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.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antimalarials / pharmacology*
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Cysteine Endopeptidases / drug effects
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Cysteine Endopeptidases / genetics
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Cysteine Endopeptidases / metabolism
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Cysteine Proteinase Inhibitors / pharmacology*
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DNA, Protozoan / analysis
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Drug Evaluation, Preclinical
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Molecular Sequence Data
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Plasmodium falciparum / drug effects*
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Plasmodium falciparum / enzymology
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Plasmodium falciparum / genetics
Substances
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Antimalarials
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Cysteine Proteinase Inhibitors
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DNA, Protozoan
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Cysteine Endopeptidases
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falcipain 2
Associated data
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GENBANK/AF282975
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GENBANK/AF282976
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GENBANK/AF282977
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GENBANK/AF282978
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GENBANK/AF282979