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Related Concept Videos

Voltage-gated Ion Channels01:26

Voltage-gated Ion Channels

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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.
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several types of...
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Voltage-gated Ion Channels01:26

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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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Mechanically-gated Ion Channels01:12

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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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Isolating and Culturing Vestibular and Spiral Ganglion Somata from Neonatal Rodents for Patch-Clamp Recordings
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Voltage-gated sodium channels.

Kevin Kwong1, Michael J Carr1

  • 1GSK, King of Prussia, PA 19406, USA.

Current Opinion in Pharmacology
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Summary
This summary is machine-generated.

Selective voltage-gated sodium channel blockers are being developed to treat various conditions. Advances in human channelopathies, animal toxins, and channel structure research are key to creating these targeted therapies.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Voltage-gated sodium channels (VGSCs) are crucial for transmitting peripheral sensory information.
  • Specific distributions of VGSC isoforms in sensory fibers present therapeutic opportunities.
  • Inappropriate signaling via VGSCs is implicated in numerous clinical conditions.

Purpose of the Study:

  • To review recent advancements relevant to the development of selective VGSC blockers.
  • To highlight the role of human channelopathies, animal toxins, and channel structure in this field.

Main Methods:

  • Review of current literature on human channelopathies.
  • Analysis of research on animal toxins targeting VGSCs.
  • Examination of studies on VGSC structure and function.

Main Results:

  • Recent studies provide insights into VGSC isoform-specific functions.
  • Understanding channelopathies and toxin mechanisms informs drug design.
  • Structural biology advances reveal potential binding sites for selective blockers.

Conclusions:

  • Targeting specific VGSC isoforms holds promise for novel therapeutics.
  • Interdisciplinary research is accelerating the development of selective VGSC inhibitors.
  • Further investigation into channel structure and function will refine drug discovery efforts.