Polymorphism in plasmodium falciparum drug transporter proteins and reversal of in vitro chloroquine resistance by a 9,10-dihydroethanoanthracene derivative.

Julie Millet, Sandrine Alibert, Marylin Torrentino-Madamet, Christophe Rogier, Christiane Santelli-Rouvier, Patricia Bigot, Joel Mosnier, Eric Baret, Jacques Barbe, Daniel Parzy, Bruno Pradines

Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé Armées, Marseille, France

Antimicrobial agents and chemotherapy 2004 Dec

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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.

Citation

Julie Millet, Sandrine Alibert, Marylin Torrentino-Madamet, Christophe Rogier, Christiane Santelli-Rouvier, Patricia Bigot, Joel Mosnier, Eric Baret, Jacques Barbe, Daniel Parzy, Bruno Pradines. Polymorphism in plasmodium falciparum drug transporter proteins and reversal of in vitro chloroquine resistance by a 9,10-dihydroethanoanthracene derivative. Antimicrobial agents and chemotherapy. 2004 Dec;48(12):4869-72