Itaconate is a covalent inhibitor of the Mycobacterium tuberculosis isocitrate lyase

Brooke X.C. Kwai, Annabelle J. Collins, Martin J. Middleditch, Jonathan Sperry, Ghader Bashiri, Ivanhoe K.H. Leung

Research output: Contribution to journalArticleResearchpeer-review

30 Citations (Scopus)

Abstract

Itaconate is a mammalian antimicrobial metabolite that inhibits the isocitrate lyases (ICLs) ofMycobacterium 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.

Original languageEnglish
Pages (from-to)57-61
Number of pages5
JournalRSC Medicinal Chemistry
Volume12
Issue number1
DOIs
Publication statusPublished - 1 Jan 2021

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