Switchable foldamer ion channels with antibacterial activity

Anna D. Peters, Stefan Borsley, Flavio Della Sala, Dominic F. Cairns-Gibson, Marios Leonidou, Jonathan Clayden, George F.S. Whitehead, Iñigo J. Vitórica-Yrezábal, Eriko Takano, John Burthem, Scott L. Cockroft, Simon J. Webb*

*Corresponding author for this work

Research output: Contribution to journalArticle (Academic Journal)

1 Citation (Scopus)
18 Downloads (Pure)

Abstract

Synthetic ion channels may have applications in treating channelopathies and as new classes of antibiotics, particularly if ion flow through the channels can be controlled. Here we describe triazole-capped octameric α-aminoisobutyric acid (Aib) foldamers that “switch on” ion channel activity in phospholipid bilayers upon copper(II) chloride addition; activity is “switched off” upon copper(II) extraction. X-ray crystallography showed that CuCl2 complexation gave chloro-bridged foldamer dimers, with hydrogen bonds between dimers producing channels within the crystal structure. These interactions suggest a pathway for foldamer self-assembly into membrane ion channels. The copper(II)-foldamer complexes showed antibacterial activity against B. megaterium strain DSM319 that was similar to the peptaibol antibiotic alamethicin, but with 90% lower hemolytic activity.
Original languageEnglish
Pages (from-to)7023-7030
Number of pages8
JournalChemical Science
Volume11
Issue number27
DOIs
Publication statusPublished - 21 Jul 2020

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