Covalent Plasmodium falciparum-selective proteasome inhibitors exhibit a low propensity for generating resistance in vitro and synergize with multiple antimalarial agents.

Therapeutics with novel modes of action and a low risk of generating resistance are urgently needed to combat drug-resistant Plasmodium falciparum malaria. Here, we report that the peptide vinyl sulfones WLL-vs (WLL) and WLW-vs (WLW), highly selective covalent inhibitors of the P. falciparum proteas...

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Bibliographic Details
Main Authors: Barbara H Stokes, Euna Yoo, James M Murithi, Madeline R Luth, Pavel Afanasyev, Paula C A da Fonseca, Elizabeth A Winzeler, Caroline L Ng, Matthew Bogyo, David A Fidock
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2019-06-01
Series:PLoS Pathogens
Online Access:https://doi.org/10.1371/journal.ppat.1007722