Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors | Zendy

Philip J. Rosenthal | Zendy; Jed Olson | Zendy; G K Lee | Zendy; James T. Palmer | Zendy; Jeffrey L. Klaus | Zendy; David Rasnick | Zendy

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Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors

Author(s) -

Philip J. Rosenthal,

Jed Olson,

G K Lee,

James T. Palmer,

Jeffrey L. Klaus,

David Rasnick

Publication year - 1996

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.40.7.1600

Subject(s) - cysteine , plasmodium falciparum , sulfone , cysteine proteinase inhibitors , enzyme , biochemistry , enzyme inhibitor , chemistry , pharmacology , biology , malaria , immunology , organic chemistry , apoptosis , programmed cell death , caspase

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.

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