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Keywords:

  • aspartic proteases;
  • drug design;
  • inhibitors;
  • malaria;
  • medicinal chemistry
Thumbnail image of graphical 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.