Targeting the Mycobacterium tuberculosis transpeptidase Ldt_Mt2 with cysteine-reactive inhibitors including ebselen.

ABSTRACT: The l,d-transpeptidases (Ldts) are promising antibiotic targets for treating tuberculosis. We report screening of cysteine-reactive inhibitors against LdtMt2 from Mycobacterium tuberculosis. Structural studies on LdtMt2 with potent inhibitor ebselen reveal opening of the benzisoselenazolone ring by a nucleophilic cysteine, forming a complex involving extensive hydrophobic interactions with a substrate-binding loop.

SUBMITTER: de Munnik M 

PROVIDER: S-EPMC6984337 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature