Drug transport and drug resistance in African trypanosomes

被引：52
作者：
Mäser, P
Lüscher, A
Kaminsky, R [1 ]
机构：
[1] Novartis Anim Hlth, Ctr Rech Sante Anim, CH-1566 St Aubin, Switzerland
[2] Univ Bern, Inst Cell Biol, CH-3012 Bern, Switzerland
来源：
DRUG RESISTANCE UPDATES | 2003年 / 6卷 / 05期
关键词：
Trypanosoma brucei; sleeping sickness; melarsoprol; pentamidine; adenosine;
D O I：
10.1016/j.drup.2003.09.001
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Drug resistance in African trypanosomes has been studied for almost a hundred years. Beginning with Paul Ehrlich's work that led to the chemoreceptor hypothesis, reduction of net drug uptake has emerged as the most frequent cause of resistance. This review, therefore, focuses on trypanosomal drug transporter genes. TbAT1 encodes purine permease P2, which mediates influx of melarsoprol and diamidines. Disruption of TbAT1 in Trypanosoma brucei reduced sensitivity to these trypanocides. TbMRPA encodes a putative trypanothione-conjugate efflux pump, and overexpression of TbMRPA in T brucei causes melarsoprol resistance. It will be important to determine the role of TbAT1 and TbMRPA in sleeping sickness treatment failures. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码：281 / 290
页数：10
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