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B6db references: 21252905

type Journal Article
authors Coombs, G. H.; Mottram, J. C.
title Trifluoromethionine, a prodrug designed against methionine gamma-lyase- containing pathogens, has efficacy in vitro and in vivo against Trichomonas vaginalis
journal Antimicrob Agents Chemother
ui 21252905
year (2001)
volume 45
number 6
pages 1743-5.
keywords Animal
abstract Methionine gamma-lyase, the enzyme which catalyzes the single-step conversion of methionine to alpha-ketobutyrate, ammonia, and methanethiol, is highly active in many anaerobic pathogenic microorganisms but has no counterpart in mammals. This study tested the hypothesis that this pathogen-specific enzyme can be exploited as a drug target by prodrugs that are exclusively activated by it. Trifluoromethionine was confirmed as such a prodrug and shown to be highly toxic in vitro to the anaerobic protozoan parasite Trichomonas vaginalis, to anaerobic bacteria containing methionine gamma-lyase, and to Escherichia coli expressing the trichomonad gene. The compound also has exceptional activity against the parasite growing in vivo, with a single dose preventing lesion formation in five of the six mice challenged. These findings suggest that trifluoromethionine represents a lead compound for a novel class of anti-infective drugs with potential as chemotherapeutic agents against a range of prokaryotic and eukaryotic anaerobic pathogens.
last changed 2008/06/09 17:52

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