化学
抗细菌
结核分枝杆菌
前药
立体化学
核糖
亚硝基
半胱氨酸
作用机理
生物化学
残留物(化学)
肺结核
酶
有机化学
医学
病理
体外
作者
Claudia Trefzer,Rengifo-Gonzalez Monica,Marlon J. Hinner,Patricia Schneider,Vadim Makarov,Stewart T. Cole,Kai Johnsson
摘要
Benzothiazinones (BTZs) form a new class of potent antimycobacterial agents. Although the target of BTZs has been identified as decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), their detailed mechanism of action remains obscure. Here we demonstrate that BTZs are activated in the bacterium by reduction of an essential nitro group to a nitroso derivative, which then specifically reacts with a cysteine residue in the active site of DprE1.
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