Abstract
DNA damage associated with the trypanocidal activity of megazol [2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole] was shown in experiments in which DNA repair-deficient RAD51(-/-) Trypanosoma brucei mutants were found to be hypersensitive to the drug. Parasites resistant to megazol were selected and showed modest cross-resistance to other trypanocides, although neither drug efflux nor changes to intracellular thiols correlated with resistance.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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DNA Damage*
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DNA-Binding Proteins / genetics
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Drug Resistance, Multiple / drug effects
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Drug Resistance, Multiple / genetics
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Inhibitory Concentration 50
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Mutation
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Thiadiazoles / chemistry
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Thiadiazoles / pharmacology*
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Trypanocidal Agents / pharmacology*
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Trypanosoma brucei brucei / drug effects
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Trypanosoma brucei brucei / genetics
Substances
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DNA-Binding Proteins
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Thiadiazoles
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Trypanocidal Agents
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megazol