Related Experiment Video
Updated: Jun 7, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Light- and drug-activated G-protein-coupled receptors to control intracellular signalling
Olivia A Masseck1, Johanna M Rubelowski, Katharina Spoida
1Department of General Zoology and Neurobiology, Ruhr-University, Bochum, Germany.
Abstract:
G-protein-coupled receptors (GPCRs) integrate extracellular cues into intracellular signals to modulate the cellular state. Owing to their diverse modulatory functions, GPCRs represent one of the major drug targets of the pharmaceutical industry. Until now, the characterization and control of GPCRs and their intracellular signalling cascades have mainly relied on chemical compounds, which either activate or inhibit GPCR pathways, albeit with limited receptor and cell-type specificity. Recently, new approaches have been developed to control signalling cascades in cell- and receptor-type-specific ways. The chemical approach focuses on GPCR design and activation by an inert chemical compound, whereas the physical approach uses designer GPCRs and activation by physical stimuli, such as light.
Related Concept Videos
Signal Transduction: Overview
Typically, signal transduction involves three...
Amplifying Signals via Enzymatic Cascade
Amplifying Signals via Second Messengers
Intracellular Signaling Cascades
G-protein Coupled Receptors
G-protein Coupled Receptors

