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Related Concept Videos

Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high affinity and are together...
Rab Cascades01:25

Rab Cascades

Rab GTPases act in a regulated cascade during membrane fusion, helping the lipid bilayers mix. The Rab family of proteins are active when bound to GTP, and inactive when bound to GDP. Hence, they act as guanine nucleotide-dependent molecular switches. Rab-GTP recognizes and binds to long or short-range tethering proteins to capture the target vesicle. These tethers coordinate with SNAREs on the vesicle and the target membrane to assemble the trans SNARE complex that locks the mixing bilayers.
Rab Proteins01:14

Rab Proteins

Rab proteins constitute the largest family of monomeric GTPases, of which 70 members are present in humans. Rab proteins and their effectors regulate consecutive stages of vesicle transport such as vesicle transport, docking, and fusion to the correct recipient membrane.
Rab proteins switch between a cytosolic, GDP-bound inactive state and a membrane-anchored, GTP-bound active state. By themselves, Rabs show slow rates of GDP/GTP exchange and GTP hydrolysis. Thus, Rab proteins are considered...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
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: May 11, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

GABAA receptor membrane insertion rates are specified by their subunit composition.

Suchitra Joshi1, Kendra J Keith, Adeel Ilyas

  • 1Department of Neurology, University of Virginia, Charlottesville, VA 22908, United States.

Molecular and Cellular Neurosciences
|May 30, 2013
PubMed
Summary

The rate of insertion of gamma-aminobutyric acid type-A receptors (GABARs) into the cell membrane depends on their subunit composition. Gamma-2 subunit-containing GABARs insert rapidly, while delta subunit-containing GABARs insert more slowly.

Keywords:
GABA-A receptorHEK293Hippocampal neuronsRate of insertionSubunit composition

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Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons
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Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons

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Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking
11:57

Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking

Published on: March 28, 2014

Related Experiment Videos

Last Updated: May 11, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons
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Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons

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Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking
11:57

Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking

Published on: March 28, 2014

Area of Science:

  • Neuroscience
  • Molecular Biology
  • Cell Biology

Background:

  • Gamma-aminobutyric acid type-A receptors (GABARs) are crucial for synaptic inhibition.
  • GABARs containing different subunits, such as gamma-2 and delta, form distinct receptor pools with unique functions and localization.
  • Understanding the trafficking dynamics of these receptor pools is essential for comprehending neuronal function.

Purpose of the Study:

  • To determine and compare the surface membrane insertion rates of GABARs containing gamma-2 versus delta subunits.
  • To investigate how different alpha subunits influence the insertion rate of delta-containing GABARs.
  • To compare the insertion rates of recombinant GABARs in cell lines with native GABARs in neurons.

Main Methods:

  • Utilized alpha-bungarotoxin binding site (BBS) tagged subunits (t-γ2 and t-δ) to track receptor insertion in HEK293 cells.
  • Assessed the influence of different alpha subunits (α1, α4) on the insertion of gamma-2 and delta subunit-containing GABARs.
  • Employed an antibody saturation assay to measure the surface membrane insertion rate of native GABARs in cultured hippocampal neurons.

Main Results:

  • Insertion of t-γ2 subunit-containing GABARs into HEK293 cell membranes was rapid, peaking within 30 minutes.
  • Insertion of t-δ subunit-containing GABARs showed a slower kinetics, peaking at 120 minutes.
  • Native γ2-GABARs inserted quickly into neuronal membranes (soma and dendrites), while native δ-GABARs inserted slowly, initially in the soma and later in dendrites.

Conclusions:

  • The rate of GABARs surface membrane insertion is significantly dependent on their specific subunit composition (γ2 vs. δ).
  • The assembly of different alpha subunits affects the insertion rate of δ-containing GABARs but not γ2-containing GABARs.
  • Findings in recombinant systems correlate with observations in native neuronal GABARs, highlighting distinct trafficking pathways.