ArticleMolecules (Basel, Switzerland)2016
Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box.
Article in Molecules (Basel, Switzerland), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 12 citations in OpenAlex.
- The "Doorstop Pocket" In Thioredoxin Reductases─An Unexpected Druggable Regulator of the Catalytic Machinery.Journal of medicinal chemistry · 2024Review
- Reactive Oxygen Species as the Brainbox in Malaria Treatment.Antioxidants (Basel, Switzerland) · 2021Review
- PfMFR3: A Multidrug-Resistant Modulator inACS infectious diseases · 2021Article
- Redox interactome in malaria parasite Plasmodium falciparum.Parasitology research · 2021Review
- The relative rate of kill of the MMV Malaria Box compounds provides links to the mode of antimalarial action and highlights scaffolds of medicinal chemistry interest.The Journal of antimicrobial chemotherapy · 2020Article
- Antimalarial activity of Malaria Box Compounds against Plasmodium falciparum clinical isolates.International journal for parasitology. Drugs and drug resistance · 2017Article
- Metabolomics-Based Screening of the Malaria Box Reveals both Novel and Established Mechanisms of Action.Antimicrobial agents and chemotherapy · 2016Article
- Metabolomic Profiling of the Malaria Box Reveals Antimalarial Target Pathways.Antimicrobial agents and chemotherapy · 2016Article
- Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.PLoS pathogens · 2016Article
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
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.
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