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Updated: Jun 17, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Agonist-selective signaling of G protein-coupled receptor: mechanisms and implications
Hui Zheng1, Horace H Loh, Ping-Yee Law
1Department of Pharmacology, University of Minnesota, Minneapolis, MN 55455-0217, USA. zhen0091@umn.edu
Abstract:
Agonist-selective signaling or ligand-biased signaling of G protein-coupled receptor (GPCR) has become the focus of an increasing number of laboratories. The principle of this concept is that agonist possesses different abilities to activate different signaling pathways. Current review summarizes the observations of agonist-selective signaling of various GPCRs, indicating the significance of agonist-selective signaling in biological processes. In addition, current review also provides an overview on how agonist-selective signaling is initiated. Especially, the relationship between GPCR-G protein interaction and GPCR-beta-arrestin interaction is discussed in depth.
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