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Updated: Aug 25, 2025

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

Genetically encoded fluorescent biosensors for GPCR research.

Hyunbin Kim^1,2, In-Yeop Baek^1,3, Jihye Seong^1,2,3

¹Brain Science Institute, Korea Institute of Science and Technology (KIST), Seoul, South Korea.

Frontiers in Cell and Developmental Biology

|October 17, 2022

Summary

This review details genetically encoded fluorescent biosensors for monitoring G protein-coupled receptor (GPCR) activation in real-time. These tools track ligand binding, conformational changes, and signaling events in live cells.

Keywords:

BRET FRET GPCR circular permutation fluorescent protein genetically encoded fluorescent biosensor nanobody

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Last Updated: Aug 25, 2025

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

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Published on: September 13, 2013

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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

Area of Science:

Cellular Biology
Molecular Pharmacology
Biochemistry

Background:

G protein-coupled receptors (GPCRs) are crucial regulators of physiological and pathophysiological processes.
Understanding GPCR activation dynamics and subcellular functions is vital.
High spatiotemporal resolution is needed to study GPCR molecular mechanisms.

Purpose of the Study:

To review genetically encoded fluorescent biosensors for real-time monitoring of GPCR activation.
To cover the entire GPCR activation process from ligand binding to downstream signaling.
To discuss various biosensor strategies and their applications in GPCR research.

Main Methods:

Fluorescent biosensors utilizing FRET, BRET, cpFP, and nanobody technologies.
Real-time monitoring of GPCR activation in live cells.
Analysis of GPCR ligand binding, conformational changes, and protein recruitment.

Main Results:

Fluorescent biosensors enable precise tracking of GPCR activation dynamics.
These sensors capture events including ligand binding, conformational shifts, and G protein/β-arrestin recruitment.
GPCR internalization, trafficking, and downstream signaling can be monitored.

Conclusions:

Genetically encoded fluorescent biosensors are powerful tools for studying GPCRs.
These biosensors offer insights into GPCR function at various subcellular locations.
Further application of these biosensors will advance GPCR research.