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Related Concept Videos

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...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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...
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...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...

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Related Experiment Video

Updated: Jun 23, 2026

Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time
08:33

Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time

Published on: March 11, 2021

Gating mechanisms in Cys-loop receptors.

Jennie M E Cederholm1, Peter R Schofield, Trevor M Lewis

  • 1School of Medical Sciences, The University of New South Wales, Sydney, NSW, 2052, Australia.

European Biophysics Journal : EBJ
|May 1, 2009
PubMed
Summary
This summary is machine-generated.

Ligand-gated ion channels, crucial for neuronal signaling, open via conformational changes. This review details how specific loop structures mediate the coupling between ligand binding and channel gating.

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Last Updated: Jun 23, 2026

Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time
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Site Directed Spin Labeling and EPR Spectroscopic Studies of Pentameric Ligand-Gated Ion Channels
11:19

Site Directed Spin Labeling and EPR Spectroscopic Studies of Pentameric Ligand-Gated Ion Channels

Published on: July 4, 2016

Area of Science:

  • Neuroscience
  • Molecular Biology
  • Structural Biology

Background:

  • Cys-loop receptors are pentameric ligand-gated ion channels vital for neuronal signaling.
  • They possess extracellular ligand-binding sites and transmembrane domains (M1-M4) forming an ion pore.
  • The mechanism coupling extracellular ligand binding to transmembrane pore opening remains incompletely understood.

Purpose of the Study:

  • To review recent findings on loop structures involved in Cys-loop receptor activation.
  • To discuss the role of these structures in the gating mechanism of ligand-gated ion channels.

Main Methods:

  • Review of recent structural and functional studies.
  • Analysis of crystal structures, including acetylcholine binding protein and Torpedo marmorata acetylcholine receptor.

Main Results:

  • Several loop structures (loop 2, Cys-loop, pre-M1, M2-M3) are implicated in receptor activation.
  • The "conformational change wave" hypothesis describes ligand binding initiating beta-sheet rotation, displacing loops, and twisting M2 domains to open the pore.
  • Recent structural data enhance understanding of ligand binding-channel gating coupling.

Conclusions:

  • Loop structures play a critical role in transducing ligand binding into channel gating.
  • Further research into these elements will elucidate the precise mechanisms of neuronal signaling.