Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors
Copyright policy )Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors
We evaluated the antimalarial effects of vinyl sulfone cysteine proteinase inhibitors. A number of vinyl sulfones strongly inhibited falcipain, a Plasmodium falciparum cysteine proteinase that is a critical hemoglobinase. In studies of cultured parasites, nanomolar concentrations of three vinyl sulfones inhibited parasite hemoglobin degradation, metabolic activity, and development. The antimalarial effects correlated with the inhibition of falcipain. Our results suggest that vinyl sulfones or related cysteine proteinase inhibitors may have promise as antimalarial agents.
- San Francisco General Hospital United States
Mice, Inbred BALB C, Erythrocytes, Plasmodium falciparum, Cysteine Proteinase Inhibitors, Antimalarials, Cysteine Endopeptidases, Hemoglobins, Mice, Animals, Humans, Sulfones, Malaria, Falciparum
Mice, Inbred BALB C, Erythrocytes, Plasmodium falciparum, Cysteine Proteinase Inhibitors, Antimalarials, Cysteine Endopeptidases, Hemoglobins, Mice, Animals, Humans, Sulfones, Malaria, Falciparum
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