Discovery and chemical optimisation of a potent, Bi-cyclic antimicrobial inhibitor of Escherichia coli PBP3

Abstract Penicillin binding proteins (PBPs) are well validated antimicrobial targets, but the prevalence of β-lactamase driven resistance and, more rarely, target-based mutations, necessitates new classes of PBP-targeting drugs. Here we describe the discovery and optimisation of bicyclic peptide (Bi...

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Main Authors: Catherine E. Rowland, Hector Newman, Tazmin T. Martin, Rachel Dods, Nikolaos Bournakas, James M. Wagstaff, Nick Lewis, Steven J. Stanway, Matthew Balmforth, Celia Kessler, Katerine van Rietschoten, Dom Bellini, David I. Roper, Adrian J. Lloyd, Christopher G. Dowson, Michael J. Skynner, Paul Beswick, Michael J. Dawson
Format: Article
Language:English
Published: Nature Portfolio 2025-05-01
Series:Communications Biology
Online Access:https://doi.org/10.1038/s42003-025-08246-x
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