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摘要
抗菌素耐药性对未来的医疗保健提供是一个重大的挑战。首字母缩略词ESKAPEE来源于生物公认的主要威胁的名字,虽然有许多其他的生物,特别是淋病奈瑟菌,已经在临床治疗同样具有挑战性。这些病原体的特点是能够迅速发展和/或获得耐药机制,以暴露于不同的抗菌剂。这些病原体的军械库的一个关键部分是一系列的外排泵,从而有效地排除或减少细胞内大量的抗生素浓度,使病原体更有耐药性。这些外排泵是相当重要的话题,无论是从基本的了解外排泵功能,和其作用的药物耐药性,还是作为新的辅助疗法的发展目标。克服抗菌素耐药性的必要性,鼓励调查的抗蚀性改变外排泵抑制剂,阻止药物挤压的机制,从而恢复抗菌药物的敏感性,并将现有的抗生素进入临床。一个更大的理解由多重耐药外排泵的药物识别和运输需要开发临床上有用的抑制剂,鉴于分子的宽度,可以由这些系统流出。本文综述了起源从天然来源和化学合成不同的细菌流出物射流泵抑制剂,探讨面临的挑战成功的流出物射流泵抑制剂,可以用于抗多药耐药菌的设计。
关键词: 抗菌素耐药性,外排泵抑制剂,合理的药物设计,药物化学优化,多排系统,计算方法。
Current Medicinal Chemistry
Title:Current Advances in Developing Inhibitors of Bacterial Multidrug Efflux Pumps
Volume: 23 Issue: 10
Author(s): Hannah Y. Mahmood, Shirin Jamshidi, J. Mark Sutton, Khondaker M. Rahman
Affiliation:
关键词: 抗菌素耐药性,外排泵抑制剂,合理的药物设计,药物化学优化,多排系统,计算方法。
摘要:
Antimicrobial resistance represents a significant challenge to future healthcare provision.An acronym ESKAPEE has been derived from the names of the organisms recognised as the major threats although there are a number of other organisms, notably Neisseria gonorrhoeae, that have become equally challenging to treat in the clinic. These pathogens are characterised by the ability to rapidly develop and/or acquire resistance mechanisms in response to exposure to different antimicrobial agents. A key part of the armoury of these pathogens is a series of efflux pumps, which effectively exclude or reduce the intracellular concentration of a large number of antibiotics, making the pathogens significantly more resistant. These efflux pumps are the topic of considerable interest, both from the perspective of basic understanding of efflux pump function, and its role in drug resistance but also as targets for the development of novel adjunct therapies. The necessity to overcome antimicrobial resistance has encouraged investigations into the characterisation of resistance-modifying efflux pump inhibitors to block the mechanisms of drug extrusion, thereby restoring antibacterial susceptibility and returning existing antibiotics into the clinic. A greater understanding of drug recognition and transport by multidrug efflux pumps is needed to develop clinically useful inhibitors, given the breadth of molecules that can be effluxed by these systems. This review discusses different bacterial EPIs originating from both natural source and chemical synthesis and examines the challenges to designing successful EPIs that can be useful against multidrug resistant bacteria.
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Hannah Y. Mahmood, Shirin Jamshidi, J. Mark Sutton, Khondaker M. Rahman , Current Advances in Developing Inhibitors of Bacterial Multidrug Efflux Pumps, Current Medicinal Chemistry 2016; 23 (10) . https://dx.doi.org/10.2174/0929867323666160304150522
DOI https://dx.doi.org/10.2174/0929867323666160304150522 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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