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Related Concept Videos

G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory organs,...
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.
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...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...

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Related Experiment Video

Updated: Jul 3, 2026

Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors (GPCRs)
09:45

Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors (GPCRs)

Published on: February 5, 2022

A role for membrane potential in regulating GPCRs?

Martyn P Mahaut-Smith1, Juan Martinez-Pinna, Iman S Gurung

  • 1Department of Cell Physiology and Pharmacology, University of Leicester, LE1 9HN, UK. mpms1@le.ac.uk

Trends in Pharmacological Sciences
|July 16, 2008
PubMed
Summary

Membrane voltage directly influences G-protein-coupled receptors (GPCRs), impacting cell signaling. This voltage-dependence, observed in muscarinic receptors, suggests a new mechanism for cellular communication.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

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Last Updated: Jul 3, 2026

Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors (GPCRs)
09:45

Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors (GPCRs)

Published on: February 5, 2022

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Area of Science:

  • Cellular Biology
  • Neuroscience
  • Biochemistry

Background:

  • G-protein-coupled receptors (GPCRs) are crucial for signal transduction.
  • Previous evidence for GPCR voltage-dependence was largely indirect.
  • Recent studies show direct voltage-dependent charge movements in GPCRs.

Purpose of the Study:

  • To explore the direct voltage modulation of GPCRs.
  • To investigate the mechanism of voltage-dependent GPCR function.
  • To discuss the physiological implications of GPCR voltage-dependence.

Main Methods:

  • Electrophysiological recordings to detect charge movements.
  • Biochemical assays to assess G protein coupling.
  • Agonist binding studies.

Main Results:

  • Demonstrated the first direct voltage-dependent charge movements in a GPCR.
  • Proposed a mechanism involving voltage-induced conformational changes affecting G protein coupling and agonist affinity.
  • Identified other GPCRs potentially regulated by membrane potential.

Conclusions:

  • GPCRs can be directly modulated by membrane voltage.
  • This voltage-dependence offers a novel layer of cellular signaling control.
  • Potential widespread physiological consequences for various cell types.