The DOI matches its Crossref record; 82 of the 83 references it cites were found in a registry or an index.
Minireview: G Protein-Coupled Estrogen Receptor-1, GPER-1: Its Mechanism of Action and Role in Female Reproductive Cancer, Renal and Vascular Physiology
Open accessAbstract
Using cDNA cloning strategies commonly employed for G protein-coupled receptors (GPCR), GPCR-30 (GPR30), was isolated from mammalian cells before knowledge of its cognate ligand. GPR30 is evolutionarily conserved throughout the vertebrates. A broad literature suggests that GPR30 is a Gs-coupled heptahelical transmembrane receptor that promotes specific binding of naturally occurring and man-made estrogens but not cortisol, progesterone, or testosterone. Its “pregenomic” signaling actions are manifested by plasma membrane-associated actions familiar to GPCR, namely, stimulation of adenylyl cyclase and Gβγ-subunit protein-dependent release of membrane-tethered heparan bound epidermal growth factor. These facts regarding its mechanism of action have led to the formal renaming of this receptor to its current functional designate, G protein-coupled estrogen receptor (ER) (GPER)-1. Further insight regarding its biochemical action and physiological functions in vertebrates is derived from receptor knockdown studies and the use of selective agonists/antagonists that discriminate GPER-1 from the nuclear steroid hormone receptors, ERα and ERβ. GPER-1-selective agents have linked GPER-1 to physiological and pathological events regulated by estrogen action, including, but not limited to, the central nervous, immune, renal, reproductive, and cardiovascular systems. Moreover, immunohistochemical studies have shown a positive association between GPER-1 expression and progression of female reproductive cancer, a relationship that is diametrically opposed from ER. Unlike ER knockout mice, GPER-1 knockout mice are fertile and show no overt reproductive anomalies. However, they do exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. Here, we discuss the role of GPER-1 in female reproductive cancers as well as renal and vascular physiology.
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In the citing paper
“Estrogen transmits signals via GPERs to transactivate epidermal growth factor receptors for cell proliferation in female reproductive cancers [26].”
From G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone (2020) · cites this paper as [26]
In the citing paper
“GPER1-mediated nongenomic activity is independent of the estrogen nuclear receptor [26].”
From G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone (2020) · cites this paper as [26]
In the citing paper
“GPR30 has shown negligible binding to estrogen (17β-estradiol) in several studies [49], which may be due to the different analytical methods [17].”
From G-protein-coupled receptor participates in 20-hydroxyecdysone signaling on the plasma membrane (2014) · cites this paper as [17]
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2 retracted
Vivacqua, A., Bonofiglio, D., Albanito, L., Madeo, A., Rago, V., Carpino, A., Musti, A. M., Picard, D., Andò, S., & Maggiolini, M. (2006) · Molecular Pharmacology · doi:10.1124/mol.106.026344 · Cited by 280
RetractedAlbanito, L., Lappano, R., Madeo, A., Chimento, A., Prossnitz, E. R., Cappello, A. R., Dolce, V., Abonante, S., Pezzi, V., & Maggiolini, M. (2008) · Environmental Health Perspectives · doi:10.1289/ehp.11297 · Cited by 105
RetractedCloning of a novel receptor expressed in rat prostate and ovary.
Kuiper, G. G. J. M., Enmark, E., Pelto‐Huikko, M., Nilsson, S., & Gustafsson, J.-Α. (1996) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.93.12.5925 · Cited by 4,802
A transmembrane intracellular estrogen receptor mediates rapid cell signaling
Revankar, C. M., Cimino, D. F., Sklar, L. A., Arterburn, J. B., & Prossnitz, E. R. (2005) · Science · doi:10.1126/science.1106943 · Cited by 2,302
Structural Basis of Integrin Regulation and Signaling
Luo, B., Carman, C. V., & Springer, T. A. (2007) · Annual Review of Immunology · doi:10.1146/annurev.immunol.25.022106.141618 · Cited by 1,662
Identity of an Estrogen Membrane Receptor Coupled to a G Protein in Human Breast Cancer Cells
Thomas, P., Pang, Y., Filardo, E. J., & Dong, J. (2004) · Endocrinology · doi:10.1210/en.2004-1064 · Cited by 1,410
Self-citationFilardo, E. J., Quinn, J. A., Bland, K. I., & Frackelton, A. R. (2000) · Molecular Endocrinology · doi:10.1210/mend.14.10.0532 · Cited by 1,387
Self-citationThe G-protein-coupled estrogen receptor GPER in health and disease
Prossnitz, E. R., & Barton, M. (2011) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2011.122 · Cited by 925 · cited 1×
“Excellent reviews have been written about the use of GPER-1-selective ligands, including the GPER-1 agonist G-1 and the GPER-1 antagonist G-15, to investigate disease models (8, 36).”
