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Ligand-gated synthetic ion channels.
Journal article

Ligand-gated synthetic ion channels.

  • 2005-08-25
Published in:
  • Chemistry (Weinheim an der Bergstrasse, Germany). - 2005
Crystallography, X-Ray
DNA
Ion Channel Gating
Ion Channels
Ligands
Lipid Bilayers
Models, Molecular
Molecular Structure
English Supramolecular pi-stack architecture is fundamental in DNA chemistry but absent in biological and synthetic ion channels and pores. Here, a novel rigid-rod pi-stack architecture is introduced to create synthetic ion channels with characteristics that are at the forefront of rational design, that is, ligand gating by a conformational change of the functional supramolecule. Namely, the intercalation of electron-rich aromatics is designed to untwist inactive electron-poor helical pi-stacks without internal space into open barrel-stave ion channels. Conductance experiments in planar lipid bilayers corroborate results from spherical bilayers and molecular modeling: Highly cooperative and highly selective ligand gating produces small, long-lived, weakly anion selective, ohmic ion channels. Structural studies conducted under conditions relevant for function provide experimental support for helix-barrel transition as origin of ligand gating. Control experiments demonstrate that minor structural changes leading to internal decrowding suffice to cleanly annihilate chiral self-organization and function.
Language
  • English
Open access status
closed
Identifiers
Persistent URL
https://sonar.ch/global/documents/49835
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