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首页> 外文期刊>Recent patents on anti-infective drug discovery >Bacterial efflux pumps involved in multidrug resistance and their inhibitors: Rejuvinating the antimicrobial chemotherapy
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Bacterial efflux pumps involved in multidrug resistance and their inhibitors: Rejuvinating the antimicrobial chemotherapy

机译：涉及多药耐药性的细菌外排泵及其抑制剂：重振抗菌化学疗法

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Active efflux of antibiotics is one of the major mechanisms of drug resistance in bacteria. The efflux process is mediated by membrane transporters with a large variety of unrelated compounds as their substrates. Though these pumps are responsible for the low intrinsic resistance of a bacterium to a drug, their overexpression, accumulation of mutations in these proteins and their synergy with other drug resistance mechanisms hampers effective antimicrobial treatment. As efflux pumps have been reported to play vital roles in mediating multidrug resistance in clinical isolates from varied geographic locations and varied populations, the inhibition of efflux pumps appears to be an attractive approach to combat the problem of drug resistance. Efflux pump inhibitors can be utilized for increasing the antibiotic concentration inside a pathogenic cell making these drugs more effective, reduce the accumulation of other resistance mechanisms in a cell and for diagnostic purposes to evaluate the presence and contribution of the efflux mechanism in a pathogen. A large number of inhibitors have been discovered and patented in last two decades but the process of discovery, testing and commercialization is rather slow. Some of the important inhibitors include the energy decouplers, phenothiazines, analogs of popular antibiotics, inhibitors of serotonin re-uptake, to name a few, that have been used as adjuvants in the antimicrobial chemotherapy to potentiate the activity of some important antimicrobials in deadly pathogens that have worried the mankind since long. This review describes the role of efflux pumps in governing the resistance phenotype of a pathogen, efflux pumps found in bacteria and the efflux pump inhibitors that have been studied and patented so far.
机译：抗生素的主动外排是细菌耐药性的主要机制之一。外排过程是由膜转运蛋白介导的，这些膜转运蛋白以各种各样的无关化合物为底物。尽管这些泵导致细菌对药物的低内在抗性，但是它们的过表达，这些蛋白质中突变的积累以及它们与其他抗药性机制的协同作用阻碍了有效的抗菌治疗。据报道，外排泵在介导来自不同地理位置和不同人群的临床分离物中的多药耐药性中起着至关重要的作用，抑制外排泵似乎是解决耐药性问题的一种有吸引力的方法。外排泵抑制剂可用于增加致病细胞内的抗生素浓度，使这些药物更有效，减少细胞中其他耐药机制的积累，并用于诊断目的以评估外泄机制在病原体中的存在和贡献。在过去的二十年中，已经发现了大量抑制剂并申请了专利，但是发现，测试和商业化的过程相当缓慢。一些重要的抑制剂包括能量解偶联剂，吩噻嗪，流行抗生素的类似物，血清素再摄取抑制剂（仅举几例），已被用作抗微生物化学疗法的佐剂，以增强致命病原体中某些重要抗微生物剂的活性。长期以来一直困扰着人类。这篇综述描述了外排泵在控制病原体的耐药表型中的作用，细菌中发现的外排泵以及迄今为止已获得专利的外排泵抑制剂。

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