Rational Design of Proteasome Inhibitors as Antimalarial Drugs.

Angew Chem Int Ed Engl

Center for Integrated Protein Science Munich (CIPSM), Department Chemie, Technische Universität München, Lichtenbergstrasse 4, 85748, Garching, Germany.

Published: May 2016

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.

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http://dx.doi.org/10.1002/anie.201602519DOI Listing

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