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

被引:11
|
作者
Millet, J
Alibert, S
Torrentino-Madamet, M
Rogier, C
Santelli-Rouvier, C
Bigot, P
Mosnier, J
Baret, E
Barbe, J
Parzy, D
Pradines, B
机构
[1] IMTSSA, Unite Parasitol, F-13998 Marseille, France
[2] GERCTOP, Fac Pharm, CNRS, UMR 6009, Marseille, France
[3] Inst Fed Rech 48, Marseille, France
关键词
D O I
10.1128/AAC.48.12.4869-4872.2004
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
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.
引用
收藏
页码:4869 / 4872
页数:4
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