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FEBS Lett. 2008 Mar 5;582(5):558-64. doi: 10.1016/j.febslet.2008.01.021. Epub 2008 Jan 31.

Label-free optical biosensor for ligand-directed functional selectivity acting on beta(2) adrenoceptor in living cells.

Author information

1
Biochemical Technologies, Science and Technology Division, Corning Incorporated, Sullivan Park, Corning, NY 14831, USA. fangy2@corning.com

Abstract

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.

PMID:
18242178
DOI:
10.1016/j.febslet.2008.01.021
[Indexed for MEDLINE]
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