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外排泵:它们在抗菌药物发现中的作用。

Efflux pumps: their role in antibacterial drug discovery.

作者信息

Lomovskaya O, Watkins W J

机构信息

Microcide Pharmaceuticals, Inc., 850 Maude Avenue, Mountain View, CA 94043, USA.

出版信息

Curr Med Chem. 2001 Dec;8(14):1699-711. doi: 10.2174/0929867013371743.

Abstract

The emergence of active efflux as a major causative factor in antibiotic resistance has been one of the most significant trends in antiinfective chemotherapy over the last decade. The phenomenon affects virtually all classes of antibiotics and frequently results in multi-drug resistant phenotypes. This review analyzes efflux pumps of clinical significance and examines their impact on different antibiotic classes relative to other mechanisms of resistance. Progress in strategies to combat efflux-mediated resistance by modification of existing antibiotics or identification of efflux pump inhibitors is also reviewed.

摘要

主动外排作为抗生素耐药性的主要致病因素出现,是过去十年抗感染化疗中最显著的趋势之一。这一现象几乎影响所有种类的抗生素,并常常导致多药耐药表型。本综述分析了具有临床意义的外排泵,并研究了它们相对于其他耐药机制对不同抗生素种类的影响。还综述了通过修饰现有抗生素或鉴定外排泵抑制剂来对抗外排介导的耐药性的策略进展。

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