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Updated: Aug 8, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
The selective interactions and functions of regulators of G-protein signalling
1BHF Laboratories and Department of Medicine, University College London, 5 University Street, London WC1E 6JJ, UK. a.tinker@ucl.ac.uk
Abstract:
There is accumulating evidence that regulators of G-protein signalling (RGS) can have roles in signal transduction that are not related to GAP activity. Furthermore, RGSs have much more selective effects in vivo than might be anticipated from their behaviour in in vitro assays. I discuss the molecular mechanisms by which these phenomena might be explained including specific interactions between the RGS and G-protein coupled receptor, G-protein and effector.
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