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Pseudomonas aeruginosa Quorum Sensing Systems as Drug Discovery Targets: Current Position and Future Perspectives

机译:假单胞菌铜绿假单胞菌对药物发现目标:当前的位置和未来的观点

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摘要

Antimicrobial resistance (AMR) is a serious threat to public health globally, manifested by the frequent emergence of multidrug resistant pathogens that render current chemotherapy inadequate. Health organizations worldwide have recognized the severity of this crisis and implemented action plans to contain its adverse consequences and prolong the utility of conventional antibiotics. Hence, there is a pressing need for new classes of antibacterial agents with novel modes of action. Quorum sensing (QS), a communication system employed by bacterial populations to coordinate virulence gene expression, is a potential target that has been intensively investigated over the past decade. This Perspective will focus on recent advances in targeting the three main quorum sensing systems (las, rhl, and pqs) of a major opportunistic human pathogen, Pseudomonas aeruginosa, and will specifically evaluate the medicinal chemistry strategies devised to develop QS inhibitors from a drug discovery perspective.
机译:抗微生物抗性(AMR)是全球对公共健康的严重威胁,表现为多药抗性病原体的频繁出现,使电流化疗不足。全球卫生组织认识到这场危机的严重程度并实施了遏制其不利后果和延长常规抗生素的效用的行动计划。因此,对具有新型作用方式的新类别的抗菌剂进行了压迫需求。仲裁感测(QS),由细菌群体采用以协调毒力基因表达的通信系统,是在过去十年中被密集地研究的潜在目标。这种观点将侧重于终止瞄准主要机会人体病原体,假单胞菌铜绿假单胞菌的三个主要批量传感系统(LAS,RHL和PQ),并将特别评估设计的药物化学策略,从药物发现中发展QS抑制剂看法。

著录项

  • 来源
    《Journal of Medicinal Chemistry》 |2018年第23期|共18页
  • 作者单位

    Univ Nottingham Ctr Biomol Sci Sch Life Sci Nottingham NG7 2RD England;

    Univ Nottingham Ctr Biomol Sci Sch Life Sci Nottingham NG7 2RD England;

    Univ Nottingham Ctr Biomol Sci Sch Pharm Nottingham NG7 2RD England;

    Univ Nottingham Ctr Biomol Sci Sch Life Sci Nottingham NG7 2RD England;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

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