Stage-specific antimalarial activity of cysteine protease inhibitors.

Abstract:

:Cysteine proteases of the malaria parasite Plasmodium falciparum, known as falcipains, are promising targets for antimalarial chemotherapy. We evaluated cultured parasites for the stage-specific expression of cysteine proteases and sensitivity to cysteine protease inhibitors. Protease activity and inhibitor sensitivity varied markedly over time. Cysteine protease activity was greatest in early trophozoites, while sensitivity to cysteine protease inhibitors was greatest in mature trophozoites. Our results indicate the importance of considering the stage-specific effects of antimalarials and are consistent with the conclusion that the principal antimalarial activity of cysteine protease inhibitors is due to a block in hemoglobin hydrolysis.

journal_name

Biol Chem

journal_title

Biological chemistry

authors

Shenai BR,Semenov AV,Rosenthal PJ

doi

10.1515/BC.2002.089

keywords:

subject

Has Abstract

pub_date

2002-05-01 00:00:00

pages

843-7

issue

5

eissn

1431-6730

issn

1437-4315

journal_volume

383

pub_type

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