Rational design of proteasome inhibitors as antimalarial drugs

Camille Le Chapelain, Michael Groll

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

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.

Original languageEnglish
Pages (from-to)6370-6372
Number of pages3
JournalAngewandte Chemie International Edition in English
Volume55
Issue number22
DOIs
StatePublished - 23 May 2016

Keywords

  • cryo-electron microscopy
  • drug design
  • malaria
  • proteasome
  • structure-activity relationship

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