Abstract
A range of cutting-edge techniques have been employed to visualize 'megaplexes' consisting of a G protein-coupled receptor (GPCR) bound to β-arrestin in intracellular endosomes following agonist-induced internalization. Surprisingly, the complex includes simultaneous binding of the heterotrimeric G protein, which retains full functional activity and supports sustained signaling from within the cell.
Copyright © 2016 Elsevier Ltd. All rights reserved.
MeSH terms
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Adrenergic beta-2 Receptor Agonists / pharmacology
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Adrenergic beta-2 Receptor Antagonists / pharmacology
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Bioluminescence Resonance Energy Transfer Techniques
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Biosensing Techniques / methods
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Cyclic AMP / biosynthesis*
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Deamino Arginine Vasopressin / pharmacology
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Endosomes / drug effects
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Endosomes / metabolism
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Fluorescence Resonance Energy Transfer
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Gene Expression Regulation
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HEK293 Cells
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Humans
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Isoproterenol / pharmacology
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Models, Molecular
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Molecular Probes / chemistry
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Propanolamines / pharmacology
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Protein Binding
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Receptors, Adrenergic, beta-2 / chemistry
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Receptors, Adrenergic, beta-2 / genetics
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Receptors, Adrenergic, beta-2 / metabolism*
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Receptors, Vasopressin / chemistry
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Receptors, Vasopressin / genetics
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Receptors, Vasopressin / metabolism*
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Recombinant Fusion Proteins / chemistry
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Recombinant Fusion Proteins / genetics
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Recombinant Fusion Proteins / metabolism
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Signal Transduction*
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beta-Arrestin 1 / chemistry
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beta-Arrestin 1 / genetics
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beta-Arrestin 1 / metabolism*
Substances
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ARRB1 protein, human
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Adrenergic beta-2 Receptor Agonists
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Adrenergic beta-2 Receptor Antagonists
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Molecular Probes
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Propanolamines
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Receptors, Adrenergic, beta-2
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Receptors, Vasopressin
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Recombinant Fusion Proteins
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beta-Arrestin 1
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ICI 118551
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Cyclic AMP
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Deamino Arginine Vasopressin
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Isoproterenol