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