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TRUPATH: An Open-Source Biosensor Platform for Interrogating the GPCR Transducerome.

Jeffrey F DiBerto¹, Reid H J Olsen², Bryan L Roth³

¹Department of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.

Methods in Molecular Biology (Clifton, N.J.)

|July 14, 2022

Summary

This summary is machine-generated.

Researchers developed TRUPATH, a novel platform for studying G protein-coupled receptors (GPCRs). This technology enables precise measurement of GPCR interactions with G proteins, aiding drug discovery for targeted therapies.

Keywords:

Biased agonism Bioluminescence resonance energy transfer (BRET)Drug discovery Drug screening Functional assays Functional selectivity G protein G protein-coupled receptors Receptor pharmacology Signal transduction

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Published on: December 1, 2020

Area of Science:

Pharmacology
Molecular Biology
Biochemistry

Background:

G protein-coupled receptors (GPCRs) are crucial drug targets, yet their full therapeutic potential is unrealized.
Traditional drug development often assumes single pathway signaling for GPCRs, overlooking complex interactions.
New technologies are emerging to dissect specific GPCR-G protein signaling pathways.

Purpose of the Study:

Introduce TRUPATH, a bioluminescence resonance energy transfer (BRET)-based platform.
Provide a detailed protocol for utilizing TRUPATH for GPCR-G protein interaction studies.
Facilitate the discovery of ligands with pathway selectivity for drug development.

Main Methods:

TRUPATH platform utilizing bioluminescence resonance energy transfer (BRET).
Measurement of receptor-catalyzed dissociation/rearrangement of 14 Gα subunits from Gβ and Gγ subunits.
Detailed protocol covering plasmid transfection, microplate preparation, assay implementation, and data analysis.

Main Results:

TRUPATH enables unambiguous measurement of GPCR-G protein interactions.
The platform allows for the study of multiple Gα subunits.
Provides a template for answering fundamental biological questions about GPCR coupling.

Conclusions:

TRUPATH is a powerful tool for basic research into GPCR signaling.
The platform can accelerate drug discovery by identifying ligands with specific pathway selectivity.
TRUPATH supports the exploration of previously underexploited therapeutic potential of GPCRs.