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A class of unimolecular channels formed by pillararene-gramicidin hybrid molecules are presented. The charge status of the peptide domain in these channels has a significant impact on their ion transport and antimicrobial activity. These channels exhibited different membrane-association abilities between microbial cells and mammalian cells. One of the channels displayed a higher antimicrobial activity towards S. aureus (IC50 = 0.55 μM) and negligible hemolytic toxicity, showing potential to serve as a systemic antibiotic.


Pengyang Xin, Lingyu Zhao, Linlin Mao, Linqi Xu, Shuaimin Hou, Huiyuan Kong, Haodong Fang, Haofeng Zhu, Tao Jiang, Chang-Po Chen. Effect of charge status on the ion transport and antimicrobial activity of synthetic channels. Chemical communications (Cambridge, England). 2020 Nov 18;56(89):13796-13799

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PMID: 33078782

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