Strategies and Approaches for Discovery of Small Molecule Disruptors of Biofilm Physiology.

Strategies and Approaches for Discovery of Small Molecule Disruptors of Biofilm Physiology.
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生物膜生理小分子破坏剂的发现策略和方法。

DOI:
10.3390/molecules26154582
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发表时间:
2021-07-29
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Yildiz FH
Yildiz FH
中科院分区:
其他
文献类型:
--
作者:
Trebino MA;Shingare RD;MacMillan JB;Yildiz FH

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生物膜是微生物的主要生长方式,对人类健康构成重大威胁。保护性生物膜基质通常由外多糖、蛋白质、核酸和脂质组成,结合生物膜培养的细菌的异质性生理机能,增强了对传统治疗方法的适应性和耐受性。有必要使用不同的方法和针对生物膜形成的不同阶段来识别生物膜抑制剂。这篇综述讨论了成功识别各种抑制剂的发现策略,以及用于表征其抑制机制和进一步改进的过程。此外,我们还研究了其中一些抑制剂的构效关系(SAR),以优化抑制剂的活性。
Biofilms, the predominant growth mode of microorganisms, pose a significant risk to human health. The protective biofilm matrix, typically composed of exopolysaccharides, proteins, nucleic acids, and lipids, combined with biofilm-grown bacteria’s heterogenous physiology, leads to enhanced fitness and tolerance to traditional methods for treatment. There is a need to identify biofilm inhibitors using diverse approaches and targeting different stages of biofilm formation. This review discusses discovery strategies that successfully identified a wide range of inhibitors and the processes used to characterize their inhibition mechanism and further improvement. Additionally, we examine the structure–activity relationship (SAR) for some of these inhibitors to optimize inhibitor activity.
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