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Antimicrob Agents Chemother. 2005 Jul;49(7):2983-5.

Antimalarial activity of human immunodeficiency virus type 1 protease inhibitors.

Author information

1
Department of Medicine, San Francisco General Hospital, University of California, San Francisco, Box 0811, San Francisco, California 94110, USA. sunil@itsa.ucsf.edu

Abstract

Aspartic proteases play key roles in the biology of malaria parasites and human immunodeficiency virus type 1 (HIV-1). We tested the activity of seven HIV-1 protease inhibitors against cultured Plasmodium falciparum. All compounds inhibited the development of parasites at pharmacologically relevant concentrations. The most potent compound, lopinavir, was active against parasites (50% inhibitory concentration [IC50], 0.9 to 2.1 microM) at concentrations well below those achieved by ritonavir-boosted lopinavir therapy. Lopinavir also inhibited the P. falciparum aspartic protease plasmepsin II at a similar concentration (IC50, 2.7 microM). These findings suggest that use of HIV-1 protease inhibitors may offer clinically relevant antimalarial activity.

PMID:
15980379
PMCID:
PMC1168637
DOI:
10.1128/AAC.49.7.2983-2985.2005
[Indexed for MEDLINE]
Free PMC Article

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