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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

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Published on: December 1, 2020

TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome.

Reid H J Olsen¹, Jeffrey F DiBerto¹, Justin G English¹

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

Nature Chemical Biology

|May 6, 2020

Summary

This summary is machine-generated.

Researchers developed TRUPATH, a novel suite of G-protein-coupled receptor (GPCR) biosensors, to precisely map cellular signaling pathways. These advanced tools enhance understanding of GPCRs, crucial drug targets.

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Area of Science:

Pharmacology
Cellular Biology
Biochemistry

Background:

G-protein-coupled receptors (GPCRs) are critical drug targets, but their complex signaling pathways involving the transducerome are not fully understood.
Existing methods for studying GPCR signaling lack the resolution to dissect individual pathways.

Purpose of the Study:

To develop and validate a novel suite of biosensors for high-resolution interrogation of the GPCR transducerome.
To provide the scientific community with accessible tools for studying GPCR molecular pharmacology.

Main Methods:

Development of an open-source suite of 14 optimized bioluminescence resonance energy transfer (BRET) Gαβγ biosensors, named TRUPATH.
Exhaustive protein engineering and empirical testing, including the creation of the first Gα15 and GαGustducin probes.
Head-to-head comparisons and benchmarking studies with existing sensors across multiple GPCRs and cell lines.

Main Results:

TRUPATH biosensors demonstrated superior performance compared to first-generation sensors in various GPCR and cell line models.
Benchmarking studies confirmed known signaling bias and identified novel coupling preferences for GPCRs.
The TRUPATH suite includes novel probes for Gα15 and GαGustducin, expanding the toolkit for transducerome research.

Conclusions:

The TRUPATH biosensor suite offers unprecedented resolution for studying GPCR signaling pathways.
These novel, high-performance biosensors will advance the understanding of GPCR molecular pharmacology and drug discovery.
TRUPATH biosensors are made accessible through Addgene, facilitating broader scientific adoption and research.