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The unfolding stories of GPR30, a new membrane-bound estrogen receptor
Open accessAbstract
Steroid hormones such as estrogens are known to signal through ligand-regulated transcription factors of the nuclear receptor superfamily. In addition, they elicit rapid nongenomic responses from membrane-associated receptors. One of these receptors belongs to an entirely different family of proteins. The G protein-coupled and seven-transmembrane receptor, GPR30, is now widely recognized as an estrogen receptor (ER), hence its official new acronym GPER. It appears to mediate a wide range of responses to estrogen in a large variety of cell types. Its functions are clearly distinct from those of the classical nuclear ERs, although these pathways may overlap and interact in some cases. Here, we review the history of the discovery of this new ER, the evidence for the claim that it is an ER, its signal transduction, and its potential functions in physiology and disease.
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“The estrogen receptor GPCR (GPR30) [23], which transmits estrogen signals from the membrane [24], has been renamed as G protein-coupled estrogen receptor 1 (GPER1) [25].”
From G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone (2020) · cites this paper as [25]
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“GPR30 is suggested as the cell membrane receptor for the steroid hormone estrogen by detection of the binding of fluorescence-labeled estrogen in Cos7 cells [25].”
From G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone (2020) · cites this paper as [25]
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Acconcia, F., Pallottini, V., & Marino, M. (2015) · Dose-Response · doi:10.1177/1559325815610582 · Cited by 425
Metadata
- Authors
- Maggiolini, M., & Picard, D.
- Affiliations
- University of Calabria (IT)
- University of Geneva (CH)
- Venue
- Journal of Endocrinology
- Publisher
- Bioscientifica
- Published
- 2009-09-18
- Volume
- 204
- Issue
- 2
- Pages
- 105-114
- ISSN
- 0022-0795 (ISSN-L)
- 1479-6805
- OpenAlex
- W2123476163
- Cited by
- 360
- References
- 94
- Citations by year
- 2026: 5 · 2025: 7 · 2024: 5 · 2023: 9 · 2022: 8 · 2021: 11 · 2020: 24 · 2019: 22 · 2018: 20 · 2017: 21 · 2016: 22 · 2015: 37 · 2014: 30 · 2013: 38 · 2012: 35
- FWCI
- 3.18
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Journal of Endocrinology (publishedVersion)
- PubMed (publishedVersion)
- Archive of Doctoral Theses and Digital Collections (University of Calabria) (submittedVersion)
- Archive ouverte UNIGE (University of Geneva) (submittedVersion)
- Archive ouverte UNIGE (University of Geneva) (submittedVersion, cc-by)
- Funders
- National Science Foundation
- Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung
- Associazione Italiana per la Ricerca sul Cancro
- Fondation Medic
- Regione Calabria
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Physical Sciences › Environmental Science › Health, Toxicology and Mutagenesis › Effects and risks of endocrine disrupting chemicals
- Keywords
- GPR30, G protein-coupled estrogen receptor, membrane-bound estrogen receptor, estrogen signaling, G protein-coupled receptors, signal transduction, nuclear estrogen receptor
- MeSH terms
- Animals, Carcinoma, Humans, Receptors, Estrogen, Signal Transduction, Receptors, G-Protein-Coupled
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