Antifungal agent tavaborole as a potential broad-spectrum serine and metallo-β-lactamases inhibitor.

ABSTRACT:

Background

The global emergence and spread of carbapenem-resistant Enterobacteriaceae in clinical settings have driven the search for inhibitors that can counteract carbapenemases. These enzymes include several serine β-lactamases (SBLs, such as KPC) and metallo-β-lactamases (MBLs, such as NDM) that hydrolyse almost all β-lactams including carbapenems. This endeavour has successful developed some SBL inhibitors, including the boron-containing compound vaborbactam. However, the challenge posed by MBLs remains unresolved.

Methods

A high-throughput screening was conducted on 1718 FDA-approved drugs as potential adjuvants to meropenem. The synergistic effect was determined by checkerboard assay. The underlying mechanisms were elucidated using enzyme inhibition assays, molecular

SUBMITTER: Zhang Y 

PROVIDER: S-EPMC12141945 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature