A rapid fluorogenic GPCR-β-arrestin interaction assay
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Updated: Feb 14, 2026

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
Qiang Zhang1,2, Yao-Wu Zheng2, Shaun R Coughlin2
1Department of Pharmaceutical Chemistry, University of California-San Francisco, San Francisco, California.
Abstract:
Detection of protein-protein interactions involved in signal transduction in live cells and organisms has a variety of important applications. We report a fluorogenic assay for G protein-coupled receptor (GPCR)-β-arrestin interaction that is genetically encoded, generalizes to multiple GPCRs, and features high signal-to-noise because fluorescence is absent until its components interact upon GPCR activation. Fluorescence after protease-activated receptor-1 activation developed in minutes and required specific serine-threonine residues in the receptor carboxyl tail, consistent with a classical G protein-coupled receptor kinase dependent β-arrestin recruitment mechanism. This assay provides a useful complement to other in vivo assays of GPCR activation.
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