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Related Concept Videos

GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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...
Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
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Non-gated Ion Channels01:24

Non-gated Ion Channels

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.
Non-gated Ion Channels01:24

Non-gated Ion Channels

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.
Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

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.
Three Subfamilies of Ligand-gated Ion Channels
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 include the...

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Related Experiment Video

Updated: Jul 6, 2026

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
12:09

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Published on: December 31, 2013

TRPV1 shows dynamic ionic selectivity during agonist stimulation.

Man-Kyo Chung1, Ali D Güler, Michael J Caterina

  • 1Department of Biological Chemistry, Center for Sensory Biology, Johns Hopkins School of Medicine, 725 North Wolfe Street, Baltimore, Maryland 21205, USA.

Nature Neuroscience
|April 9, 2008
PubMed
Summary
This summary is machine-generated.

Transient receptor potential vanilloid 1 (TRPV1) channels dynamically alter ion permeability upon activation. Agonists and phosphorylation change TRPV1 selectivity, impacting pain and cellular signaling.

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Related Experiment Videos

Last Updated: Jul 6, 2026

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
12:09

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Published on: December 31, 2013

Controllable Ion Channel Expression through Inducible Transient Transfection
10:00

Controllable Ion Channel Expression through Inducible Transient Transfection

Published on: February 17, 2017

Purification and Reconstitution of TRPV1 for Spectroscopic Analysis
11:53

Purification and Reconstitution of TRPV1 for Spectroscopic Analysis

Published on: July 3, 2018

Area of Science:

  • Ion channel physiology
  • Molecular neurobiology
  • Cellular signaling

Background:

  • Transient receptor potential vanilloid 1 (TRPV1) is a nonselective cation channel activated by heat and capsaicin.
  • TRPV1's ion permeability is generally considered static, preferring Ca2+ over Na+.
  • Understanding TRPV1's dynamic properties is crucial for its role in pain and cellular processes.

Purpose of the Study:

  • To investigate dynamic changes in TRPV1 ion permeability upon activation.
  • To identify the molecular mechanisms underlying these permeability alterations.
  • To explore the modulatory role of phosphorylation on TRPV1 selectivity.

Main Methods:

  • Utilized native and recombinant rat TRPV1.
  • Employed electrophysiological techniques to assess ion permeability.
  • Applied the substituted cysteine accessibility method to probe the selectivity filter.
  • Investigated the effect of protein kinase C (PKC) dependent phosphorylation.

Main Results:

  • TRPV1 activation induced time- and agonist concentration-dependent increases in permeability to larger cations.
  • Agonist type influenced the extent of ionic selectivity changes.
  • Alterations in the TRPV1 selectivity filter were identified as the cause of permeability changes.
  • PKC-dependent phosphorylation of Ser800 potentiated agonist-evoked selectivity changes.

Conclusions:

  • TRPV1 ion selectivity is not static but dynamically modulated during channel activation.
  • These dynamic changes are mediated by alterations within the TRPV1 selectivity filter.
  • Phosphorylation further fine-tunes TRPV1's response, influencing its role in pain and neurotransmission.