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Related Concept Videos

Antiepileptic Drugs: Potassium Channel Activators01:20

Antiepileptic Drugs: Potassium Channel Activators

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Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
Ezogabine has gained approval as an adjunctive treatment...
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Non-gated Ion Channels01:24

Non-gated Ion Channels

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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.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism....
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Non-gated Ion Channels01:24

Non-gated Ion Channels

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Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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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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Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein01:20

Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein

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Antiepileptic drugs, such as levetiracetam (Keppra) and brivaracetam (Briviact), have emerged as crucial tools in managing epilepsy. These medications exert their therapeutic effects by targeting the synaptic vesicle protein SV2A, a transmembrane glycoprotein primarily found in the brain.
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...
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Voltage-gated Ion Channels01:26

Voltage-gated Ion Channels

13.3K
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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Updated: Apr 5, 2026

Capturing the Interaction Kinetics of an Ion Channel Protein with Small Molecules by the Bio-layer Interferometry Assay
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Capturing the Interaction Kinetics of an Ion Channel Protein with Small Molecules by the Bio-layer Interferometry Assay

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EAG2 potassium channel with evolutionarily conserved function as a brain tumor target.

Xi Huang1,2, Ye He1,2, Adrian M Dubuc3

  • 1Howard Hughes Medical Institute, Department of Physiology, University of California, San Francisco, San Francisco, California, USA.

Nature Neuroscience
|August 11, 2015
PubMed
Summary
This summary is machine-generated.

Scientists discovered the EAG2 potassium channel drives brain tumor growth and metastasis. An existing drug, thioridazine, blocks this channel, reducing tumor progression in preclinical models and a human patient.

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Author Spotlight: Exploring the Role of Ion Channels in Cancer: Characterization and Potential Treatment Approaches
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Author Spotlight: Exploring the Role of Ion Channels in Cancer: Characterization and Potential Treatment Approaches
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Area of Science:

  • Oncology
  • Neuroscience
  • Molecular Biology

Background:

  • Ion channels are crucial drug targets, yet none are FDA-approved for cancer.
  • The EAG2 potassium channel's role in cancer, particularly brain tumors, is largely unexplored.

Observation:

  • EAG2 potassium channel is essential for brain tumor growth and metastasis.
  • EAG2 localizes to the trailing edge of migrating medulloblastoma cells, influencing cell volume and motility.

Findings:

  • EAG2 potassium channel functionally cooperates with other potassium channels to regulate cell volume during mitosis and tumor progression.
  • The FDA-approved drug thioridazine effectively blocks EAG2 channels, inhibiting medulloblastoma growth and metastasis in preclinical models.
  • A case study demonstrates thioridazine's potential in treating a human patient with medulloblastoma.

Implications:

  • Targeting the EAG2 potassium channel represents a novel therapeutic strategy for brain cancers.
  • Drug repurposing of thioridazine offers a potential new treatment avenue for medulloblastoma.
  • This research highlights the broader potential of targeting ion channels in cancer therapy.