Inhibitors of aspartic proteases – potential antimalarial agents

Abstract

This review emphasises the importance of research in the field of new antimalarial therapeutic agents, summarises the biology of plasmepsin II, a protozoal aspartic protease, and other related plasmepsins, and analyses the scientific literature and the patent literature describing efforts in the search for inhibitors of plasmepsins. As there are only very limited efforts in this area by the pharmaceutical industry, the patent literature reviewed covers the period of the last 10 years and, in addition, the article discusses results published by academic research groups. Several approaches are based on earlier work in the field of HIV-1 protease inhibitors and of renin inhibitors.

Keywords::

• aspartic protease inhibitor
• malaria
• plasmepsin
• Plasmodium falciparum
• structure-based drug design

Acknowledgements

The opinions and statements made in this article are the private views of the authors and do not necessarily reflect the corporate views of Actelion Pharmaceuticals Ltd.