ArticleScience translational medicine2020
Preclinical efficacy of the GPER-selective agonist G-1 in mouse models of obesity and diabetes.
Article in Science translational medicine, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 64 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Who cites it
64 citing papers in PubMed, 105 citations in OpenAlex.
- Tranexamic acid protects human dermal fibroblasts from D-galactose-induced senescence via the GPR30/MAPK pathway.Annals of medicine · 2026Trial
- Quercetin alleviates endoplasmic reticulum stress and apoptosis through activation of g protein-coupled estrogen receptor signaling in laying hens with fatty liver hemorrhagic syndrome.Poultry science · 2026Article
- Review
- GPER agonist G1 suppresses neuronal apoptosis mediated by endoplasmic reticulum stress after exertional heat stroke injury.Scientific reports · 2026Article
- Longitudinal association of frailty levels with knee osteoarthritis in middle-aged and elderly chinese: a longitudinal cohort study.Scientific reports · 2026Article
- Multidimensional regulation of estrogen signaling in pelvic floor connective tissue homeostasis and remodeling.Frontiers in immunology · 2026Review
- Neuroendocrine crosstalk between sex and metabolic hormones: mechanisms and implications across the female reproductive spectrum.Discover endocrinology and metabolism · 2026Review
- GPER1 as a therapeutic target in MASLD: evidence for steatosis attenuation by agonist G1 in preclinical models.Frontiers in pharmacology · 2026Article
- G Protein-Coupled Estrogen Receptor Regulates Mesenchymal Stem Cell Mechanotransduction and Differentiation.Cellular and molecular bioengineering · 2025Article
- GPER in metabolic homeostasis and disease: molecular mechanisms, nutritional regulation, and therapeutic potential.Journal of translational medicine · 2025Review
- G-Protein-Coupled Estrogen Receptor (GPER) in Inflammatory Myopathies.Neurology international · 2025Article
- G-protein-coupled estrogen receptor-1 facilitates chondrocyte proliferation in pubertal epiphyseal growth plate via PTHrP/Ihh regulation.Bone & joint research · 2025Article
- Female sex hormones exacerbate retinal neurodegeneration.Science advances · 2025Article
- GPR30-driven fatty acid oxidation targeted by ginsenoside Rd maintains mitochondrial redox homeostasis to restore vascular barrier in diabetic retinopathy.Cardiovascular diabetology · 2025Article
- Article
- Beyond Hormone Replacement: Multifaceted Effects of Phytoestrogens for Optimizing Kinesiological and Physiological Adaptations in Postmenopausal Women.Clinical interventions in aging · 2025Review
- The GPR30 agonist G-1 promotes hair growth via Wnt/Hedgehog signaling in mice.Frontiers in pharmacology · 2025Article
- GPER expression prevents estrogen-induced urinary retention in obese mice.The Journal of steroid biochemistry and molecular biology · 2024Article
- Effects of the Pituitary-targeted Gland Axes on Hepatic Lipid Homeostasis in Endocrine-associated Fatty Liver Disease-A Concept Worth Revisiting.Journal of clinical and translational hepatology · 2024Review
- Selective Activation of G Protein-coupled Estrogen Receptor 1 Attenuates Atherosclerosis.Current medicinal chemistry · 2024Review
4 more citing papers are in PubMed but not listed here.
Corrections and comments
- Erratum issued
Authors and funding
11 authors at 4 institutions in 1 country.
Funding
Abstract
Human obesity has become a global health epidemic, with few safe and effective pharmacological therapies currently available. The systemic loss of ovarian estradiol (E2) in women after menopause greatly increases the risk of obesity and metabolic dysfunction, revealing the critical role of E2 in this setting. The salutary effects of E2 are traditionally attributed to the classical estrogen receptors ERα and ERβ, with the contribution of the G protein-coupled estrogen receptor (GPER) still largely unknown. Here, we used ovariectomy- and diet-induced obesity (DIO) mouse models to evaluate the preclinical activity of GPER-selective small-molecule agonist G-1 (also called Tespria) against obesity and metabolic dysfunction. G-1 treatment of ovariectomized female mice (a model of postmenopausal obesity) reduced body weight and improved glucose homeostasis without changes in food intake, fuel source usage, or locomotor activity. G-1-treated female mice also exhibited increased energy expenditure, lower body fat content, and reduced fasting cholesterol, glucose, insulin, and inflammatory markers but did not display feminizing effects on the uterus (imbibition) or beneficial effects on bone health. G-1 treatment of DIO male mice did not elicit weight loss but prevented further weight gain and improved glucose tolerance, indicating that G-1 improved glucose homeostasis independently of its antiobesity effects. However, in ovariectomized DIO female mice, G-1 continued to elicit weight loss, reflecting possible sex differences in the mechanisms of G-1 action. In conclusion, this work demonstrates that GPER-selective agonism is a viable therapeutic approach against obesity, diabetes, and associated metabolic abnormalities in multiple preclinical male and female models.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.