Ontology highlight
ABSTRACT:
SUBMITTER: Tooke CL
PROVIDER: S-EPMC7536818 | biostudies-literature | 2020 Apr
REPOSITORIES: biostudies-literature
RSC medicinal chemistry 20200110 4
<i>Klebsiella pneumoniae</i> carbapenemase-2 (KPC-2) is a serine-β-lactamase (SBL) capable of hydrolysing almost all β-lactam antibiotics. We compare KPC-2 inhibition by vaborbactam, a clinically-approved monocyclic boronate, and VNRX-5133 (taniborbactam), a bicyclic boronate in late-stage clinical development. Vaborbactam inhibition is slowly reversible, whereas taniborbactam has an off-rate indicating essentially irreversible complex formation and a 15-fold higher on-rate, although both potent ...[more]