Ontology highlight
ABSTRACT:
SUBMITTER: Brem J
PROVIDER: S-EPMC4979060 | biostudies-literature | 2016 Aug
REPOSITORIES: biostudies-literature
Brem Jürgen J Cain Ricky R Cahill Samuel S McDonough Michael A MA Clifton Ian J IJ Jiménez-Castellanos Juan-Carlos JC Avison Matthew B MB Spencer James J Fishwick Colin W G CW Schofield Christopher J CJ
Nature communications 20160808
β-Lactamases enable resistance to almost all β-lactam antibiotics. Pioneering work revealed that acyclic boronic acids can act as 'transition state analogue' inhibitors of nucleophilic serine enzymes, including serine-β-lactamases. Here we report biochemical and biophysical analyses revealing that cyclic boronates potently inhibit both nucleophilic serine and zinc-dependent β-lactamases by a mechanism involving mimicking of the common tetrahedral intermediate. Cyclic boronates also potently inhi ...[more]