This research demonstrates the effectiveness of species-selective proteasome inhibitors against Plasmodium falciparum, suggesting new antimalarial strategies.
Key Points
Highly potent and selective inhibitors targeting P. falciparum were developed.
Lead compounds displayed nanomolar potency in inhibiting the parasite's proteasome.
Iterative structure-activity relationship studies were conducted on carboxypiperidine scaffolds.
Binding to the β5 subunit of the proteasome was confirmed through Cryo-EM structural studies.