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G Protein-coupled Receptors

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...

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Related Experiment Video

Updated: Dec 20, 2025

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

Published on: December 2, 2022

The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs.

Andrea J Vernall¹, Stephen J Hill, Barrie Kellam

¹School of Pharmacy, Centre for Biomolecular Sciences, University of Nottingham, Nottingham, UK.

British Journal of Pharmacology

|June 6, 2013

Summary

Fluorescent ligands offer a safer alternative to radioligands for studying drug targets like GPCRs. Careful design of these fluorescent probes is crucial for accurate pharmacological studies and drug discovery.

Keywords:

G-protein coupled receptor binding fluorescence microscopy fluorescent ligand conjugate imaging screening

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

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Last Updated: Dec 20, 2025

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

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

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

Published on: September 13, 2013

Area of Science:

Molecular Pharmacology
Drug Discovery
Biochemistry

Background:

Fluorescently tagged drug molecules are increasingly used as pharmacological tools.
They enable visualization of receptor targets and affinity measurements at the single-cell level.
Fluorescence-based assays are a safer and more adaptable substitute for radioligands in screening.

Purpose of the Study:

To review recent developments in fluorescent ligand design for G protein-coupled receptors (GPCRs).
To assess fluorescent conjugates for GPCRs, highlighting their strengths and weaknesses.
To emphasize the importance of careful planning in fluorescent ligand synthesis.

Main Methods:

Receptor-family-based approach to assess fluorescent conjugates.
Review of recently reported fluorescent ligands for GPCRs.
Analysis of factors influencing conjugate properties, such as dye, linker, and attachment point.

Main Results:

Fluorescent ligands provide valuable data on receptor targets, approaching single-molecule detection limits.
Design choices (dye, linker, attachment site) significantly impact ligand potency and selectivity.
Optimized fluorescent conjugates are effective in various assay formats.

Conclusions:

Fluorescent ligand design and synthesis require meticulous planning and execution.
Fluorescently labeled GPCR ligands are a dynamic and evolving area of research.
These tools are vital for advancing molecular pharmacology and drug discovery.