Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T96215 | ||||
Target Name | Plasmodium Glutamate dehydrogenase (Malaria gdh) | ||||
Type of Target |
Successful |
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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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