Target Validation Information
TTD ID T96215
Target Name Plasmodium Glutamate dehydrogenase (Malaria gdh)
Type of Target
Successful
Drug Potency against Target Hexachlorophene Drug Info I50 = 1600 nM [2]
Action against Disease Model Hexachlorophene Drug Info Brain succinate dehydrogenase (SDH) activity was inhibited by in vitro hexachlorophene (HCP) with a half inhibitory concentration (IC50) of 0.65 x 10(-3) M. The HCP exerted noncompetitive inhibition at 0.5 mM (<IC50), uncompetitive inhibition at 0.65 mM (= IC50), and mixed-type inhibition at 0.8 mM (>IC50) on SDH activity. The brain SDH demands more energy of activation (deltaE) in the presence of HCP. The ionizable groups of SDH such as the sulfhydral group of cysteine and alpha-amino groups of cysteine were not altered qualitatively in the presence of HCP. [1]
References
REF 1 In vitro kinetics of the rat brain succinate dehydrogenase inhibition by hexachlorophene. J Biochem Mol Toxicol. 1999;13(6):303-6.
REF 2 Inhibition of dehydrogenase enzymes by hexachlorophene. Biochem Pharmacol. 1978;27(24):2947-53.

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