G-protein-coupled receptor kinase 2 terminates G-protein-coupled receptor function in steroid hormone 20-hydroxyecdysone signaling
Open accessAbstract
G-protein-coupled receptors (GPCRs) transmit extracellular signals across the cell membrane. GPCR kinases (GRKs) desensitize GPCR signals in the cell membrane. However, the role and mechanism of GRKs in the desensitization of steroid hormone signaling are unclear. In this study, we propose that GRK2 is phosphorylated by protein kinase C (PKC) in response to induction by the steroid hormone 20-hydroxyecdysone (20E), which determines its translocation to the cell membrane of the lepidopteran Helicoverpa armigera. GRK2 protein expression is increased during the metamorphic stage because of induction by 20E. Knockdown of GRK2 in larvae causes accelerated pupation, an increase in 20E-response gene expression and advanced apoptosis and metamorphosis. 20E induces translocation of GRK2 from the cytoplasm to the cell membrane via steroid hormone ecdysone-responsive GPCR (ErGPCR-2). GRK2 is phosphorylated by PKC on serine 680 after induction by 20E, which leads to the translocation of GRK2 to the cell membrane. GRK2 interacts with ErGPCR-2. These data indicate that GRK2 terminates the ErGPCR-2 function in 20E signaling in the cell membrane by a negative feedback mechanism.
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GRK2 terminates the ErGPCR-2 function in 20E signaling at the cell membrane via a negative feedback mechanism.
“Therefore, GRK2 terminates the ErGPCR-2 function in 20E signaling at the cell membrane via a negative feedback mechanism [63].”
From G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone (2020) · cites this paper as [63]
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References 51 · Cited by 12
- Authors
- Zhao, W.-L., Wang, D., Liu, C.-Y., & Zhao, X.-F.
- Affiliations
- Shandong University (CN)
- Corresponding author
- Zhao, Xiao-Fan
- Venue
- Scientific Reports
- Published
- 2016-07-14
- Volume
- 6
- Issue
- 1
- Pages
- 29205-29205
- ISSN
- 2045-2322 (ISSN-L)
- PMC
- PMC4944123
- OpenAlex
- W2471628533
- Cited by
- 12
- References
- 51
- Citations by year
- 2026: 2 · 2025: 1 · 2023: 1 · 2021: 2 · 2020: 4 · 2019: 1 · 2016: 1
- FWCI
- 0.35
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Locations
- Scientific Reports (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (973 Program, 31230067)
- National Key Research and Development Program of China (2012CB114101)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurobiology and Insect Physiology Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Keywords
- G protein-coupled receptor kinase 2, GRK2, 20-hydroxyecdysone, ecdysone signaling, steroid hormone signaling, receptor desensitization, protein kinase C phosphorylation, Helicoverpa armigera, metamorphosis, negative feedback regulation, apoptosis
- MeSH terms
- Animals, Cell Membrane, Cytoplasm, Ecdysterone, Larva, Lepidoptera, Phosphorylation, Protein Kinase C, Signal Transduction, Gene Expression Regulation, Developmental, Protein Transport, G-Protein-Coupled Receptor Kinase 2
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