ArticleScientific reports2017
Antagonizing effects of membrane-acting androgens on the eicosanoid receptor OXER1 in prostate cancer.
Article in Scientific reports, 2017. 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, 50 citations in OpenAlex.
- Testosterone and cancers: biological functions, molecular mechanisms and therapy.Molecular cancer · 2026Review
- Sex differences in innate immune cell responses: Impact on cancer immunity and response to therapy.Frontiers in immunology · 2026Review
- The G-protein coupled receptor OXER1 is a tissue redox sensor essential for intestinal epithelial barrier integrity.bioRxiv : the preprint server for biology · 2025Article
- Testosterone acts through the membrane protein GPRC6A to cause cardiac edema in zebrafish embryos.Development (Cambridge, England) · 2024Article
- 5-Oxo-ETE/OXER1: A Link between Tumor Cells and Macrophages Leading to Regulation of Migration.Molecules (Basel, Switzerland) · 2023Article
- Mitogen-Activated Protein Kinase and Nuclear Hormone Receptor Crosstalk in Cancer Immunotherapy.International journal of molecular sciences · 2023Review
- 'Toxic Masculinity': What Is Known about the Role of Androgen Receptors in Head and Neck Squamous Cell Carcinoma.International journal of molecular sciences · 2023Review
- Membrane-Initiated Estrogen, Androgen, and Progesterone Receptor Signaling in Health and Disease.Endocrine reviews · 2022Review
- From Traditional Ethnopharmacology to Modern Natural Drug Discovery: A Methodology Discussion and Specific Examples.Molecules (Basel, Switzerland) · 2022Review
- A review of non-prostanoid, eicosanoid receptors: expression, characterization, regulation, and mechanism of action.Journal of cell communication and signaling · 2022Review
- Endocrine Disruptors and Prostate Cancer.International journal of molecular sciences · 2022Review
- Targeting the OXE receptor with a selective antagonist inhibits allergen-induced pulmonary inflammation in non-human primates.British journal of pharmacology · 2022Article
- Diverse role of androgen action in human breast cancer.Endocrine oncology (Bristol, England) · 2022Review
- New Antagonists of the Membrane Androgen Receptor OXER1 from the ZINC Natural Product Database.ACS omega · 2021Article
- Review
- The Interface of Nuclear and Membrane Steroid Signaling.Endocrinology · 2021Review
- Binding of Androgen- and Estrogen-Like Flavonoids to Their Cognate (Non)Nuclear Receptors: A Comparison by Computational Prediction.Molecules (Basel, Switzerland) · 2021Article
- OXER1 and RACK1-associated pathway: a promising drug target for breast cancer progression.Oncogenesis · 2020Article
- Targeting the OXE receptor as a potential novel therapy for asthma.Biochemical pharmacology · 2020Review
- A simple open source bioinformatic methodology for initial exploration of GPCR ligands' agonistic/antagonistic properties.Pharmacology research & perspectives · 2020Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Accumulating evidence during the last decades revealed that androgen can exert membrane initiated actions that involve signaling via specific kinases and the modulation of significant cellular processes, important for prostate cancer cell growth and metastasis. Results of the present work clearly show that androgens can specifically act at the membrane level via the GPCR oxoeicosanoid receptor 1 (OXER1) in prostate cancer cells. In fact, OXER1 expression parallels that of membrane androgen binding in prostate cancer cell lines and tumor specimens, while in silico docking simulation of OXER1 showed that testosterone could bind to OXER1 within the same grove as 5-OxoETE, the natural ligand of OXER1. Interestingly, testosterone antagonizes the effects of 5-oxoETE on specific signaling pathways and rapid effects such as actin cytoskeleton reorganization that ultimately can modulate cell migration and metastasis. These findings verify that membrane-acting androgens exert specific effects through an antagonistic interaction with OXER1. Additionally, this interaction between androgen and OXER1, which is an arachidonic acid metabolite receptor expressed in prostate cancer, provides a novel link between steroid and lipid actions and renders OXER1 as new player in the disease. These findings should be taken into account in the design of novel therapeutic approaches in prostate cancer.
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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.