Article
Mechanisms of Resistance Associated with the Inhibition of the Dehydration Step of Type II Fatty Acid Synthase in Mycobacterium tuberculosis.
ACS infectious diseases - 14 Feb 2020
Grzegorzewicz Anna E, Gee Clifford, Das Sourav, Liu Jiuyu, Belardinelli Juan Manuel, Jones Victoria, McNeil Michael R, Lee Richard E, Jackson Mary
Abstract excerpt
Isoxyl (ISO) and thiacetazone (TAC) are two antitubercular prodrugs that abolish mycolic acid biosynthesis and kill Mycobacterium tuberculosis (Mtb) through the inhibition of the essential type II fatty acid synthase (FAS-II) dehydratase HadAB. While mutations preventing ISO and TAC either from being converted to their active form or from covalently modifying their target are the most frequent spontaneous...
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