期刊
FEBS LETTERS
卷 582, 期 5, 页码 558-564出版社
WILEY
DOI: 10.1016/j.febslet.2008.01.021
关键词
optical biosensor; G protein-coupled receptor; beta(2)-adrenoceptor; ligand-directed functional selectivity
Recent realization of ligand-directed functional selectivity demands high-resolution tools for studying receptor biology and ligand pharmacology. Here we use label-free optical biosensor to examine the dynamic mass redistribution of human epidermoid A431 cells in response to diverse beta(2)-adrenoceptor ligands. Multi-parameter analysis reveals distinct patterns in activation and signaling of the receptor induced by different agonists. Sequential and co-stimulation assays categorize various ligands for their ability to modulate signaling induced by catechol, a structural component of catecholamines. This study documents multiple ligand-specific states of the beta(2)-adrenoceptor and highlights the power of the biosensor assays for screening pathway-biased ligands. (C) 206 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
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