A Two Amino Acid Duplication, L167E168, in the Ω-Loop Drastically Decreases Carbapenemase Activity of KPC-53, a Natural Class A β-Lactamase

Antimicrob Agents Chemother. 2022 Jun 21;66(6):e0240221. doi: 10.1128/aac.02402-21. Epub 2022 Jun 1.

Abstract

KPC-53 enzyme is a natural KPC variant which showed a duplication of L167E168 residues in the Ω-loop structure. The blaKPC-53 gene was cloned both into pBC-SK and pET-24a vectors, and the recombinant plasmids were transferred by transformation in Escherichia coli competent cells to evaluate the antimicrobial susceptibility and to produce the enzyme. Compared to KPC-3, the KPC-53 was less stable and showed a dramatic reduction of kcat and kcat/Km versus several β-lactams, in particular carbapenems. Indeed, a 2,000-fold reduction was observed in the kcat values of KPC-53 for imipenem and meropenem. Concerning inhibitors, KPC-53 was susceptible to tazobactam and clavulanic acid but maintained resistance to avibactam. The molecular modeling indicates that the L167E168 duplication in KPC-53 modifies the interactions between residues involved in the catalytic pocket, changing the flexibility of the Ω-loop, which is directly coupled with the catalytic properties of the KPC enzymes.

Keywords: KPC-53; carbapenemase; serine-β-lactamase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids*
  • Anti-Bacterial Agents / metabolism
  • Anti-Bacterial Agents / pharmacology
  • Azabicyclo Compounds / pharmacology
  • Bacterial Proteins / metabolism
  • Drug Combinations
  • Escherichia coli / metabolism
  • Klebsiella pneumoniae
  • Microbial Sensitivity Tests
  • beta-Lactamase Inhibitors / pharmacology
  • beta-Lactamases* / metabolism

Substances

  • Amino Acids
  • Anti-Bacterial Agents
  • Azabicyclo Compounds
  • Bacterial Proteins
  • Drug Combinations
  • beta-Lactamase Inhibitors
  • beta-Lactamases
  • carbapenemase