Label‐free optical biosensor for ligand‐directed functional selectivity acting on β2 adrenoceptor in living cells

FEBS Letters - Tập 582 - Trang 558-564 - 2008
Ye Fang1, Ann M. Ferrie1
1Biochemical Technologies, Science and Technology Division, Corning Incorporated, Sullivan Park, Corning, NY 14831, United States

Tóm tắt

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 β2‐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 β2‐adrenoceptor and highlights the power of the biosensor assays for screening pathway‐biased ligands.

Tài liệu tham khảo

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FEBS Letters

Tập 582

558-564

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