Article
Characterization of DprE1-Mediated Benzothiazinone Resistance in Mycobacterium tuberculosis.
Antimicrobial agents and chemotherapy - 1 Nov 2016
Foo Caroline Shi-Yan, Lechartier Benoit, Kolly Gaëlle S, Boy-Röttger Stefanie, Neres João, Rybniker Jan, Lupien Andréanne, Sala Claudia, Piton Jérémie, Cole Stewart T
Abstract excerpt
Benzothiazinones (BTZs) are a class of compounds found to be extremely potent against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. The potency of BTZs is explained by their specificity for their target decaprenylphosphoryl-d-ribose oxidase (DprE1), in particular by covalent binding of the activated form of the compound to the critical cysteine 387 residue of the enzyme. To probe...
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