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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GPR30, renamed GPER1, transmits estrogen signals from the membrane.
“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]
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.
“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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The G-protein-coupled estrogen receptor GPER in health and disease
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Copper activates HIF-1α/GPER/VEGF signalling in cancer cells
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Self-citationPosition paper: The membrane estrogen receptor GPER – Clues and questions
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Self-citationAnalysis, occurrence, and function of 9-cis-retinoic acid
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GPR30 Regulates Glutamate Transporter GLT-1 Expression in Rat Primary Astrocytes
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Self-citationIdentification of the estrogen receptor GPER in neoplastic and non-neoplastic human testes
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Estrogen Facilitates Spinal Cord Synaptic Transmission via Membrane-bound Estrogen Receptors
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Deciphering the selective androgen receptor modulators paradigm
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GPER activates Notch signaling in breast cancer cells and cancer-associated fibroblasts (CAFs)
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Self-citationNeuronal Control of Breathing: Sex and Stress Hormones
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- 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 › Genetics › 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
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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