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• W2317871805 abstract "Receptor internalization is a useful indicator of the activity of ligands. The N-terminus of the β2-adrenergic receptor expressed on the cell surface was labeled with fluorophores using a novel coiled-coil labeling system. Endocytosis of the receptors was automatically detected using a fluorescence image analyzer by evaluating (1) translocation of the receptor from cell-surface to intracellular regions and (2) acidification in endosomes. Both parameters increased upon agonist stimulation in a dose-dependent manner. The extent of endocytosis was significantly dependent on the agonist used, indicating the presence of a biased signaling for endocytosis. The receptor antagonists can also be screened by competitive inhibition of agonist-induced endocytosis. The image analysis approach has proven to be useful for high-throughput characterization and screening of GPCR ligands." @default.
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• W2317871805 date "2012-01-30" @default.
• W2317871805 modified "2023-10-16" @default.
• W2317871805 title "High-Throughput Analysis of Ligand-Induced Internalization of β₂-Adrenoceptors Using the Coiled-Coil Tag–Probe Method" @default.
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• W2317871805 doi "https://doi.org/10.1021/ac203231n" @default.
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