Abstract
BG958 reverses resistance in chloroquine-resistant isolates from different countries. Five mutations in the Plasmodium falciparum crt (pfcrt) gene resulting in the amino acid changes K76T, M74I, N75E, A220S, and R371I are systematically identified in resistance-reversed Asian, African, and Brazilian parasites which possess the pfcrt (CIET) haplotype. In combination with BG958, the activity of chloroquine is increased in parasites with the N86Y mutation in pfmdr1.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anthracenes / pharmacology*
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Antimalarials / pharmacology*
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Carrier Proteins / genetics*
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Chloroquine / pharmacology*
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DNA, Protozoan / genetics
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DNA, Protozoan / isolation & purification
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Drug Resistance
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Drug Synergism
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Genes, MDR / genetics
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Humans
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Malaria, Falciparum / parasitology
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Membrane Proteins / genetics
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Membrane Transport Proteins
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Mutation / genetics
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Plasmodium falciparum / drug effects
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Plasmodium falciparum / genetics*
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Plasmodium falciparum / metabolism
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Polymorphism, Genetic / genetics*
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Protozoan Proteins
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RNA, Protozoan / genetics
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RNA, Protozoan / isolation & purification
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Reverse Transcriptase Polymerase Chain Reaction
Substances
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Anthracenes
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Antimalarials
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BG 958
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Carrier Proteins
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DNA, Protozoan
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Membrane Proteins
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Membrane Transport Proteins
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PfCRT protein, Plasmodium falciparum
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Protozoan Proteins
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RNA, Protozoan
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Chloroquine