Crown ether helical peptides are preferentially inserted in lipid bilayers as a transmembrane ion channels. Issue 4 (July 2015) - Savoie, Jean‐Daniel
ABSTRACT: Oriented circular dichroism was used to study the alignment crown ether‐modified peptides. The influence of different N‐ and C‐functionalities was assessed using at variable peptide:lipid ratios from 1:20 to 1:200. Neither the functionalities nor the concentration had any major effect on the orientation. The alignment of the 21‐mer peptides was also examined with lipid membranes of different bilayer thickness. The use of synchrotron radiation as light source allowed the study of peptide:lipid molar ratios from 1:20 to 1:1000. For all conditions studied, the peptides were found to be predominantly incorporated as a transmembrane helix into the membrane, especially at low peptide concentration, but started to aggregate on the membrane surface at higher peptide:lipid ratios. The structural information on the preferred trans‐bilayer alignment of the crown ether functional groups explains their ion conductivity and is useful for the further development of membrane‐active nanochemotherapeutics. © 2015 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 104: 427–433, 2015.