Blair, R. M. (2000) · Toxicological Sciences · doi:10.1093/toxsci/54.1.138 · Cited by 806
Seifert, R., & Wenzel‐Seifert, K. (2002) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-002-0588-0 · Cited by 657
Research works printed but not linked: 1
- Filardo, 2007, Activation of the novel estrogen receptor G protein coupled receptor 30 (GPR30) at the plasma membrane., Endocrinology, 148, 3236, 10.1210/en.2006-1605 · DOI
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Estrogen receptor signaling mechanisms
Fuentes, N., & Silveyra, P. (2019) · Advances in protein chemistry and structural biology · doi:10.1016/bs.apcsb.2019.01.001 · Cited by 1,082
The Concise Guide to PHARMACOLOGY 2013/14: G Protein‐Coupled Receptors
Alexander, S. P. H., Benson, H. E., Faccenda, E., Pawson, A. J., Sharman, J. L., Spedding, M., Peters, J. A., Harmar, A. J., & Collaborators, C. (2013) · British Journal of Pharmacology · doi:10.1111/bph.12445 · Cited by 561
Progress in the Chemistry of Tetrahydroquinolines
Muthukrishnan, I., Sridharan, V., & Menéndez, J. C. (2019) · Chemical Reviews · doi:10.1021/acs.chemrev.8b00567 · Cited by 512
The many faces of estrogen signaling
Vrtačnik, P., Ostanek, B., Mencej-Bedrač, S., & Marc, J. (2014) · Biochemia Medica · doi:10.11613/bm.2014.035 · Cited by 403
Estrogen biology: New insights into GPER function and clinical opportunities
Prossnitz, E. R., & Barton, M. (2014) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2014.02.002 · Cited by 404
Metadata
- Authors
- Filardo, E. J., & Thomas, P.
- Affiliations
- Brown University (US)
- University of Texas at Austin Marine Science Institute (US)
- Corresponding author
- Filardo, Edward J.
- Venue
- Endocrinology
- Publisher
- The Endocrine Society
- Published
- 2012-04-11
- Volume
- 153
- Issue
- 7
- Pages
- 2953-2962
- ISSN
- 0013-7227 (ISSN-L)
- 1945-7170
- PMC
- PMC3380306
- OpenAlex
- W2137207319
- Cited by
- 366
- References
- 83
- Citations by year
- 2026: 16 · 2025: 10 · 2024: 24 · 2023: 16 · 2022: 18 · 2021: 28 · 2020: 31 · 2019: 30 · 2018: 29 · 2017: 26 · 2016: 28 · 2015: 36 · 2014: 36 · 2013: 29 · 2012: 9
- FWCI
- 4.34
- Type
- journal article
- Language
- en
- Open access
- green
- europepmc.org
- Locations
- Endocrinology (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Cancer Institute (R01CA119165)
- 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
- G protein-coupled estrogen receptor, GPR30, estrogen signaling, female reproductive cancers, renal physiology, vascular physiology, adenylate cyclase, Gβγ subunits, estrogen receptor knockout mice, thymic atrophy, glucose tolerance, bone growth
- MeSH terms
- Animals, Biopsy, Female, Genital Neoplasms, Female, Humans, Kidney, Ligands, Models, Biological, Models, Genetic, Receptors, Estrogen, Transcriptional Activation, Gene Expression Regulation, Neoplastic, Receptors, G-Protein-Coupled, Mice, ErbB Receptors
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