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LK‑157 is a synthetic small molecule belonging to the trinem class of beta-lactamase inhibitors. It was designed as part of a series of 4-substituted trinems to address bacterial resistance mediated by beta-lactamases—enzymes that hydrolyze and inactivate beta-lactam antibiotics. LK‑157 acts as a mechanism-based inactivator targeting class C (AmpC) and class A beta-lactamases by acylating the active site serine residue (Ser64), thereby inhibiting enzyme activity and restoring the efficacy of co-administered beta-lactam antibiotics. The compound has demonstrated significant in vitro inhibitory activity against these enzymes but is not itself an antibiotic; rather it serves as an adjunctive agent to overcome resistance[3][7].
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