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BRET1-Assay using the FDSS/µCELL Imaging Plate Reader

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BRET1-Assay using the FDSS/µCELL Imaging Plate Reader

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The GPCRs represent the largest family of cell surface receptors and are the main target for drugs available on the pharmaceutical market. To prevent receptors from both acute and chronic overstimulation, GPCR activity is regulated by an intensively studied mechanism called desensitization or internalization. Following ligand exposure, arrestins interact with phosphorylated GPCRs, uncoupling them from their cognate G protein, blocking further activation and promoting endocytosis. Interaction between receptors and β-arrestins is a measurable functional event in the GPCR-mediated signaling cascade. The biophysical technique named Bioluminescence Resonance Energy Transfer (BRET) has been widely used to monitor and quantify agonist-promoted β-arrestin recruitment, including high throughput screenings.

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