Boriack-Sjodin, P A | + | [[Category: Boriack-Sjodin, P A]] |
| - | [[Category: Eakin, A E | + | [[Category: Eakin, A E]] |
| - | [[Category: Read, J | + | [[Category: Read, J]] |
| - | [[Category: Sherer, B A | + | [[Category: Sherer, B A]] |
[[Category: Antimicrobial]] | [[Category: Antimicrobial]] | ||
[[Category: Atp-binding]] | [[Category: Atp-binding]] | ||
Revision as of 17:36, 9 December 2014
Crystal structure of a topoisomerase ATPase inhibitor
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