Rational Design of Proteasome Inhibitors as Antimalarial Drugs
Angew. Chem. Int. Ed. 2016, 55, 6370–6372, DOI: 10.1002/anie.201602519
Angew. Chem. Int. Ed., online article
One life, two strategies: Crucial structural differences between the human and the Plasmodium falciparum proteasomes were recently identified. A combination of cryo-EM and functional characterization enabled the design of a selective antimalarial proteasome inhibitor that shows low toxicity in the host. When used with artemisinin, this ligand offers a new approach for the efficient treatment of malaria at all stages of the parasite lifecycle.