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Rational Design of Proteasome Inhibitors as Antimalarial Drugs
Author(s) -
Le Chapelain Camille,
Groll Michael
Publication year - 2016
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201602519
Subject(s) - proteasome , plasmodium falciparum , artemisinin , malaria , rational design , drug design , computational biology , pharmacology , antimalarial agent , ligand (biochemistry) , plasmodium (life cycle) , drug discovery , chemistry , biology , parasite hosting , biochemistry , immunology , computer science , genetics , receptor , world wide web
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.