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

Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

4.0K
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,...
4.0K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

16.6K
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...
16.6K
GPCR Desensitization01:12

GPCR Desensitization

7.9K
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...
7.9K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

7.3K
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...
7.3K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

131.6K
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.
131.6K
Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

6.5K
Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
6.5K

You might also read

Related Articles

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

Sort by
Same author

A probabilistic approach to the analysis of elastic light scatter profiles for identification of culturable bacteria.

Systematic and applied microbiology·2026
Same author

CARGO: A Cytometry Analysis framework via Regularized Graph Optimal-transport.

PLoS computational biology·2026
Same author

Profiling the CFTR Variant Selectivity and Off-Target Interactions of VX-121.

bioRxiv : the preprint server for biology·2026
Same author

Toward a Random Background for Ligand Optimization.

bioRxiv : the preprint server for biology·2026
Same author

Protein Stability, Turnover Kinetics, and Abundance Constrain the Scaling of Protein Interaction Networks.

bioRxiv : the preprint server for biology·2026
Same author

ANYI: The ANnotated Yeast Interactome.

bioRxiv : the preprint server for biology·2026

Related Experiment Video

Updated: Jan 16, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

15.7K

Deep Receptor Scanning Reveals General Sequence Constraints on GPCR Biosynthesis.

Austin Tedman1, Muskan Goel1, Sohan Shah1

  • 1The James Tarpo Jr. and Margaret Tarpo Department of Chemistry, Purdue University, West Lafayette, IN, USA.

Biorxiv : the Preprint Server for Biology
|September 26, 2025
PubMed
Summary
This summary is machine-generated.

Researchers developed a deep receptor scanning platform to analyze 766 human G protein-coupled receptors (GPCRs) and their variants. This method identifies structural features influencing GPCR expression, advancing pharmacological target exploration.

Keywords:
CodonDeep Mutational ScanningGPCRMachine LearningMembrane Protein FoldingPharmacologyProteostasisReceptorRibo-SeqSignaling

More Related Videos

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
09:19

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization

Published on: March 16, 2020

7.4K
Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
08:21

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

7.3K

Related Experiment Videos

Last Updated: Jan 16, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

15.7K
Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
09:19

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization

Published on: March 16, 2020

7.4K
Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
08:21

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

7.3K

Area of Science:

  • Biochemistry
  • Pharmacology
  • Genomics

Background:

  • G protein-coupled receptors (GPCRs) are crucial signaling molecules and major drug targets.
  • Many GPCRs remain understudied despite their importance.
  • Existing methods are insufficient for large-scale GPCR characterization.

Purpose of the Study:

  • To develop and validate a high-throughput platform for comprehensive GPCR characterization.
  • To quantitatively assess GPCR transcript abundance, translation, and cell surface expression.
  • To identify structural determinants of GPCR expression using machine learning.

Main Methods:

  • A "deep receptor scanning" platform was established to analyze 766 human GPCRs and 174 splice variants in parallel.
  • Quantitative characterization of canonical and alternative receptor transcripts, translational efficiency, and plasma membrane expression.
  • Machine learning algorithms were applied to identify structural features modulating GPCR expression.

Main Results:

  • The platform successfully characterized a large number of human GPCRs and their variants.
  • Data revealed insights into transcript abundance, translational efficiency, and cell surface expression patterns.
  • Machine learning identified key structural features influencing GPCR expression levels.

Conclusions:

  • The deep receptor scanning platform offers a versatile tool for efficient GPCRome exploration.
  • This approach facilitates the study of underrepresented GPCRs and their functional properties.
  • The findings provide a foundation for future drug discovery targeting GPCRs.