Enhanced Bystander BRET (ebBRET) Biosensors as Biophysical Tools to Map the Signaling Profile of Neuropsychiatric Drugs Targeting GPCRs

Supriya A Gaitonde; Michel Bouvier

doi:10.1007/978-1-0716-3307-6_2

Enhanced Bystander BRET (ebBRET) Biosensors as Biophysical Tools to Map the Signaling Profile of Neuropsychiatric Drugs Targeting GPCRs

Methods Mol Biol. 2023:2687:15-30. doi: 10.1007/978-1-0716-3307-6_2.

Authors

Supriya A Gaitonde¹, Michel Bouvier²

Affiliations

¹ Department of Biochemistry and Molecular Medicine, Institute for Research in Immunology and Cancer (IRIC), Université de Montréal, Montréal, QC, Canada. supriya.ajit.gaitonde@umontreal.ca.
² Department of Biochemistry and Molecular Medicine, Institute for Research in Immunology and Cancer (IRIC), Université de Montréal, Montréal, QC, Canada.

PMID: 37464159
DOI: 10.1007/978-1-0716-3307-6_2

Abstract

Bioluminescence resonance energy transfer (BRET) is a non-radiative energy transfer between a bioluminescent donor and a fluorescent acceptor with far-reaching applications in detecting physiologically relevant protein-protein interactions. The recently developed enhanced bystander BRET (ebBRET) biosensors have made it possible to rapidly determine the signaling profile of a series of ligands across a large number of GPCRs and their signaling repertoires, which has tremendous implications in the drug discovery process. Here we describe BRET and the ebBRET biosensors as investigational tools in establishing functional selectivity downstream of GPCRs.

Keywords: Antipsychotics; BRET; Biosensors; Enhanced bystander BRET (ebBRET); Functional selectivity; GPCR; Signaling profile.

MeSH terms

Bioluminescence Resonance Energy Transfer Techniques
Biosensing Techniques*
Energy Transfer
HEK293 Cells
Humans
Signal Transduction*