Department of Biochemistry and Molecular Medicine, Institute for Research in Immunology and Cancer (IRIC), Université de Montréal, Montréal, QC, Canada.
Methods Mol Biol. 2023;2687:15-30. doi: 10.1007/978-1-0716-3307-6_2.
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.
生物发光共振能量转移（BRET）是生物发光供体和荧光受体之间的非辐射能量转移，在检测与生理相关的蛋白质-蛋白质相互作用方面具有广泛的应用。最近开发的增强旁观者 BRET（ebBRET）生物传感器使得能够快速确定一系列配体在大量 GPCR 及其信号谱中的信号特征，这在药物发现过程中具有巨大的意义。在这里，我们将 BRET 和 ebBRET 生物传感器描述为在 GPCR 下游建立功能选择性的研究工具。
