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

Chem Commun (Camb). 2016 Jun 4;52(44):7086-9. doi: 10.1039/c6cc00628k. Epub 2016 Apr 19.

Authors

Yahong Sun¹, Nan Li, Mingliang Zhang, Wei Zhou, Jinghe Yuan, Rong Zhao, Jimin Wu, Zijian Li, Youyi Zhang, Xiaohong Fang

Affiliation

¹ 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. xfang@iccas.ac.cn.

PMID: 27090587
DOI: 10.1039/c6cc00628k

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.

MeSH terms

Carbazoles / chemistry
Carbazoles / pharmacology*
Carvedilol
Green Fluorescent Proteins / agonists
Green Fluorescent Proteins / metabolism
HEK293 Cells
Humans
Isoproterenol / chemistry
Isoproterenol / pharmacology
Ligands
Microscopy, Fluorescence
Optical Imaging*
Propanolamines / chemistry
Propanolamines / pharmacology*
Propranolol / chemistry
Propranolol / pharmacology
Receptors, Adrenergic, beta-2 / metabolism*
Stereoisomerism

Substances

Carbazoles
Ligands
Propanolamines
Receptors, Adrenergic, beta-2
Carvedilol
Green Fluorescent Proteins
Propranolol
Isoproterenol