title: Voltage-driven reversible insertion into and leaving from a lipid bilayer: tuning transmembrane transport of artificial channels.
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.
authors.affiliation: Department of Chemistry, Fudan University, 220 Handan Road, Shanghai 200433 (China).
authors.forename: Wen
authors.initials: W
authors.lastname: Si
authors.forename: Zhan-Ting
authors.initials: ZT
authors.lastname: Li
authors.forename: Jun-Li
authors.initials: JL
authors.lastname: Hou
mesh_terms: D000408:Alamethicin / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D001412:Bacillus subtilis / Q000187:drug effects*; D001692:Biological Transport; D047250:Calixarenes; D004553:Electric Conductivity; D015640:Ion Channel Gating; D007473:Ion Channels / Q000502:physiology*; D008051:Lipid Bilayers / Q000737:chemistry*; D008564:Membrane Potentials; D010446:Peptide Fragments / Q000494:pharmacology*; D011188:Potassium / Q000378:metabolism*; D000644:Quaternary Ammonium Compounds / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D007473:Ion Channels; D008051:Lipid Bilayers; D010446:Peptide Fragments; D000644:Quaternary Ammonium Compounds; C570642:pillar(5)arene; D047250:Calixarenes; D000408:Alamethicin; D011188:Potassium
keywords: artificial channels; lipid bilayers; transmembrane transport; vesicles; voltage gating