Making metallo-β-lactamase inhibitors with mimicry
Carbapenems, like meropenem, are antibiotics that are commonly used to treat serious Gram-negative infections. They are, however, prone to hydrolysis by metallo-β-lactamases (MBLs). A multidisciplinary team led by Jürgen Brem and Christopher J. Schofield have now shown that indole-2-carboxylates are inhibitors of MBLs and can restore the in vivo activity of meropenem. These inhibitors show minimal in vivo toxicity and are, therefore, promising candidates for clinical development. The cover image depicts an indole-2-carboxylate binding to an MBL.
See Brem et al.