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 Experiment Videos

Quantitative cell-based high-content screening for vasopressin receptor agonists using transfluor technology.

Richik N Ghosh1, Richard DeBiasio, Christine C Hudson

  • 1Cellomics, Inc., Pittsburgh, PA 15219, USA. rghosh@cellomics.com

Journal of Biomolecular Screening
|August 12, 2005
PubMed
Summary

Related Concept Videos

You might also read

Related Articles

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

Sort by
Same author

Glucocorticoid Receptor Translational Isoforms Generate Unique Glucocorticoid Responses in the Mouse Brain.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology·2026
Same author

Methionine Deprivation-induced Reprogramming of Hepatic Rhythms Is Mediated by Glucocorticoid Receptor.

bioRxiv : the preprint server for biology·2026
Same author

Recapitulation of clinical and molecular hallmarks of lipid-induced hepatic insulin resistance in a zonated, vascularized human liver acinus microphysiological system during metabolic dysfunction-associated steatotic liver disease (MASLD) progression.

BMC biotechnology·2026
Same author

Road map for primary hepatocyte qualification in human liver organ models.

BMC methods·2026
Same author

Timing of Glucocorticoid Treatment Dictates Glucocorticoid Receptor Actions Modulating the NLRP3-Inflammasome Activation in Macrophages.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology·2026
Same author

Cardiomyocyte Glucocorticoid Receptors Exacerbate Stress Effects in Myocardial Ischemia Injury in Mice.

Cells·2025

A universal G-protein-coupled receptor (GPCR) assay effectively screened for vasopressin V2 receptor (V2R) agonists. This high-content screening method identified potent peptide agonists by detecting receptor internalization via fluorescently tagged beta-arrestin.

Area of Science:

  • Pharmacology
  • Cell Biology
  • Biochemistry

Background:

  • G-protein-coupled receptors (GPCRs) are crucial drug targets.
  • Developing robust assays for GPCR agonist screening is essential for drug discovery.
  • Vasopressin V2 receptor (V2R) plays a role in regulating water balance.

Purpose of the Study:

  • To demonstrate a universal assay for screening GPCR agonists.
  • To identify novel agonists for the vasopressin V2 receptor (V2R).
  • To validate the utility of high-content screening (HCS) for GPCR drug discovery.

Main Methods:

  • Utilized cells with stable expression of V2R and a green fluorescent protein (GFP)-labeled beta-arrestin fusion protein.
  • Employed a high-content screening (HCS) assay to analyze a peptide library for V2R agonists.

Related Experiment Videos

  • Automated imaging and quantitative analysis of intracellular fluorescent spots indicative of receptor activation.

    • Main Results:

    • Successfully screened a peptide library for V2R agonists using the developed GPCR assay.
    • Identified V2R agonists characterized by V2R internalization and associated GFP-beta-arrestin in endosomes.
    • Hits were further evaluated for potency, demonstrating the assay's effectiveness in lead identification.

    Conclusions:

    • The developed GPCR assay is a simple and universal method for screening agonists.
    • Automated HCS combined with beta-arrestin recruitment provides a powerful platform for GPCR drug discovery.
    • This approach facilitates the identification and validation of potent GPCR-targeting drug leads.