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Related Concept Videos

Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

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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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Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
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Non-gated Ion Channels01:24

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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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Voltage-gated Ion Channels01:26

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Voltage-gated ion channels are transmembrane proteins that open and close in response to changes in the membrane potential. They are present on the membranes of all electrically excitable cells such as neurons, heart, and muscle cells.
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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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Acid-sensing ion channels as potential therapeutic targets.

Stephanie A Heusser1, Stephan A Pless1

  • 1Department for Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.

Trends in Pharmacological Sciences
|October 22, 2021
PubMed
Summary

Acid-sensing ion channels (ASICs) show therapeutic potential for diseases like stroke and pain. Developing selective ASIC modulators faces challenges but offers future treatment opportunities.

Keywords:
animal modelsischemialigand-gated ion channelpainpharmacological targetingstroke

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Physiology

Background:

  • Tissue acidification is linked to various diseases.
  • Acid-sensing ion channels (ASICs) detect pH changes and are potential drug targets.
  • ASICs are implicated in conditions including ischemic stroke, pain, anxiety, and cardiac issues.

Purpose of the Study:

  • To review recent animal study insights on ASIC therapeutic potential.
  • To assess ASICs for treating ischemic stroke, pain, anxiety, and cardiac pathologies.
  • To identify challenges in developing ASIC-targeting drugs.

Main Methods:

  • Review of recent animal studies.
  • Analysis of ASIC modulators (small molecules and biopharmaceuticals).
  • Evaluation of therapeutic potential in disease models.

Main Results:

  • ASICs demonstrate potential in preclinical models of stroke, pain, anxiety, and cardiac disease.
  • Various modulators exist, but challenges in selectivity and potency remain.
  • Animal studies provide valuable insights into ASIC function and therapeutic relevance.

Conclusions:

  • ASICs are promising therapeutic targets for multiple disease states.
  • Further research is needed to overcome challenges in developing selective ASIC modulators.
  • Targeting ASICs could lead to novel treatments for significant health conditions.