Antibiotic resistance continues to increase as a threat to public health. The DHA-1 β-lactamase is a plasmid-based class C enzyme that is widespread throughout Asia and the Middle East. It is relatively distantly related to other class C enzymes of known structure, being only 56% identical to <i>E. coli</i> AmpC, its closest relative. Its frequent appearance in drug-resistant infections makes it a clinically relevant target. Relebactam is an FDA-approved diazabicyclooctane (DBO) β-lactamase inhibitor (BLI). BLIs prevents the hydrolysis β-lactam antibiotics, allowing the antibiotics to inhibit cell wall synthesis with higher potency. To further elucidate the interaction between class C β-lactamases and DBOs, the x-ray crystal structure of DHA-1 was determined to 1.75 Å resolution for apo DHA-1 and the relebactam/DHA-1 complex. Comparison of these structures with AmpC and FOX-4 bound to DBOs suggests a common binding mode and a specific binding pocket for the piperidine ring of relebactam.<br/><br/>

X-ray crystal structure of the class C β-lactamase DHA-1 with relebactam, a diazabicyclooctane β-lactamase inhibitor

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.