Starving the malaria parasite: Inhibitors active against the aspartic proteases plasmepsins I, II, and IV

Fraser Hof, Andri Schütz, Christoph Fäh, Solange Meyer, Daniel Bur, Jun Liu, Daniel E. Goldberg, François Diederich

Research output: Contribution to journalArticlepeer-review

74 Scopus citations

Abstract

Clamping down: A new class of aspartic protease inhibitors that target the malarial protease family Plasmepsin are reported. These ligands utilize a novel "diamine clamp" to engage the catalytic dyad. They are potent inhibitors of plasmepsins I, II, and IV, while retaining good selectivity against the closely related human cathepsins D and E. (Chemical Equation Presented) .

Original languageEnglish
Pages (from-to)2138-2141
Number of pages4
JournalAngewandte Chemie - International Edition
Volume45
Issue number13
DOIs
StatePublished - Mar 20 2006

Keywords

  • Aspartic proteases
  • Drug design
  • Inhibitors
  • Malaria
  • Medicinal chemistry

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