Article
Rational drug design approach for overcoming drug resistance: application to pyrimethamine resistance in malaria.
Journal of medicinal chemistry - 23 Apr 1998
McKie J H, Douglas K T, Chan C, Roser S A, Yates R, Read M, Hyde J E, Dascombe M J, Yuthavong Y, Sirawaraporn W
Abstract excerpt
Pyrimethamine acts by selectively inhibiting malarial dihydrofolate reductase-thymidylate synthase (DHFR-TS). Resistance in the most important human parasite, Plasmodium falciparum, initially results from an S108N mutation in the DHFR domain, with additional mutation (most commonly C59R or N51I o...
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