关键词: Antibacterial agent Antibiotic adjuvant Bacterial resistance Response regulator Two-component system

Mesh : Anti-Bacterial Agents / pharmacology chemistry chemical synthesis Drug Resistance, Bacterial / drug effects Bacteria / drug effects Microbial Sensitivity Tests Molecular Structure Humans Adjuvants, Pharmaceutic / pharmacology chemistry

来  源:   DOI:10.1016/j.bioorg.2024.107606

Abstract:
The number of new antibacterial agents currently being discovered is insufficient to combat bacterial resistance. It is extremely challenging to find new antibiotics and to introduce them to the pharmaceutical market. Therefore, special attention must be given to find new strategies to combat bacterial resistance and prevent bacteria from developing resistance. Two-component system is a transduction system and the most prevalent mechanism employed by bacteria to respond to environmental changes. This signaling system consists of a membrane sensor histidine kinase that perceives environmental stimuli and a response regulator which acts as a transcription factor. The approach consisting of developing response regulators inhibitors with antibacterial activity or antibiotic adjuvant activity is a novel approach that has never been previously reviewed. In this review we report for the first time, the importance of targeting response regulators and summarizing all existing studies carried out from 2008 until now on response regulators inhibitors as antibacterial agents or / and antibiotic adjuvants. Moreover, we describe the antibacterial activity and/or antibiotic adjuvants activity against the studied bacterial strains and the mechanism of different response regulator inhibitors when it\'s possible.
摘要:
目前发现的新抗菌剂的数量不足以抵抗细菌耐药性。寻找新的抗生素并将其引入制药市场极具挑战性。因此,必须特别注意寻找新的策略来对抗细菌耐药性并防止细菌产生耐药性。双组分系统是一种转导系统,是细菌响应环境变化的最普遍的机制。该信号系统由感知环境刺激的膜传感器组氨酸激酶和充当转录因子的反应调节剂组成。由开发具有抗菌活性或抗生素佐剂活性的反应调节剂抑制剂组成的方法是一种以前从未被审查过的新方法。在这次审查中,我们首次报告,靶向反应调节剂的重要性,并总结了从2008年至今关于反应调节剂抑制剂作为抗菌剂或/和抗生素佐剂的所有现有研究。此外,我们描述了抗菌活性和/或抗生素佐剂活性对所研究的细菌菌株和不同的反应调节抑制剂的机制,当它是可能的。
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