RSC Medicinal Chemistry · 2020 · 16 citations · 28 references
Life SciencesMedicinal ChemistryPharmacologyAntimicrobial ResistanceDrug DiscoveryLead OptimizationAntibacterial ResistanceAntibiotic ResistanceAntibiotic Resistance MechanismsBeta-lactam ResistanceCarbapenem ResistanceMultidrug ResistanceBeta-lactamase Inhibitor ResistanceBeta-lactamase InhibitorsCarbapenem AntibioticsCarbapenem Resistance MechanismsCarbapenem-hydrolyzing EnzymesCarbapenemase EnzymesNovel Beta-lactamase Discovery
at a super-resolution level (3D-SIM) showed that the target was initially associated on the surface of the cells, then there was a high density of uniform localization distributed in the cytosol of cells, and it finally accumulated in the formation of inclusion bodies at the cell poles. Docking studies suggested that the sulfonamide group acted as a zinc-binding group to coordinate with Zn(ii) and the residual amino acid within the CphA active center, tightly anchoring the inhibitor at the active site. This study provides a highly promising scaffold for the development of inhibitors of ImiS, even the B2 subclasses of MβLs.
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Aspergillomarasmine A overcomes metallo-β-lactamase antibiotic resistance
Andrew King, Sarah A. Reid‐Yu, Wenliang Wang et al. · Nature · 2014 · 540 citations
Kinetics of Avibactam Inhibition against Class A, C, and D β-Lactamases
David E. Ehmann, Haris Jahić, Philip L. Ross et al. · Journal of Biological Chemistry · 2013 · 355 citations · Full text