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

28 Mar 2016

Neil K. Tiwari,  Priscilla J. Reynolds and  Angela I. Calderón.

Molecules

doi: 10.3390/molecules21040424

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 the full article on the Molecules website.