An expression system to screen for inhibitors of parasite glucose transporters.

Molecular and Biochemical Parasitology
Torben FeistelScott Landfear

Abstract

Chemotherapy of parasitic protists is limited by general toxicity, high expense and emergence of resistance to currently available drugs. Thus methods to identify new leads for further drug development are increasingly important. Previously, glucose transporters have been validated as new drug targets for protozoan parasites including Plasmodium falciparum, Leishmania mexicana and Trypanosoma brucei. A recently derived glucose transporter null mutant (Deltalmgt) of L. mexicana was used to functionally express various heterologous glucose transporters including those from T. brucei THT1, P. falciparum PfHT and human GLUT1-resulting in recovery of growth of the Deltalmgt null mutant in glucose replete medium. This heterologous expression system can be employed to screen for compounds that retard growth by inhibiting the expressed glucose transporter. The ability of this expression system to identify specific glucose transporter inhibitors was demonstrated using 3-O-undec-10-enyl-d-glucose, a previously described specific inhibitor of PfHT.

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Citations

Dec 21, 2010·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Martin BlumeNishith Gupta
Jul 21, 2009·Eukaryotic Cell·Jeffrey Sabina, Victoria Brown
Jul 13, 2016·Cellular Microbiology·Patrícia MeirelesMiguel Prudêncio
Dec 30, 2017·PLoS Neglected Tropical Diseases·Diana OrtizScott M Landfear

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