A dual covalent binder for labelling and inhibiting serine and metallo-carbapenemases

Chem Commun (Camb). 2023 Jul 25;59(60):9227-9230. doi: 10.1039/d3cc02373g.

Abstract

The continuous emergence of multi-drug resistant pathogens co-expressing serine and metallo-carbapenemases seriously threatens the efficacy of carbapenem. Here, we report the first SeCN-derived dual inhibitor of serine and metallo-carbapenemases with IC50 values ranging from 0.0038 to 1.27 μg mL-1. The inhibitor was shown to form covalent bonds with Cys221 of NDM-1 and Ser70 of KPC-2, respectively, achieving selective labelling and cross-class inhibition for carbapenemases. Our results provide a potential strategy to develop clinically useful dual inhibitors targeting serine and metallo-carbapenemases to combat superbugs.

MeSH terms

  • Anti-Bacterial Agents* / chemistry
  • Bacterial Proteins*
  • Carbapenems
  • Microbial Sensitivity Tests
  • beta-Lactamases / chemistry

Substances

  • carbapenemase
  • Anti-Bacterial Agents
  • Bacterial Proteins
  • beta-Lactamases
  • Carbapenems