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Role of β-Arrestin in Mediating Agonist-Promoted G Protein-Coupled Receptor Internalization
Abstract
β-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 β-arrestins in human embryonic kidney cells rescued the sequestration of β 2 -adrenergic receptor (β 2 AR) mutants defective in their ability to sequester, an effect enhanced by simultaneous overexpression of β-adrenergic receptor kinase 1. Wild-type β 2 AR sequestration was inhibited by the overexpression of two β-arrestin mutants. These findings suggest that β-arrestins play an integral role in GPCR internalization and thus serve a dual role in the regulation of GPCR function.
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Cited by
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McMahon, H. T., & Boucrot, E. (2011) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm3151 · Cited by 2,223
Oakley, R. H., Laporte, S. A., Holt, J. A., Barak, L. S., & Caron, M. G. (1999) · Journal of Biological Chemistry · doi:10.1074/jbc.274.45.32248 · Cited by 567
Self-citationKirchhausen, T. (2000) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.69.1.699 · Cited by 560
Kirchhausen, T. (2000) · Nature Reviews Molecular Cell Biology · doi:10.1038/35043117 · Cited by 560
Claing, A. (2002) · Progress in Neurobiology · doi:10.1016/s0301-0082(01)00023-5 · Cited by 519
Metadata
- Authors
- Ferguson, S. S. G., Downey, W. E., Colapietro, A.-M., Barak, L. S., Ménard, L., & Caron, M. G.
- Venue
- Science
- Published
- 1996-01-19
- Volume
- 271
- Issue
- 5247
- Pages
- 363-366
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2135319033
- Cited by
- 972
- References
- 0
- FWCI
- 26.35
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Role of β-Arrestin in Mediating Agonist-Promoted G Protein-Coupled Receptor Internalization. https://app.cochat.ai/papers/10.1126/science.271.5247.363
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- Ferguson, S. S. G., Downey, W. E., Colapietro, A.-M., Barak, L. S., Ménard, L., & Caron, M. G. (1996). Role of β-Arrestin in Mediating Agonist-Promoted G Protein-Coupled Receptor Internalization. Science. https://doi.org/10.1126/science.271.5247.363
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Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.