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Drug transport and drug resistance in African trypanosomes.
- Source :
-
Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy [Drug Resist Updat] 2003 Oct; Vol. 6 (5), pp. 281-90. - Publication Year :
- 2003
-
Abstract
- 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.
- Subjects :
- Animals
Biological Transport genetics
Structure-Activity Relationship
Switzerland
Trypanocidal Agents chemistry
Trypanocidal Agents pharmacology
Trypanosoma brucei gambiense drug effects
Trypanosoma brucei gambiense genetics
Trypanosoma brucei gambiense metabolism
Trypanosoma brucei rhodesiense drug effects
Trypanosoma brucei rhodesiense genetics
Trypanosoma brucei rhodesiense metabolism
Trypanosomiasis, African genetics
Trypanosomiasis, African metabolism
Biological Transport drug effects
Drug Resistance drug effects
Trypanosomiasis, African drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1368-7646
- Volume :
- 6
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy
- Publication Type :
- Academic Journal
- Accession number :
- 14643298
- Full Text :
- https://doi.org/10.1016/j.drup.2003.09.001