Voltage-driven reversible insertion into and leaving from a lipid bilayer: tuning transmembrane transport of artificial channels

Angew Chem Int Ed Engl. 2014 Apr 25;53(18):4578-81. doi: 10.1002/anie.201311249. Epub 2014 Mar 28.

Abstract

Three new artificial transmembrane channel molecules have been designed and synthesized by attaching positively charged Arg-incorporated tripeptide chains to pillar[5]arene. Fluorescent and patch-clamp experiments revealed that voltage can drive the molecules to insert into and leave from a lipid bilayer and thus switch on and off the transport of K(+) ions. One of the molecules was found to display antimicrobial activity toward Bacillus subtilis with half maximal inhibitory concentration (IC50 ) of 10 μM which is comparable to that of natural channel-forming peptide alamethicin.

Keywords: artificial channels; lipid bilayers; transmembrane transport; vesicles; voltage gating.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alamethicin / pharmacology
  • Anti-Bacterial Agents / pharmacology
  • Bacillus subtilis / drug effects*
  • Biological Transport
  • Calixarenes
  • Electric Conductivity*
  • Ion Channel Gating
  • Ion Channels / physiology*
  • Lipid Bilayers / chemistry*
  • Membrane Potentials
  • Peptide Fragments / pharmacology*
  • Potassium / metabolism*
  • Quaternary Ammonium Compounds / chemistry*

Substances

  • Anti-Bacterial Agents
  • Ion Channels
  • Lipid Bilayers
  • Peptide Fragments
  • Quaternary Ammonium Compounds
  • pillar(5)arene
  • Calixarenes
  • Alamethicin
  • Potassium