Proteasome inhibitors have significant promise as components of novel combination therapies to treat multidrug-resistant malaria, according to a study published June 6 in the open-access journal PLOS Pathogens by David Fidock, Caroline Ng, and Barbara Stokes of Columbia University Irving Medical Center, Matthew Bogyo of Stanford University School of Medicine, and colleagues.
The spread of drug-resistant malaria, caused by the protozoan parasite Plasmodium falciparum, across Southeast Asia highlights the urgent need to develop new treatment options with compounds that are not susceptible to existing mechanisms of antimalarial drug resistance. Recent work has identified the P. falciparum proteasome—a protein complex that degrades unneeded or damaged proteins—as a promising drug target. In the new study, the researchers characterized the antimalarial activity of two P. falciparum-selective proteasome inhibitors—the covalent peptide vinyl sulfones WLL-vs (WLL) and WLW-vs (WLW).
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