F.H. thanks the Novartis Foundation and the Human Frontier Science Program for financial support. This research was supported by the ETH Research Council. We thank Anna Oksman for technical assistance.
Starving the Malaria Parasite: Inhibitors Active against the Aspartic Proteases Plasmepsins I, II, and IV†
Article first published online: 27 FEB 2006
Copyright © 2006 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 45, Issue 13, pages 2138–2141, March 20, 2006
How to Cite
Hof, F., Schütz, A., Fäh, C., Meyer, S., Bur, D., Liu, J., Goldberg, D. E. and Diederich, F. (2006), Starving the Malaria Parasite: Inhibitors Active against the Aspartic Proteases Plasmepsins I, II, and IV. Angew. Chem. Int. Ed., 45: 2138–2141. doi: 10.1002/anie.200504119
- Issue published online: 13 MAR 2006
- Article first published online: 27 FEB 2006
- Manuscript Received: 19 NOV 2005
- aspartic proteases;
- drug design;
- medicinal chemistry
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.