New boronate drugs and evolving NDM-mediated beta-lactam resistance

Antimicrob Agents Chemother. 2023 Sep 19;67(9):e0057923. doi: 10.1128/aac.00579-23. Epub 2023 Aug 31.

Abstract

Taniborbactam and xeruborbactam are dual serine-/metallo-beta-lactamase inhibitors (BLIs) based on a cyclic boronic acid pharmacophore that undergo clinical development. Recent report demonstrated that New Delhi metallo-beta-lactamase (NDM)-9 (differs from NDM-1 by a single amino acid substitution, E152K, evolved to overcome Zn (II) deprivation) is resistant to inhibition by taniborbactam constituting pre-existing taniborbactam resistance mechanism. Using microbiological and biochemical experiments, we show that xeruborbactam is capable of inhibiting NDM-9 and propose the structural basis for differences between two BLIs.

Keywords: NDM; NDM-9; metallo-β-lactamase; taniborbactam; xeruborbactam.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Substitution
  • Borinic Acids*
  • Boronic Acids / pharmacology
  • beta-Lactam Resistance / genetics
  • beta-Lactamase Inhibitors / pharmacology

Substances

  • taniborbactam
  • Borinic Acids
  • Boronic Acids
  • beta-Lactamase Inhibitors