Article
Introduction of Scaffold Nitrogen Atoms Renders Inhibitors of the Malarial l-Lactate Transporter, PfFNT, Effective against the Gly107Ser Resistance Mutation.
Journal of medicinal chemistry - 10 Sept 2020
Walloch Philipp, Henke Björn, Häuer Susan, Bergmann Bärbel, Spielmann Tobias, Beitz Eric
Abstract excerpt
The spreading of malaria parasites, Plasmodium falciparum, with resistance to all known drugs calls for novel classes of inhibitors with new modes of action. Recently, we discovered and validated the plasmodial l-lactate transporter, PfFNT, as a novel antimalarial drug target. However, treatment of parasites with a screening hit from the malaria box compound collection, MMV007839, gave rise to a PfFNT Gly107Ser...
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