title: Polymorphism in plasmodium falciparum drug transporter proteins and reversal of in vitro chloroquine resistance by a 9,10-dihydroethanoanthracene derivative.
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.
authors.affiliation: Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé Armées, Marseille, France
authors.forename: Julie
authors.initials: J
authors.lastname: Millet
authors.forename: Sandrine
authors.initials: S
authors.lastname: Alibert
authors.forename: Marylin
authors.initials: M
authors.lastname: Torrentino-Madamet
authors.forename: Christophe
authors.initials: C
authors.lastname: Rogier
authors.forename: Christiane
authors.initials: C
authors.lastname: Santelli-Rouvier
authors.forename: Patricia
authors.initials: P
authors.lastname: Bigot
authors.forename: Joel
authors.initials: J
authors.lastname: Mosnier
authors.forename: Eric
authors.initials: E
authors.lastname: Baret
authors.forename: Jacques
authors.initials: J
authors.lastname: Barbe
authors.forename: Daniel
authors.initials: D
authors.lastname: Parzy
authors.forename: Bruno
authors.initials: B
authors.lastname: Pradines
mesh_terms: D000818:Animals; D000873:Anthracenes / Q000494:pharmacology*; D000962:Antimalarials / Q000494:pharmacology*; D002352:Carrier Proteins / Q000235:genetics*; D002738:Chloroquine / Q000494:pharmacology*; D016054:DNA, Protozoan / Q000235:genetics / Q000302:isolation & purification; D004351:Drug Resistance; D004357:Drug Synergism; D019450:Genes, MDR / Q000235:genetics; D006801:Humans; D016778:Malaria, Falciparum / Q000469:parasitology; D008565:Membrane Proteins / Q000235:genetics; D026901:Membrane Transport Proteins; D009154:Mutation / Q000235:genetics; D010963:Plasmodium falciparum / Q000187:drug effects / Q000235:genetics* / Q000378:metabolism; D011110:Polymorphism, Genetic / Q000235:genetics*; D015800:Protozoan Proteins; D016053:RNA, Protozoan / Q000235:genetics / Q000302:isolation & purification; D020133:Reverse Transcriptase Polymerase Chain Reaction
chemical_list: D000873:Anthracenes; D000962:Antimalarials; C495224:BG 958; D002352:Carrier Proteins; D016054:DNA, Protozoan; D008565:Membrane Proteins; D026901:Membrane Transport Proteins; C416369:PfCRT protein, Plasmodium falciparum; D015800:Protozoan Proteins; D016053:RNA, Protozoan; D002738:Chloroquine