ArticleDisease models & mechanisms2015
A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models.
Article in Disease models & mechanisms, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 39 citations in OpenAlex.
- Emerging agents that target signaling pathways in cancer fibroblast cells (Review).International journal of oncology · 2026Review
- GPER in metabolic homeostasis and disease: molecular mechanisms, nutritional regulation, and therapeutic potential.Journal of translational medicine · 2025Review
- Article
- Estrogen dysregulation, intraocular pressure, and glaucoma risk.Experimental eye research · 2023Review
- The G Protein-Coupled Estrogen Receptor (GPER): A Critical Therapeutic Target for Cancer.Cells · 2023Review
- Generation of a Yeast Cell Model Potentially Useful to Identify the Mammalian MitochondrialBiomolecules · 2023Article
- A Picrocrocin-Enriched Fraction from a Saffron Extract Affects Lipid Homeostasis in HepG2 Cells through a Non-Statin-like Mode.International journal of molecular sciences · 2023Article
- Fraisinib: a calixpyrrole derivative reducing A549 cell-derived NSCLC tumorFrontiers in pharmacology · 2023Article
- Two calix[4]pyrroles as potential therapeutics for castration-resistant prostate cancer.Investigational new drugs · 2022Article
- The Interplay of GPER1 with 17β-Aminoestrogens in the Regulation of the Proliferation of Cervical and Breast Cancer Cells: A Pharmacological Approach.International journal of environmental research and public health · 2022Article
- Separation of Mercury(II) from Industrial Wastewater through Polymer Inclusion Membranes with Calix[4]pyrrole Derivative.Membranes · 2022Article
- Article
- Neurodegenerative Disease: Roles for Sex, Hormones, and Oxidative Stress.Endocrinology · 2021Review
- Is the Way to Fight Cancer Paved with Gold? Metal-Based Carbene Complexes with Multiple and Fascinating Biological Features.Pharmaceuticals (Basel, Switzerland) · 2020Article
- A novel GPER antagonist protects against the formation of estrogen-induced cholesterol gallstones in female mice.Journal of lipid research · 2020Article
- Therapeutic Perspectives on the Modulation of G-Protein Coupled Estrogen Receptor, GPER, Function.Frontiers in endocrinology · 2020Review
- G Protein-Coupled Estrogen Receptor, GPER1, Offers a Novel Target for the Treatment of Digestive Diseases.Frontiers in endocrinology · 2020Review
- New dimensions in calix[4]pyrrole: the land of opportunity in supramolecular chemistry.RSC advances · 2019Review
- Sequential ligand- and structure-based virtual screening approach for the identification of potential G protein-coupled estrogen receptor-1 (GPER-1) modulators.RSC advances · 2019Article
- Molecular Engineering of Free-Base Porphyrins as Ligands-The N-H⋅⋅⋅X Binding Motif in Tetrapyrroles.Angewandte Chemie (International ed. in English) · 2019Review
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Estrogens regulate numerous pathophysiological processes, mainly by binding to and activating estrogen receptor (ER)α and ERβ. Increasing amounts of evidence have recently demonstrated that G-protein coupled receptor 30 (GPR30; also known as GPER) is also involved in diverse biological responses to estrogens both in normal and cancer cells. The classical ER and GPER share several features, including the ability to bind to identical compounds; nevertheless, some ligands exhibit opposed activity through these receptors. It is worth noting that, owing to the availability of selective agonists and antagonists of GPER for research, certain differential roles elicited by GPER compared with ER have been identified. Here, we provide evidence on the molecular mechanisms through which a calixpyrrole derivative acts as a GPER antagonist in different model systems, such as breast tumor cells and cancer-associated fibroblasts (CAFs) obtained from breast cancer patients. Our data might open new perspectives toward the development of a further class of selective GPER ligands in order to better dissect the role exerted by this receptor in different pathophysiological conditions. Moreover, calixpyrrole derivatives could be considered in future anticancer strategies targeting GPER in cancer cells.
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Registered trials
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.