Fumarate hydratase-IN-1

Fumarate hydratase-IN-1, an enzyme of the TCA cycle. Inhibition of fumarate hydratase-IN-1 can contribute to tumorigenicity in some cells. The use of a photoaffinity labeling strategy identified fumarate hydratase as the principal pharmacological target.[1] In vitro: The activity of this enzyme was measured using a well-established assay that monitored the conversion of fumarate into L-malate and subsequent oxidation of L-malate to oxaloacetate by malate dehydrogenase. Initial controls established that neither the carboxylic acid 3 nor ester 2 inhibited malate dehydrogenase Using this two-enzyme protocol we found that carboxylic acid 3 inhibited fumarate hydratase in a dose-dependent fashion in vitro. Besides, inhibition of fumarate hydratase can contribute to tumorigenicity in some cells.[1]