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research article
Studies on the Mechanism of Action of Isoniazid and Ethionamide in the Chemotherapy of Tuberculosis
The inactivation of the enoyl-reductase InhA from Mycobacterium tuberculosis by reactive intermediates formed during the oxidn. of isoniazid and ethionamide was studied. Both drugs can generate electrophilic intermediates capable of reacting with a nucleophilic group of InhA, leading to its inactivation. After inactivation of InhA by isoniazid, one mol. of isoniazid per InhA is covalently bound to the enzyme. Mapping studies suggest that Cys243 is the residue modified in the course of the inactivation. [on SciFinder (R)]
Type
research article
Authors
Publication date
1995
Published in
Volume
117
Issue
17
Start page
5009
End page
10
Peer reviewed
REVIEWED
EPFL units
Available on Infoscience
February 27, 2006
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