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Comparison of efficacies of cysteine protease inhibitors against five strains of Plasmodium falciparum.

ABSTRACT: Falcipain-2, a cysteine protease and essential hemoglobinase of Plasmodium falciparum, is a potential antimalarial drug target. We compared the falcipain-2 sequences and sensitivities to cysteine protease inhibitors of five parasite strains that differ markedly in sensitivity to established antimalarial drugs. The sequence of falcipain-2 was highly conserved, and the sensitivities of all of the strains to falcipain-2 inhibitors were very similar. Thus, cross-resistance between cysteine protease inhibitors and other antimalarial agents is not expected in parasites that are now circulating and falcipain-2 remains a promising chemotherapeutic target.

SUBMITTER: Singh A

PROVIDER: S-EPMC90401 | biostudies-literature | 2001 Mar

REPOSITORIES: biostudies-literature

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Comparison of efficacies of cysteine protease inhibitors against five strains of Plasmodium falciparum.

Singh A A Rosenthal P J PJ

Antimicrobial agents and chemotherapy 20010301 3

Falcipain-2, a cysteine protease and essential hemoglobinase of Plasmodium falciparum, is a potential antimalarial drug target. We compared the falcipain-2 sequences and sensitivities to cysteine protease inhibitors of five parasite strains that differ markedly in sensitivity to established antimalarial drugs. The sequence of falcipain-2 was highly conserved, and the sensitivities of all of the strains to falcipain-2 inhibitors were very similar. Thus, cross-resistance between cysteine protease ...[more]

PMID: 11181388

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