Issue 1, 2021

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.

Graphical abstract: Itaconate is a covalent inhibitor of the Mycobacterium tuberculosis isocitrate lyase

  • This article is part of the themed collection: Tuberculosis

Supplementary files

Article information

Article type
Research Article
Submitted
27 Aug 2020
Accepted
07 Oct 2020
First published
19 Oct 2020

RSC Med. Chem., 2021,12, 57-61

Itaconate is a covalent inhibitor of the Mycobacterium tuberculosis isocitrate lyase

B. X. C. Kwai, A. J. Collins, M. J. Middleditch, J. Sperry, G. Bashiri and I. K. H. Leung, RSC Med. Chem., 2021, 12, 57 DOI: 10.1039/D0MD00301H

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