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Related Concept Videos

GPCR Desensitization01:12

GPCR Desensitization

6.1K
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...
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Related Experiment Video

Updated: Apr 30, 2026

Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
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Self-Checking Cell-Based Assays for GPCR Desensitization and Resensitization.

Gregory W Fisher1, Margaret H Fuhrman1, Sally A Adler1

  • 1Department of Biological Sciences and Molecular Biosensor and Imaging Center, Carnegie Mellon University, Pittsburgh, PA, USA.

Journal of Biomolecular Screening
|May 14, 2014
PubMed
Summary
This summary is machine-generated.

New live-cell assays enable efficient quantification of G protein-coupled receptor (GPCR) desensitization and resensitization. These high-throughput assays utilize a fluorogen-activating protein (FAP) reporter for drug discovery.

Keywords:
G protein–coupled receptorsGPCRscell based assaysreceptor desensitizationreceptor resensitization

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Area of Science:

  • Biochemistry
  • Cell Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial for numerous physiological processes and represent a major drug target class.
  • Most GPCRs remain poorly characterized, with over 100 human orphans lacking identified endogenous ligands.
  • Understanding GPCR cell biology, including desensitization and resensitization, is vital for drug development.

Purpose of the Study:

  • To develop novel live-cell assays for quantifying GPCR desensitization and resensitization.
  • To create assays adaptable for high-throughput screening in drug discovery.

Main Methods:

  • Utilized recombinant GPCRs in live-cell assays.
  • Employed a fluorogen-activating protein (FAP) reporter system.
  • Assays involved reversible complexation of FAP with fluorogens, enhancing fluorescence upon binding.

Main Results:

  • Developed assays to quantify GPCR desensitization and resensitization.
  • Assays require no wash or cleanup steps.
  • Assays are readily performed in microwell plates, suitable for high-throughput applications.

Conclusions:

  • The new live-cell assays provide efficient tools for studying GPCR cell biology.
  • These assays facilitate the characterization of orphan GPCRs and drug discovery efforts.
  • The FAP-based system offers a versatile platform for quantitative GPCR research.