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Inhibitors of Plasmepsin II-potential antimalarial agents |
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| Authors: | Corminboeuf Olivier Dunet Guillaume Hafsi Mehdi Grimont Julien Grisostomi Corinna Meyer Solange Binkert Christoph Bur Daniel Jones Andrew Prade Lars Brun Reto Boss Christoph |
| Institution: | aDrug Discovery Chemistry and Biochemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland bEcole Nationale Supérieure de Chimie de Mulhouse, 3, rue Alfred Werner, 68093 Mulhouse Cedex, France cEcole d’ingénieurs et d’architectes de Fribourg, Département de chimie, Bd de Pérolles 80, 1705 Fribourg, Switzerland dSwiss Tropical Institute (STI), Socinstrasse 57, 4002 Basel, Switzerland |
| Abstract: | In order to overcome the problem of drug resistance in malaria, it appears wise to concentrate drug discovery efforts toward new structural classes and new mechanisms of action. We report our results, targeting Plasmepsin II, a Plasmodium falciparum aspartic protease active in hemoglobin degradation, a parasite specific catabolic pathway. The results show that the new structural class is not only inhibiting PMII in vitro but is also active in a P. falciparum infected human red blood cell assay. |
| Keywords: | Malaria Plasmepsin II |
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