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

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


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.

MeSH terms

  • Adrenergic beta-2 Receptor Antagonists
  • Adrenergic beta-Antagonists / pharmacology
  • Albuterol / analogs & derivatives
  • Albuterol / pharmacology
  • Biosensing Techniques / instrumentation*
  • Catechols / pharmacology
  • Cell Line
  • Cell Survival / drug effects
  • Epinephrine / pharmacology
  • Humans
  • Kinetics
  • Ligands
  • Optics and Photonics / instrumentation*
  • Receptors, Adrenergic, beta-2 / metabolism*
  • Salmeterol Xinafoate
  • Signal Transduction / drug effects


  • Adrenergic beta-2 Receptor Antagonists
  • Adrenergic beta-Antagonists
  • Catechols
  • Ligands
  • Receptors, Adrenergic, beta-2
  • Salmeterol Xinafoate
  • catechol
  • Albuterol
  • Epinephrine