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Leishmaniasis: efflux pumps and chemoresistance

机译:利什曼病:外排泵和化学耐药性

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Resistance of parasitic protozoa such as Leishmania to therapeutic drugs continues to escalate in developing countries. Treatment programs for human leishmaniasis are still based on pentavalent antimonials but resistance to these compounds has been a persistent problem. In many instances, resistance of the parasite is due to over-expressed ABC efflux pumps. In Leishmania different classes of ABC transporters extrude antimonials, azoles and folates resulting in drug-resistant phenotypes. Although some studies have focused on developing inhibitors against these resistant phenotypes, new efficient modulators that are able to inhibit drug efflux are needed. (C) 2003 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved. [References: 80]
机译:在发展中国家,诸如利什曼原虫这样的寄生原生动物对治疗药物的抵抗力继续上升。人类利什曼病的治疗方案仍基于五价锑,但对这些化合物的抗药性一直是一个持续的问题。在许多情况下,寄生虫的抵抗力是由于过表达的ABC外排泵。在利什曼原虫中,不同种类的ABC转运蛋白会挤出锑,唑类和叶酸,从而产生耐药性表型。尽管一些研究集中于开发针对这些抗性表型的抑制剂,但仍需要能够抑制药物外排的新型有效调节剂。 (C)2003年Elsevier B.V.和国际化学疗法学会。版权所有。 [参考:80]

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