title: Single-molecule imaging reveals the stoichiometry change of β2-adrenergic receptors by a pharmacological biased ligand.
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.
authors.affiliation: 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.
authors.forename: Yahong
authors.initials: Y
authors.lastname: Sun
authors.forename: Nan
authors.initials: N
authors.lastname: Li
authors.forename: Mingliang
authors.initials: M
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Zhou
authors.forename: Jinghe
authors.initials: J
authors.lastname: Yuan
authors.forename: Rong
authors.initials: R
authors.lastname: Zhao
authors.forename: Jimin
authors.initials: J
authors.lastname: Wu
authors.forename: Zijian
authors.initials: Z
authors.lastname: Li
authors.forename: Youyi
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Fang
mesh_terms: D002227:Carbazoles / Q000737:chemistry / Q000494:pharmacology*; D000077261:Carvedilol; D049452:Green Fluorescent Proteins / Q000819:agonists / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D007545:Isoproterenol / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D008856:Microscopy, Fluorescence; D061848:Optical Imaging; D011412:Propanolamines / Q000737:chemistry / Q000494:pharmacology*; D011433:Propranolol / Q000737:chemistry / Q000494:pharmacology; D018343:Receptors, Adrenergic, beta-2 / Q000378:metabolism*; D013237:Stereoisomerism
chemical_list: D002227:Carbazoles; D008024:Ligands; D011412:Propanolamines; D018343:Receptors, Adrenergic, beta-2; D000077261:Carvedilol; D049452:Green Fluorescent Proteins; D011433:Propranolol; D007545:Isoproterenol