Quorum sensing inhibitors: a patent review (2014-2018)

被引:56
|
作者
Chen, Xin [1 ]
Zhang, Likun [1 ]
Zhang, Mingxiang [1 ]
Liu, Huayu [1 ]
Lu, Panrui [1 ]
Lin, Kejiang [1 ]
机构
[1] China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Jiangsu, Peoples R China
基金
国家重点研发计划;
关键词
Quorum sensing; inhibitor; antibacterial; biofilm formation; acyl-homoserine lactones; autoinducer peptides; autoinducer-2; PSEUDOMONAS-AERUGINOSA; TRANSCRIPTIONAL ACTIVATOR; VIRULENCE REGULATION; SENSOR KINASE; DSF-FAMILY; GENE; SYSTEM; IDENTIFICATION; BIOSYNTHESIS; PRINCIPLES;
D O I
10.1080/13543776.2018.1541174
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Introduction: Quorum sensing (QS) is a cell density-dependent phenomenon in which specific pathways are activated after autoinducers (AIs) outside the microorganism reach a threshold concentration. QS creates a positive feedback loop that induces a cascade of gene expression and causes biofilm formation, virulence and sporulation. QS signals are diverse, acyl-homoserine lactone (AHL), AI peptide (AIP) and AI-2 are three major categories of QS signals. QS inhibitors (QSIs) can disrupt or prevent the formation of biofilm and reduce virulence while exerting less selective pressure on the bacteria, suggesting that QSIs are potential alternatives for antibiotics. Areas covered: This review summarized the pertinent patents on QS inhibition available from 2014 to 2018. The authors analyze these patents and provided an overview of them and their potential applications. Expert opinion: The main strategy for QS inhibition is to use the analogues of various QS signals to block downstream signal transducers. The inactivation of signal molecules or the stimulation of the immune response is also attractive strategies to inhibit QS. However, additional clinical trials are needed to assess their efficacy in mammals. In sum, QS inhibition can reduce the virulence of bacteria without affecting their growth or killing them and the reduced pressure may minimize the increasingly resistance.
引用
收藏
页码:849 / 865
页数:17
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