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Label‐free optical biosensor for ligand‐directed functional selectivity acting on β 2 adrenoceptor in living cells
Author(s) -
Fang Ye,
Ferrie Ann M.
Publication year - 2008
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2008.01.021
Subject(s) - biosensor , ligand (biochemistry) , functional selectivity , receptor , chemistry , biophysics , stimulation , signal transduction , biochemistry , g protein coupled receptor , microbiology and biotechnology , computational biology , biology , neuroscience
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 β 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 β 2 ‐adrenoceptor and highlights the power of the biosensor assays for screening pathway‐biased ligands.