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Updated: Aug 12, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Common and selective signal transduction mechanisms of GPCRs
1Molecular Biology, Genetics and Bioengineering Program, Faculty of Engineering and Natural Sciences, Sabanci University, Istanbul, Turkey.
Abstract:
G protein-coupled receptors (GPCRs) are coupled by four major subfamilies of G proteins. GPCR coupling is processed through a combination of common and selective activation mechanisms together. Common mechanisms are shared for a group of receptors. Recently, researchers managed to identify shared activation pathways for the GPCRs belonging to the same subfamilies. On the other hand, selective mechanisms are responsible for the variations within activation mechanisms. Selective processes can regulate subfamily-specific interactions between the receptor and the G proteins, and intermediate receptor conformations are required to couple particular G proteins through G protein-specific activation mechanisms. Moreover, G proteins can also selectively interact with RGS (regulators of G protein signaling) proteins as well. Selective processes modulate the signaling profile of the receptor and the tissue they are present. This chapter summarizes the recent research conducted on common and selective signal transduction mechanisms within GPCRs from an evolutionary perspective.
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