5a5z: Difference between revisions
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''' | ==Approved Drugs Containing Thiols as Inhibitors of Metallo-beta- lactamases: Strategy To Combat Multidrug-Resistant Bacteria== | ||
<StructureSection load='5a5z' size='340' side='right' caption='[[5a5z]], [[Resolution|resolution]] 2.60Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5a5z]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5A5Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5A5Z FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=WJZ:TIOPRONIN'>WJZ</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | |||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Beta-lactamase Beta-lactamase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.2.6 3.5.2.6] </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=5a5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5a5z OCA], [http://www.rcsb.org/pdb/explore.do?structureId=5a5z RCSB], [http://www.ebi.ac.uk/pdbsum/5a5z PDBsum]</span></td></tr> | |||
</table> | |||
== Function == | |||
[[http://www.uniprot.org/uniprot/BLAN1_KLEPN BLAN1_KLEPN]] Confers resistance to many beta-lactam antibiotics, including some carbapenems. Does not confer resistance to the polymixin colistin or the fluoroquinolone ciprofloxacin. | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Resistance to beta-lactam antibiotics can be mediated by metallo-beta-lactamase enzymes (MBLs). An MBL inhibitor could restore the effectiveness of beta-lactams. We report on the evaluation of approved thiol-containing drugs as inhibitors of NDM-1, VIM-1, and IMP-7. Drugs were assessed by a novel assay using a purchasable fluorescent substrate and thermal shift. Best compounds were tested in antimicrobial susceptibility assay. Using these orthogonal screening methods, we identified drugs that restored the activity of imipenem. | |||
Approved Drugs Containing Thiols as Inhibitors of Metallo-beta-lactamases: Strategy To Combat Multidrug-Resistant Bacteria.,Klingler FM, Wichelhaus TA, Frank D, Cuesta-Bernal J, El-Delik J, Muller HF, Sjuts H, Gottig S, Koenigs A, Pos KM, Pogoryelov D, Proschak E J Med Chem. 2015 Apr 23;58(8):3626-30. doi: 10.1021/jm501844d. Epub 2015 Apr 13. PMID:25815530<ref>PMID:25815530</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
== References == | |||
<references/> | |||
[[Category: | __TOC__ | ||
</StructureSection> | |||
[[Category: Beta-lactamase]] | |||
[[Category: Cuesta-Bernal, J]] | [[Category: Cuesta-Bernal, J]] | ||
[[Category: El-Delik, J]] | |||
[[Category: Frank, D]] | |||
[[Category: Goettig, S]] | |||
[[Category: Klingler, F M]] | |||
[[Category: Koenigs, A]] | [[Category: Koenigs, A]] | ||
[[Category: Mueller, H F]] | |||
[[Category: Pogoryelov, D]] | [[Category: Pogoryelov, D]] | ||
[[Category: | [[Category: Proschak, E]] | ||
[[Category: Sjuts, H]] | [[Category: Sjuts, H]] | ||
[[Category: | [[Category: Wichelhaus, T A]] | ||
[[Category: | [[Category: Hydrolase]] | ||
[[Category: | [[Category: Metallo-beta-lactamase]] | ||
[[Category: | [[Category: Ndm-1]] | ||
[[Category: New delhi metallo- beta-lactamase 1]] | |||
[[Category: Tiopronin]] | |||
Revision as of 14:43, 8 July 2015
Approved Drugs Containing Thiols as Inhibitors of Metallo-beta- lactamases: Strategy To Combat Multidrug-Resistant Bacteria
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