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Volume 209, 2018
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A synthetic channel that efficiently inserts into mammalian cell membranes and destroys cancer cells

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Abstract

Despite the fact that a large number of synthetic channels have been developed in the last three decades, few of them can function in mammalian cell membranes because of their weak membrane insertion abilities. This study describes a tubular molecule with terminal positively charged amino groups that displays a strong ability to insert into lipid bilayers composed of phosphatidylcholine and consequently forming unimolecular transmembrane channels. It has been demonstrated that the insertion of the channel into the phosphatidylcholine bilayers was driven by the electrostatic interaction between the positively charged amino groups of the channel molecules and the negatively charged phosphate groups of the lipid molecules. The high affinity of the channels for lipid bilayers led to efficient mammalian cell membrane insertion. The channels showed high effective activity against HepG2 cancer cells at concentrations above 5.1 μM.

Graphical abstract: A synthetic channel that efficiently inserts into mammalian cell membranes and destroys cancer cells

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Publication details

The article was received on 31 Jan 2018, accepted on 21 Mar 2018 and first published on 21 Mar 2018


Article type: Paper
DOI: 10.1039/C8FD00009C
Citation: Faraday Discuss., 2018,209, 149-159
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    A synthetic channel that efficiently inserts into mammalian cell membranes and destroys cancer cells

    J. Chen, W. Haoyang, M. Zhang, G. Wu, Z. Li and J. Hou, Faraday Discuss., 2018, 209, 149
    DOI: 10.1039/C8FD00009C

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