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Molecules 2016, 21(4), 424; doi:10.3390/molecules21040424

Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box

Department of Drug Discovery and Development, Auburn University, 4306 Walker Building, Auburn, AL 36849, USA
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Academic Editor: Derek J. McPhee
Received: 28 February 2016 / Revised: 11 March 2016 / Accepted: 24 March 2016 / Published: 28 March 2016
(This article belongs to the Special Issue Thioredoxin and Glutathione Systems)
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Abstract

Plasmodium falciparum thioredoxin reductase (PfTrxR) has been identified as a potential drug target to combat growing antimalarial drug resistance. Medicines for Malaria Venture (MMV) has pre-screened and identified a set of 400 antimalarial compounds called the Malaria Box. From those, we have evaluated their mechanisms of action through inhibition of PfTrxR and found new active chemical scaffolds. Five compounds with significant PfTrxR inhibitory activity, with IC50 values ranging from 0.9–7.5 µM against the target enzyme, were found out of the Malaria Box. View Full-Text
Keywords: Plasmodium falciparum thioredoxin reductase; antimalarial; screening for mechanism of action; Malaria Box Plasmodium falciparum thioredoxin reductase; antimalarial; screening for mechanism of action; Malaria Box
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MDPI and ACS Style

Tiwari, N.K.; Reynolds, P.J.; Calderón, A.I. Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box. Molecules 2016, 21, 424.

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