Role of beta-arrestin in mediating agonist-promoted G protein-coupled receptor internalization.
Journal Article (Journal Article)
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.
- Ferguson, SS; Downey, WE; Colapietro, AM; Barak, LS; Ménard, L; Caron, MG
- January 19, 1996
Volume / Issue
- 271 / 5247
Start / End Page
- 363 - 366
International Standard Serial Number (ISSN)
Digital Object Identifier (DOI)
- United States