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Updated: Aug 10, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Identification and characterization of a G-protein regulatory motif in WAVE1
Kyoung Seob Song1, Yuri K Peterson, Andrew Freidman
1Department of Pharmacology and Experimental Therapeutics, Louisiana State University Health Sciences Center, 1901 Perdido Street, New Orleans, LA 70112, USA.
Abstract:
The G-protein regulatory (GPR) motif is a approximately 25 amino acid sequence that stabilizes the GDP-bound conformation of Gialpha. To identify additional GPR motifs, we expanded a motif-based search strategy and identified an additional 4 mammalian proteins (WAVE1-3, rat GHRH) and 10 plant proteins with candidate GPR motifs. The WAVE1 GPR peptide inhibited GTPgammaS binding to purified G-protein. Endogenous Gialpha and WAVE1 coimmunoprecipitated from brain lysates. A WAVE1-G-protein complex was also observed following transfection of COS7 cells with Gialpha3 and WAVE1. The docking of Gialpha within a WAVE1 scaffolding complex may facilitate dynamic cycling and/or targeting for efficient and localized control of actin polymerization.
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