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GPCR Signaling Regulation: The Role of GRKs and Arrestins
Open accessAbstract
Every animal species expresses hundreds of different G protein-coupled receptors (GPCRs) that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are involved in pretty much every physiological function and in many pathologies. Therefore, GPCRs are targeted by about a third of clinically used drugs. The signaling of most GPCRs via G proteins is terminated by the phosphorylation of active receptor by specific kinases (GPCR kinases, or GRKs) and subsequent binding of arrestin proteins, that selectively recognize active phosphorylated receptors. In addition, GRKs and arrestins play a role in multiple signaling pathways in the cell, both GPCR-initiated and receptor-independent. Here we focus on the mechanisms of GRK- and arrestin-mediated regulation of GPCR signaling, which includes homologous desensitization and redirection of signaling to additional pathways by bound arrestins.
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The Neuroscience of Drug Reward and Addiction
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Fusion protein strategies for cryo-EM study of G protein-coupled receptors
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New light on cortical neuropeptides and synaptic network plasticity
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Metadata
- Authors
- Gurevich, V. V., & Gurevich, E. V.
- Venue
- Frontiers in Pharmacology
- Publisher
- Frontiers Media SA
- Published
- 2019-02-19
- Volume
- 10
- Pages
- 125-125
- ISSN
- 1663-9812 (ISSN-L)
- OpenAlex
- W2917973990
- Cited by
- 545
- References
- 7
- FWCI
- 18.76
- Type
- journal article
- Language
- en
- Open access
- gold
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- Gurevich, V. V., & Gurevich, E. V. (2019). GPCR Signaling Regulation: The Role of GRKs and Arrestins. Frontiers in Pharmacology. https://doi.org/10.3389/fphar.2019.00125
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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