Biomolecules, Volume 10, Issue 5 (May 2020) – 148 articles
Cover Story (view full-size image): β-Lactamase inhibitors (BLIs) are used in combination with existing β-lactam antibiotics to overcome β-lactamase-mediated antibiotic resistance. Boronic acid transition state analog inhibitors (BATSIs) are promising BLIs that form a reversible dative bond with the active site serine and mimic the tetrahedral transition state. Here, we report microbiological, biochemical, and structural studies of four BATSIs with a class C cephamycinase, FOX-4. X-ray crystal structures reveal that the compound, SM23, adopts different binding modes across class C β-lactamases. Comparison of the FOX-4/SM23 and FOX-4/cefoxitin complexes provides a rationale for the rapid turnover of cephamycins by FOX-4. Our analyses suggest new opportunities for the design of novel transition-state analogs of class C enzymes to be used as BLIs. View this paper.
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