Mechanisms of estrogen signaling and gene expression via GPR30

Prossnitz, Eric R.; Maggiolini, Marcello

doi:10.1016/j.mce.2009.03.026

Cited by 346Estrogen and related hormone effectsReceptor Mechanisms and SignalingEffects and risks of endocrine disrupting chemicals

Mechanisms of estrogen signaling and gene expression via GPR30

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Prossnitz, Eric R., Maggiolini, Marcello·2009·Molecular and Cellular Endocrinology

DOI 10.1016/j.mce.2009.03.026PMC PMC2847286

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Abstract

The effects of estrogen are widespread throughout the body. Although the classical nuclear estrogen receptors have been known for many years to decades and their primary modes of action as transcriptional regulators is well understood, certain aspects of estrogen biology remain inconsistent with the mechanisms of action of these receptor. More recently, the G protein-coupled receptor, GPR30/GPER, has been suggested to contribute to some of the cellular and physiological effects of estrogen. Not only does GPR30 mediate some of the rapid signal transduction events following cell stimulation, such as calcium mobilization and kinase activation, it also appears to regulate rapid transcriptional activation of genes such as c-fos. Since many cells and tissues co-express classical estrogen receptors and GPR30, there exists great diversity in the possible avenues of synergism and antagonism. In this review, we will provide an overview of GPR30 function, focusing on the rapid signaling events that culminate in the transcriptional activation of certain genes.

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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 [24]
GPR30 can act as the membrane receptor for estrogen.
“A G-protein-coupled seven transmembrane receptor (GPR30) can act as the membrane receptor for estrogen [12]”
From G-protein-coupled receptor participates in 20-hydroxyecdysone signaling on the plasma membrane (2014) · cites this paper as [12]

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Authors: Prossnitz, E. R., & Maggiolini, M.
Affiliations: University of New Mexico (US)
University of Calabria (IT)
Corresponding author: Prossnitz, Eric R.
Maggiolini, Marcello
ORCID: Prossnitz, Eric R.
Maggiolini, Marcello
Venue: Molecular and Cellular Endocrinology
Publisher: Elsevier BV
Published: 2009-09
Volume: 308
Issue: 1-2
Pages: 32-38
ISSN: 0303-7207 (ISSN-L)
DOI: 10.1016/j.mce.2009.03.026
PMC: PMC2847286
OpenAlex: W2078275530
Cited by: 346
References: 86
Citations by year: 2026: 6 · 2025: 7 · 2024: 4 · 2023: 19 · 2022: 15 · 2021: 16 · 2020: 28 · 2019: 23 · 2018: 25 · 2017: 12 · 2016: 22 · 2015: 26 · 2014: 26 · 2013: 25 · 2012: 32
FWCI: 2.87
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Molecular and Cellular Endocrinology (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Institute of Mental Health (MH-084690, U54MH074425, U54MH084690)
National Cancer Institute (CA 118743, R01CA116662, R01CA127731, CA 116662, CA-127731, R01CA118743)
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, estrogen signaling, rapid estrogen signaling, calcium mobilization, kinase activation, c-fos, transcriptional activation
MeSH terms: Animals, Estrogens, Humans, Receptors, Estrogen, Signal Transduction, Transcriptional Activation, Gene Expression, Receptors, G-Protein-Coupled

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Mechanisms of estrogen signaling and gene expression via GPR30

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