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research article
Benzothiazinones: prodrugs that covalently modify the decaprenylphosphoryl-β-D-ribose 2'-epimerase DprE1 of Mycobacterium tuberculosis
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.
Type
research article
Web of Science ID
WOS:000282864100034
Authors
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Schneider, Patricia
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Makarov, Vadim
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Publication date
2010
Publisher
Published in
Volume
132
Issue
39
Start page
13663
End page
5
Subjects
Peer reviewed
NON-REVIEWED
Available on Infoscience
October 14, 2010
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