6li6

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==Crystal structure of MCR-1-S treated by Au(PEt3)Cl==
==Crystal structure of MCR-1-S treated by Au(PEt3)Cl==
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<StructureSection load='6li6' size='340' side='right'caption='[[6li6]]' scene=''>
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<StructureSection load='6li6' size='340' side='right'caption='[[6li6]], [[Resolution|resolution]] 1.68&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LI6 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6LI6 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6li6]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/"bacillus_coli"_migula_1895 "bacillus coli" migula 1895]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LI6 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6LI6 FirstGlance]. <br>
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</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6li6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6li6 OCA], [http://pdbe.org/6li6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6li6 RCSB], [http://www.ebi.ac.uk/pdbsum/6li6 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6li6 ProSAT]</span></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3EP:TRIETHYLPHOSPHANE'>3EP</scene>, <scene name='pdbligand=AU:GOLD+ION'>AU</scene></td></tr>
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<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">mcr1, mcr-1, APZ14_31440 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6li6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6li6 OCA], [http://pdbe.org/6li6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6li6 RCSB], [http://www.ebi.ac.uk/pdbsum/6li6 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6li6 ProSAT]</span></td></tr>
</table>
</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/MCR1_ECOLX MCR1_ECOLX]] Probably catalyzes the addition of a phosphoethanolamine moiety to lipid A. Phosphoethanolamine modification of lipid A gives polymyxin resistance (PubMed:26603172).<ref>PMID:26603172</ref> Confers resistance to polymyxin-type antibiotics; expression of the Mcr-1 protein in E.coli increases colistin and polymyxin B minimal inhibitory concentration (MIC) from 0.5 mg/ml to 2.0 mg/ml. The pHNSHP45 plasmid can transfer efficiently (0.1 to 0.001) to other E.coli strains by conjugation and increases polymxin MIC by 8- to 16-fold; it may not require selective pressure to be maintained in the cell. When transformed into K.pneumoniae or P.aeruginosa it also increases polymxin MIC 8- to 16-fold. In a murine (BALB/c mice) thigh infection study using an mcr1-encoding plasmid isolated from a human patient, the plasmid confers in vivo protection against colistin (PubMed:26603172).<ref>PMID:26603172</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Global emergence of Gram-negative bacteria carrying the plasmid-borne resistance genes, blaMBL and mcr, raises a significant challenge to the treatment of life-threatening infections by the antibiotics, carbapenem and colistin (COL). Here, we identify an antirheumatic drug, auranofin (AUR) as a dual inhibitor of metallo-beta-lactamases (MBLs) and mobilized colistin resistance (MCRs), two resistance enzymes that have distinct structures and substrates. We demonstrate that AUR irreversibly abrogates both enzyme activity via the displacement of Zn(II) cofactors from their active sites. We further show that AUR synergizes with antibiotics on killing a broad spectrum of carbapenem and/or COL resistant bacterial strains, and slows down the development of beta-lactam and COL resistance. Combination of AUR and COL rescues all mice infected by Escherichia coli co-expressing MCR-1 and New Delhi metallo-beta-lactamase 5 (NDM-5). Our findings provide potential therapeutic strategy to combine AUR with antibiotics for combating superbugs co-producing MBLs and MCRs.
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Resensitizing carbapenem- and colistin-resistant bacteria to antibiotics using auranofin.,Sun H, Zhang Q, Wang R, Wang H, Wong YT, Wang M, Hao Q, Yan A, Kao RY, Ho PL, Li H Nat Commun. 2020 Oct 16;11(1):5263. doi: 10.1038/s41467-020-18939-y. PMID:33067430<ref>PMID:33067430</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 6li6" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Bacillus coli migula 1895]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Sun H]]
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[[Category: Sun, H]]
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[[Category: Wang M]]
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[[Category: Wang, M]]
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[[Category: Zhang Q]]
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[[Category: Zhang, Q]]
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[[Category: Antibiotic]]
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[[Category: Transferase]]

Revision as of 20:41, 28 October 2020

Crystal structure of MCR-1-S treated by Au(PEt3)Cl

PDB ID 6li6

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