5a5z: Difference between revisions

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New page: '''Unreleased structure''' The entry 5a5z is ON HOLD Authors: Klingler, F.M., Wichelhaus, T.A., Frank, D., Cuesta-Bernal, J., El-Delik, J., Mueller, H.F., Sjuts, H., Goettig, S., Koenig...
 
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'''Unreleased structure'''


The entry 5a5z is ON HOLD
==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]] 2.60&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5a5z]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Klebsiella_pneumoniae Klebsiella pneumoniae]. 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 [https://proteopedia.org/fgij/fg.htm?mol=5A5Z FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.6&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=WJZ:TIOPRONIN'>WJZ</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5a5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5a5z OCA], [https://pdbe.org/5a5z PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5a5z RCSB], [https://www.ebi.ac.uk/pdbsum/5a5z PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5a5z ProSAT]</span></td></tr>
</table>
== Function ==
[https://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.


Authors: Klingler, F.M., Wichelhaus, T.A., Frank, D., Cuesta-Bernal, J., El-Delik, J., Mueller, H.F., Sjuts, H., Goettig, S., Koenigs, A., Pogoryelov, D., Proschak, E.
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>


Description: Approved Drugs Containing Thiols as Inhibitors of Metallo-beta-lactamases: Strategy To Combat Multidrug-Resistant Bacteria
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[Category: Unreleased Structures]]
</div>
[[Category: Proschak, E]]
<div class="pdbe-citations 5a5z" style="background-color:#fffaf0;"></div>
[[Category: Cuesta-Bernal, J]]
 
[[Category: Koenigs, A]]
==See Also==
[[Category: Pogoryelov, D]]
*[[Beta-lactamase 3D structures|Beta-lactamase 3D structures]]
[[Category: Klingler, F.M]]
== References ==
[[Category: Goettig, S]]
<references/>
[[Category: Sjuts, H]]
__TOC__
[[Category: Frank, D]]
</StructureSection>
[[Category: El-Delik, J]]
[[Category: Klebsiella pneumoniae]]
[[Category: Mueller, H.F]]
[[Category: Large Structures]]
[[Category: Wichelhaus, T.A]]
[[Category: Cuesta-Bernal J]]
[[Category: El-Delik J]]
[[Category: Frank D]]
[[Category: Goettig S]]
[[Category: Klingler FM]]
[[Category: Koenigs A]]
[[Category: Mueller HF]]
[[Category: Pogoryelov D]]
[[Category: Proschak E]]
[[Category: Sjuts H]]
[[Category: Wichelhaus TA]]
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