Single-molecule imaging reveals the stoichiometry change of β2-adrenergic receptors by a pharmacological biased ligand

Yahong Sun; Nan Li; Mingliang Zhang; Wei Zhou; Jinghe Yuan; Rong Zhao; Jimin Wu; Zijian Li; Youyi Zhang; Xiaohong Fang

doi:10.1039/C6CC00628K

Single-molecule imaging reveals the stoichiometry change of β₂-adrenergic receptors by a pharmacological biased ligand†

Yahong Sun,^a Nan Li,^a Mingliang Zhang,^ab Wei Zhou,^a Jinghe Yuan,^a Rong Zhao,^a Jimin Wu,^b Zijian Li,^b Youyi Zhang*^b and Xiaohong Fang*^a

Author affiliations

* Corresponding authors

^a Beijing National Laboratory for Molecular Sciences, Institute of Chemistry, Key Laboratory of Molecular Nanostructures and Nanotechnology, Chinese Academy of Sciences, Beijing 100190, P. R. China
E-mail: xfang@iccas.ac.cn

^b Institute of Vascular Medicine Peking University Third Hospital and Academy for Advanced Interdisciplinary Studies, Peking University, Beijing Key Laboratory of Cardiovascular Receptors Research, Beijing 100191, China
E-mail: zhangyy@bjmu.edu.cn

Abstract

The stoichiometry of the β₂-adrenergic receptor (β₂AR) was determined using single-molecule fluorescence imaging in living cells. The results showed that β₂AR mainly existed as monomers under physiological conditions and exhibited β-arrestin-dependent dimerization upon stimulation with the pharmacological biased ligand carvedilol. The association of β₂AR dimerization with biased signalling is revealed.

Chemical Communications

Single-molecule imaging reveals the stoichiometry change of β₂-adrenergic receptors by a pharmacological biased ligand†

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Single-molecule imaging reveals the stoichiometry change of β₂-adrenergic receptors by a pharmacological biased ligand

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Chemical Communications