Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

12.5K
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...
12.5K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

120.7K
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.
120.7K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

2.2K
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,...
2.2K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

7.3K
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...
7.3K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

5.8K
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...
5.8K
GPCR Desensitization01:12

GPCR Desensitization

6.2K
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...
6.2K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Obesity due to MC4R deficiency is associated with reduced cholesterol, triglycerides and cardiovascular disease risk.

Nature medicine·2025
Same author

Loss-of-function Gα<sub>s</sub> rare disease variants exert mutation-specific effects on GPCR signaling.

Science signaling·2025
Same author

Large scale investigation of GPCR molecular dynamics data uncovers allosteric sites and lateral gateways.

Nature communications·2025
Same author

Molecular determinants of ligand efficacy and potency in GPCR signaling.

Science (New York, N.Y.)·2023
Same author

Author Correction: Combinatorial expression of GPCR isoforms affects signalling and drug responses.

Nature·2020
Same author

Combinatorial expression of GPCR isoforms affects signalling and drug responses.

Nature·2020

Related Experiment Video

Updated: Aug 13, 2025

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

16.5K

A multi-dimensional view of context-dependent G protein-coupled receptor function.

Maria Marti-Solano1

  • 1Department of Pharmacology, University of Cambridge, Cambridge CB2 1PD, U.K.

Biochemical Society Transactions
|January 23, 2023
PubMed
Summary

G protein-coupled receptors (GPCRs) are key drug targets, but linking their activation to specific physiological outcomes remains challenging. New research reveals context-dependent GPCR signaling, improving understanding for drug development.

Keywords:
G-protein-coupled receptorsbiological networkscellular localizationdrug discovery and designsignallingsystems biology

More Related Videos

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

9.0K
Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

40.7K

Related Experiment Videos

Last Updated: Aug 13, 2025

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

16.5K
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

9.0K
Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

40.7K

Area of Science:

  • Pharmacology
  • Cell Biology
  • Biochemistry

Background:

  • G protein-coupled receptors (GPCRs) are vital cell surface receptors involved in numerous physiological processes.
  • Their role in homeostasis and as drug targets highlights their significance in medicine.
  • Understanding the precise links between GPCR activation and cellular responses is crucial but complex.

Approach:

  • Utilizing novel biosensors and high-throughput techniques to study GPCR signaling.
  • Analyzing receptor function with increasing spatial, temporal, and cell-specific resolution.
  • Reviewing recent examples of context-dependent GPCR signaling.

Key Points:

  • GPCRs mediate diverse cellular responses to various biomolecules.
  • Challenges persist in connecting specific receptor activation events to distinct physiological outcomes.
  • Emerging research demonstrates that GPCR signaling is context-dependent, varying by location, timing, and cell type.

Conclusions:

  • Context-dependent GPCR signaling provides deeper insights into receptor function in health and disease.
  • This understanding can guide the development of more selective and safer GPCR-targeted drugs.
  • Further research into GPCR signaling complexity is essential for advancing therapeutic strategies.