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Updated: Apr 28, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Targeting CB2-GPR55 receptor heteromers modulates cancer cell signaling
Estefanía Moreno1, Clara Andradas2, Mireia Medrano1
1From the Department of Biochemistry and Molecular Biology, University of Barcelona, 08028 Barcelona, Spain, the Centro de Investigación Biomédica en Red de Enfermedades Neurodegenerativas (CIBERNED), 28031 Madrid, Spain, the Institute of Biomedicine of the University of Barcelona, 08028 Barcelona, Spain.
Abstract:
The G protein-coupled receptors CB2 (CB2R) and GPR55 are overexpressed in cancer cells and human tumors. Because a modulation of GPR55 activity by cannabinoids has been suggested, we analyzed whether this receptor participates in cannabinoid effects on cancer cells. Here we show that CB2R and GPR55 form heteromers in cancer cells, that these structures possess unique signaling properties, and that modulation of these heteromers can modify the antitumoral activity of cannabinoids in vivo. These findings unveil the existence of previously unknown signaling platforms that help explain the complex behavior of cannabinoids and may constitute new targets for therapeutic intervention in oncology.
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