Article
Demonstration of the activation of prodrug CB 1954 using human DT-diaphorase mutant Q104Y-transfected MDA-MB-231 cells and mouse xenograft model.
Archives of biochemistry and biophysics - 1 Jan 2001
Wu K, Eng E, Knox R, Chen S
Abstract excerpt
The rat form of DT-diaphorase (NAD(P)H: quinone acceptor oxidoreductase; EC 1.6.99.2) is more effective than the human form in activating prodrugs such as CB 1954 (5-(aziridin-1-yl)-2,4-dinitrobenzamide). Our site-directed mutagenesis study has revealed that residue 104 (Tyr in the rat enzyme and Gln in the human enzyme) is an important residue responsible for the catalytic differences between the rat and the...
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