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Itaconate is a covalent inhibitor of the Mycobacterium tuberculosis isocitrate lyase.

ABSTRACT: Itaconate is a mammalian antimicrobial metabolite that inhibits the isocitrate lyases (ICLs) of Mycobacterium tuberculosis. Herein, we report that ICLs form a covalent adduct with itaconate through their catalytic cysteine residue. These results reveal atomic details of itaconate inhibition and provide insights into the catalytic mechanism of ICLs.

SUBMITTER: Kwai BXC

PROVIDER: S-EPMC8130629 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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Itaconate is a covalent inhibitor of the Mycobacterium tuberculosis isocitrate lyase.

Kwai Brooke X C BXC Collins Annabelle J AJ Middleditch Martin J MJ Sperry Jonathan J Bashiri Ghader G Leung Ivanhoe K H IKH

RSC medicinal chemistry 20201019 1

Itaconate is a mammalian antimicrobial metabolite that inhibits the isocitrate lyases (ICLs) of Mycobacterium tuberculosis. Herein, we report that ICLs form a covalent adduct with itaconate through their catalytic cysteine residue. These results reveal atomic details of itaconate inhibition and provide insights into the catalytic mechanism of ICLs. ...[more]

PMID: 34046597

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