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Beta-lactam antibiotics act as structural analogs of the D-alanyl-D-alanine terminus of peptidoglycan precursors, covalently binding to the active site serine of penicillin-binding proteins (PBPs) (Bush & Bradford, 2016, Cold Spring Harb Perspect Med). This irreversible inhibition prevents the transpeptidation reaction required for peptidoglycan cross-linking, leading to a weakened cell wall, triggering of autolysins, and eventual bacterial cell lysis (Sauvage et al., 2008, FEMS Microbiol Rev).
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