Role of beta-arrestin in mediating agonist-promoted G protein-coupled receptor internalization.
beta-Arrestins are proteins that bind phosphorylated heterotrimeric GTP-binding protein (G protein)-coupled receptors (GPCRs) and contribute to the desensitization of GPCRs by uncoupling the signal transduction process. Resensitization of GPCR responsiveness involves agonist-mediated receptor sequestration. Overexpression of beta-arrestins in human embryonic kidney cells rescued the sequestration of beta 2-adrenergic receptor (beta 2AR) mutants defective in their ability to sequester, an effect enhanced by simultaneous overexpression of beta-adrenergic receptor kinase 1. Wild-type beta 2AR sequestration was inhibited by the overexpression of two beta-arrestin mutants. These findings suggest that beta-arrestins play an integral role in GPCR internalization and thus serve a dual role in the regulation of GPCR function.
Duke Scholars
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- beta-Arrestins
- beta-Adrenergic Receptor Kinases
- Transfection
- Receptors, Adrenergic, beta-2
- Point Mutation
- Phosphorylation
- Mutation
- Isoproterenol
- Humans
- General Science & Technology
Citation
Published In
DOI
ISSN
Publication Date
Volume
Issue
Start / End Page
Location
Related Subject Headings
- beta-Arrestins
- beta-Adrenergic Receptor Kinases
- Transfection
- Receptors, Adrenergic, beta-2
- Point Mutation
- Phosphorylation
- Mutation
- Isoproterenol
- Humans
- General Science & Technology