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

被引：64

作者：

Fang, Ye ^{[1
]}

Ferrie, Ann M. ^{[1
]}

机构：

[1] Corning Inc, Biochem Technol Sci & Technol Div, Corning, NY 14831 USA

来源：

FEBS LETTERS | 2008年 / 582卷 / 05期

关键词：

optical biosensor; G protein-coupled receptor; beta(2)-adrenoceptor; ligand-directed functional selectivity;

D O I：

10.1016/j.febslet.2008.01.021

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：558 / 564

页数：7

共 28 条

[1] Src-mediated tyrosine phosphorylation of dynamin is required for β2-adrenergic receptor internalization and mitogen-activated protein kinase signaling [J].

Ahn, S ;

Maudsley, S ;

Luttrell, LM ;

Lefkowitz, RJ ;

Daaka, Y .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1999, 274 (03) :1185-1188

[2] β-Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors [J].

Azzi, M ;

Charest, PG ;

Angers, S ;

Rousseau, G ;

Kohout, T ;

Bouvier, M ;

Piñeyro, G .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2003, 100 (20) :11406-11411

[3] Pharmacological characterization of CGP 12177 at the human β2-adrenoceptor [J].

Baker, JG ;

Hall, IP ;

Hill, SJ .

BRITISH JOURNAL OF PHARMACOLOGY, 2002, 137 (03) :400-408

[4]

BARER R, 1954, Q J MICROSC SCI, V95, P399

[5] Characterization of isoprenaline- and salmeterol-stimulated interactions between β2-adrenoceptors and β-arrestin 2 using β-galactosidase complementation in C2C12 cells [J].

Carter, AA ;

Hill, SJ .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2005, 315 (02) :839-848

[6] Optical biosensors in drug discovery [J].

Cooper, MA .

NATURE REVIEWS DRUG DISCOVERY, 2002, 1 (07) :515-528

[7] Plasmon-waveguide resonance studies of ligand binding to the human β2-adrenergic receptor [J].

Devanathan, S ;

Yao, ZP ;

Salamon, Z ;

Kobilka, B ;

Tollin, G .

BIOCHEMISTRY, 2004, 43 (11) :3280-3288

[8] Characteristics of dynamic mass redistribution of epidermal growth factor receptor signaling in living cells measured with label-free optical biosensors [J].

Fang, Y ;

Ferrie, AM ;

Fontaine, NH ;

Yuen, PK .

ANALYTICAL CHEMISTRY, 2005, 77 (17) :5720-5725

[9] Optical biosensor provides insights for bradykinin B2 receptor signaling in A431 cells [J].

Fang, Y ;

Li, GS ;

Peng, JL .

FEBS LETTERS, 2005, 579 (28) :6365-6374

[10] Optical biosensor differentiates signaling of endogenous PAR1 and PAR2 in A431 cells [J].

Fang, Ye ;

Ferrie, Ann M. .

BMC CELL BIOLOGY, 2007, 8 (1)

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