Bioluminescence in G protein-coupled receptors drug screening using nanoluciferase and halo-tag technology

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Item Type:	Article
Title:	Bioluminescence in G protein-coupled receptors drug screening using nanoluciferase and halo-tag technology
Creators Name:	Schihada, H., Nemec, K., Lohse, M.J. and Maiellaro, I.
Abstract:	Here we describe the stepwise application of bioluminescence resonance energy transfer (BRET)-based conformational receptor biosensors to study GPCR activation in intact cells. This technology can be easily adopted to various plate reader devices and microtiter plate formats. Due to the high sensitivity of these BRET-based receptor biosensors and their ability to quantify simultaneously receptor activation/de-activation kinetics as well as compound efficacy and potency, these optical tools provide the most direct and unbiased approach to monitor GPCR activity in a high-throughput-compatible assay format, representing a novel promising tool for the discovery of potential GPCR therapeutics.
Keywords:	Bioluminescence Resonance Energy Transfer, G Protein-Coupled Receptors, Conformational Biosensors, Activation Dynamics, Drug Screening, Z-Factor
Source:	Methods in Molecular Biology
Series Name:	Methods in Molecular Biology
Title of Book:	G Protein-coupled receptor screening assays : methods and protocols
ISSN:	1064-3745
ISBN:	978-1-0716-1220-0
Publisher:	Springer / Humana Press
Volume:	2268
Page Range:	137-147
Date:	2021
Official Publication:	https://doi.org/10.1007/978-1-0716-1221-7_9
PubMed:	View item in PubMed

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