6vhs
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==CTX-M-14 in complex with ETX317== | |
| + | <StructureSection load='6vhs' size='340' side='right'caption='[[6vhs]], [[Resolution|resolution]] 1.28Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6VHS OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6VHS 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]] 1.28Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=PCA:PYROGLUTAMIC+ACID'>PCA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=X57:(2R)-({[(3R,6S)-6-carbamoyl-1-formyl-4-methyl-1,2,3,6-tetrahydropyridin-3-yl]amino}oxy)(fluoro)acetic+acid'>X57</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=6vhs FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vhs OCA], [https://pdbe.org/6vhs PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6vhs RCSB], [https://www.ebi.ac.uk/pdbsum/6vhs PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6vhs ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Multidrug resistant Gram-negative bacterial infections are an increasing public health threat due to rapidly rising resistance toward beta-lactam antibiotics. The hydrolytic enzymes called beta-lactamases are responsible for a large proportion of the resistance phenotype. beta-Lactamase inhibitors (BLIs) can be administered in combination with beta-lactam antibiotics to negate the action of the beta-lactamases, thereby restoring activity of the beta-lactam. Newly developed BLIs offer some advantage over older BLIs in terms of enzymatic spectrum but are limited to the intravenous route of administration. Reported here is a novel, orally bioavailable diazabicyclooctane (DBO) beta-lactamase inhibitor. This new DBO, ETX1317, contains an endocyclic carbon-carbon double bond and a fluoroacetate activating group and exhibits broad spectrum activity against class A, C, and D serine beta-lactamases. The ester prodrug of ETX1317, ETX0282, is orally bioavailable and, in combination with cefpodoxime proxetil, is currently in development as an oral therapy for multidrug resistant and carbapenem-resistant Enterobacterales infections. | ||
| - | + | Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine beta-Lactamases.,Durand-Reville TF, Comita-Prevoir J, Zhang J, Wu X, May-Dracka TL, Romero JAC, Wu F, Chen A, Shapiro AB, Carter NM, McLeod SM, Giacobbe RA, Verheijen JC, Lahiri SD, Sacco MD, Chen Y, O'Donnell JP, Miller AA, Mueller JP, Tommasi RA J Med Chem. 2020 Jul 24. doi: 10.1021/acs.jmedchem.0c00579. PMID:32658473<ref>PMID:32658473</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 6vhs" style="background-color:#fffaf0;"></div> |
| - | [[Category: | + | == References == |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Chen Y]] | ||
| + | [[Category: Sacco MD]] | ||
Current revision
CTX-M-14 in complex with ETX317
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