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Related Concept Videos

Ion Channels01:19

Ion Channels

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The movement of ions like sodium, potassium, and calcium into and out of the cell is essential to maintain the electrochemical gradient in living cells. The ion channels—a class of membrane transport proteins—help maintain this ionic gradient for the smooth functioning of physiological activities such as maintaining cell size and volume, conducting nerve impulses, and gas and nutrient exchange.
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Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
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Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
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Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
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Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
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A Proteoliposome-Based Efflux Assay to Determine Single-molecule Properties of Cl- Channels and Transporters
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Switchable foldamer ion channels with antibacterial activity.

Anna D Peters1,2, Stefan Borsley1,3, Flavio Della Sala1,2

  • 1Department of Chemistry , University of Manchester , Oxford Road , Manchester M13 9PL , UK .

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Researchers developed synthetic ion channels using alpha-aminoisobutyric acid (Aib) foldamers. These novel channels switch ion flow on with copper(II) and off with its removal, showing promise as antibiotics.

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Area of Science:

  • Biomimetic chemistry
  • Membrane biophysics
  • Synthetic biology

Background:

  • Ion channels are crucial for cellular function.
  • Channelopathies and antibiotic resistance necessitate novel therapeutic agents.
  • Controllable synthetic ion channels offer potential therapeutic applications.

Purpose of the Study:

  • To design and characterize novel synthetic ion channels with controllable activity.
  • To investigate the self-assembly mechanism of foldamers into membrane channels.
  • To evaluate the therapeutic potential of these foldamers as antibiotics.

Main Methods:

  • Synthesis of triazole-capped octameric alpha-aminoisobutyric acid (Aib) foldamers.
  • Incorporation of foldamers into phospholipid bilayers.
  • Induction and inhibition of ion channel activity using copper(II) chloride.
  • X-ray crystallography for structural analysis.
  • Antibacterial and hemolytic activity assays.

Main Results:

  • Foldamers formed controllable ion channels in phospholipid bilayers, activated by CuCl2.
  • X-ray crystallography revealed CuCl2-mediated foldamer dimerization and self-assembly into channels.
  • The copper(II)-foldamer complexes exhibited potent antibacterial activity against B. megaterium.
  • Hemolytic activity was significantly lower (90% reduction) compared to alamethicin.

Conclusions:

  • Copper(II)-triggered foldamer self-assembly provides a mechanism for controllable synthetic ion channels.
  • These foldamers represent a promising new class of antibiotics with reduced toxicity.
  • The findings open avenues for developing targeted therapies for channelopathies and infections.