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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Autores principales: Tiwari, Neil K., Reynolds, Priscilla J., Calderón, Angela I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273446/
https://www.ncbi.nlm.nih.gov/pubmed/27043496
http://dx.doi.org/10.3390/molecules21040424
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author Tiwari, Neil K.
Reynolds, Priscilla J.
Calderón, Angela I.
author_facet Tiwari, Neil K.
Reynolds, Priscilla J.
Calderón, Angela I.
author_sort Tiwari, Neil K.
collection PubMed
description 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 IC(50) values ranging from 0.9–7.5 µM against the target enzyme, were found out of the Malaria Box.
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spelling pubmed-62734462018-12-28 Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box Tiwari, Neil K. Reynolds, Priscilla J. Calderón, Angela I. Molecules Article 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 IC(50) values ranging from 0.9–7.5 µM against the target enzyme, were found out of the Malaria Box. MDPI 2016-03-28 /pmc/articles/PMC6273446/ /pubmed/27043496 http://dx.doi.org/10.3390/molecules21040424 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons by Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tiwari, Neil K.
Reynolds, Priscilla J.
Calderón, Angela I.
Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box
title Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box
title_full Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box
title_fullStr Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box
title_full_unstemmed Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box
title_short Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box
title_sort preliminary lc-ms based screening for inhibitors of plasmodium falciparum thioredoxin reductase (pftrxr) among a set of antimalarials from the malaria box
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273446/
https://www.ncbi.nlm.nih.gov/pubmed/27043496
http://dx.doi.org/10.3390/molecules21040424
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