Regulatory role of G protein-coupled estrogen receptor for vascular function and obesity
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We found that the selective stimulation of the intracellular, transmembrane G protein–coupled estrogen receptor (GPER), also known as GPR30, acutely lowers blood pressure after infusion in normotensive rats and dilates both rodent and human arterial blood vessels. Stimulation of GPER blocks vasoconstrictor-induced changes in intracellular calcium concentrations and vascular tone, as well as serum-stimulated cell proliferation of human vascular smooth muscle cells. Deletion of the GPER gene in mice abrogates vascular effects of GPER activation and is associated with visceral obesity. These findings suggest novel roles for GPER in protecting from cardiovascular disease and obesity.
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GPER1 knockout mice are more prone to obesity, insulin resistance, inflammation, and dyslipidemia than control mice.
“GPER1 KO mice are more prone to obesity, insulin resistance, inflammation, and dyslipidemia than control mice (147–149).”
From Metabolic impact of endogenously produced estrogens by adipose tissue in females and males across the lifespan (2025) · cites this paper as [147]
The passage on GPER deletion (labeled Abstract; page unavailable) reports increased body weight and visceral adiposity in knockout mice of both sexes compared with wild-type mice. Our copy does not report that these mice had greater insulin resistance, inflammation, or dyslipidemia; those parts of the claim are unsupported by this source. (LLM, conf=0.88)
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G-Protein-Coupled Estrogen Receptor (GPER) and Sex-Specific Metabolic Homeostasis
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- Authors
- Haas, E., Bhattacharya, I., Brailoiu, E., Damjanović, M., Brailoiu, G. C., Gao, X., Mueller-Guerre, L., Marjon, N. A., Gut, A., Minotti, R., Meyer, M. R., Amann, K., Ammann, E., Perez-Dominguez, A., Genoni, M., Clegg, D. J., Dun, N. J., Resta, T. C., Prossnitz, E. R., & Barton, M.
- Affiliations
- University of Zurich (CH)
- From the Departement für Innere Medizin (E.H., I.B., M.D., L.M.-G., A.G., R.M., M.R.M., E.A., A.P.-D., M.B.), Klinik und Poliklinik für Innere Medizin; and Klinik für Herz- und Gefässchirurgie (M.G.), Universitätsspital Zürich, Switzerland; Department of Pharmacology (E.B., G.C.B., X.G., N.J.D.), Temple University School of Medicine, Philadelphia, Pa; Department of Cell Biology and Physiology (N.A.M., T.C.R., E.R.P.) and University of New Mexico Cancer Center (E.R.P.), University of New Mexico...
- ORCID
- Venue
- Circulation Research
- Published
- 2009-02-13
- Volume
- 104
- Issue
- 3
- Pages
- 288-291
- ISSN
- 0009-7330 (ISSN-L)
- 1524-4571
- PMC
- PMC2782532
- OpenAlex
- W2140002693
- Cited by
- 373
- References
- 18
- Citations by year
- 2026: 8 · 2025: 11 · 2024: 14 · 2023: 18 · 2022: 20 · 2021: 32 · 2020: 21 · 2019: 17 · 2018: 26 · 2017: 27 · 2016: 18 · 2015: 26 · 2014: 22 · 2013: 27 · 2012: 21
- FWCI
- 16.86
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Circulation Research (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Zurich Open Repository and Archive (University of Zurich) (submittedVersion)
- Funders
- Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung (108258)
- National Heart, Lung, and Blood Institute (HL 51314, HL-88192, R01HL051314, HL-77876, R01HL088192, R01HL077876, R01HL090804, HL-90804)
- National Cancer Institute (CA 118743, R01CA116662, R01CA127731, CA 116662, R01CA118743)
- National Institute of Neurological Disorders and Stroke (NS-18710, R37NS018710, R01NS018710)
- 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
- Health Sciences › Medicine › Pharmacology › Apelin-related biomedical research
- Keywords
- G protein-coupled estrogen receptor, GPR30, vascular function, blood pressure, arterial dilatation, intracellular calcium, vascular smooth muscle cell proliferation, visceral obesity, cardiovascular disease, gene deletion
- MeSH terms
- Animals, Blood Pressure, Estradiol, Female, Humans, Male, Mammary Arteries, Mice, Mutant Strains, Obesity, Receptors, Estrogen, Vasodilation, Rats, Sprague-Dawley, Receptors, G-Protein-Coupled, Atherosclerosis, Mice, Rats
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