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

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 eval...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2016-03, Vol.21 (4), p.424-424
Main Authors: Tiwari, Neil K, Reynolds, Priscilla J, Calderón, Angela I
Format: Article
Language:English
Subjects:
Animals
antimalarial
Antimalarials - chemistry
Antimalarials - pharmacology
Antiparasitic agents
Chromatography, Liquid
Drug resistance
Enzymes
Humans
Malaria
Malaria Box
Malaria, Falciparum - drug therapy
Malaria, Falciparum - parasitology
Mass Spectrometry
Molecular Structure
Oxidation-Reduction - drug effects
Oxidative stress
Parasites
Pharmaceutical industry
Plasmodium falciparum
Plasmodium falciparum - drug effects
Plasmodium falciparum - enzymology
Plasmodium falciparum - pathogenicity
Plasmodium falciparum thioredoxin reductase
screening for mechanism of action
Thioredoxin-Disulfide Reductase - antagonists & inhibitors
Thioredoxin-Disulfide Reductase - chemistry
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Summary: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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules21040424