Itaconate is a covalent inhibitor of the Mycobacterium tuberculosis isocitrate lyase. Issue 1 (19th October 2020)

• Record Type: Journal Article
• Authors: Kwai, Brooke X. C.; Collins, Annabelle J.; Middleditch, Martin J.; Sperry, Jonathan; Bashiri, Ghader; Leung, Ivanhoe K. H.
• Is Part Of: RSC medicinal chemistry. Volume 12:Issue 1(2021)
• Page Start: 57
• Page End: 61
• Publication Date: 2020-10-19
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1039/d0md00301h
• Languages: English
• ISSNs: 2632-8682

Abstract

Abstract : Mycobacterium tuberculosis isocitrate lyases (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. 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.