Volume 55, Issue 22 pp. 6370-6372
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Rational Design of Proteasome Inhibitors as Antimalarial Drugs

Dr. Camille Le Chapelain

Corresponding Author

Dr. Camille Le Chapelain

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

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Prof. Dr. Michael Groll

Corresponding Author

Prof. Dr. Michael Groll

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

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First published: 15 April 2016
Citations: 11

Graphical Abstract

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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