Enhanced Activity against Multi-drug Resistant Bacteria through Coapplication of an Analogue of Tachyplesin I and an Inhibitor of the QseC/B Signaling Pathway.

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ID: 92801
2020
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Abstract
Tachyplesin I (TPI) is a cationic β-hairpin antimicrobial peptide with broad-spectrum, potent antimicrobial activity. In this study the all D-amino acid analog of TPI (TPAD) was synthesized, and its structure and activity were determined. TPAD has comparable antibacterial activity to TPI on 14 bacterial strains, including four drug-resistant bacteria. Importantly, TPAD has significantly improved stability against enzymatic degradation and decreased hemolytic activity compared to TPI, indicating that it has better therapeutic potential. The induction of bacterial resistance using low concentrations of TPAD resulted in activation of the QseC/B two-component system. Deletion of this system resulted in at least five-fold improvement of TPAD activity, and the combined use of TPAD with LED209, a QseC/B inhibitor, significantly enhanced the bactericidal effect against three classes of multi-drug resistant bacteria.
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yu2020enhancedjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Yu, Rilei;Wang, Jiayi;So, Lok-Yan;Harvey, Peta J;Shi, Juan;Liang, Jiazhen;Dou, Qin;Li, Xiao;Yan, Xiayi;Huang, Yen-Hua;Xu, Qingliang;Kaas, Quentin;Chow, Ho-Yin;Wong, Kwok-Yin;Craik, David J;Zhang, Xiaohua;Jiang, Tao;Wang, Yan;
Journal Journal of medicinal chemistry
Year 2020
DOI
10.1021/acs.jmedchem.9b01563
URL
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