Nature Communications (Nov 2022)

An active site loop toggles between conformations to control antibiotic hydrolysis and inhibition potency for CTX-M β-lactamase drug-resistance enzymes

  • Shuo Lu,
  • Liya Hu,
  • Hanfeng Lin,
  • Allison Judge,
  • Paola Rivera,
  • Murugesan Palaniappan,
  • Banumathi Sankaran,
  • Jin Wang,
  • B. V. Venkataram Prasad,
  • Timothy Palzkill

DOI
https://doi.org/10.1038/s41467-022-34564-3
Journal volume & issue
Vol. 13, no. 1
pp. 1 – 13

Abstract

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β-lactamases are a source of antibiotic resistance. Here, the authors show that an active site loop in β-lactamase toggles between conformations that control antibiotic hydrolysis and inhibitor susceptibility, highlighting the role of active site conformations in enzyme activity and inhibition.