Abstract
Observations on the role of ovarian hormones in breast cancer growth, as well as interest in contraception, stimulated research into the biology of estrogens. The identification of the classical receptors ERα and ERβ and the transmembrane receptor GPER and the resolution of the structure of the ligand bound to its receptor established the principal molecular mechanisms of estrogen action. The presence of estrogen-like compounds in many plants used in traditional medicine or ingested as food ingredients, phytoestrogens, as well as the estrogenic activities of many industrial pollutants and pesticides, xenoestrogens, have prompted investigations into their role in human health. Phyto- and xenoestrogens bind to the estrogen receptors with a lower affinity than the endogenous estrogens and can compete or substitute the hormone. Xenoestrogens, which accumulate in the body throughout life, are believed to increase breast cancer risk, especially in cases of prenatal and prepuberal exposure whereas the role of phytoestrogens is still a matter of debate. At present, the application of phytoestrogens appears to be limited to the treatment of post-menopausal symptoms in women where the production of endogenous estrogens has ceased. In this review we discuss chemistry, structure and classification, estrogen signaling and the consequences of the interactions of estrogens, phytoestrogens and xenoestrogens with their receptors, the complex interactions of endogenous and exogenous ligands, the evaluation of the health risks related to xenoestrogens, and the perspectives toward the synthesis of potent third generation selective estrogen receptor modulators (SERMs).
Keywords: Breast cancer, estrogen receptor-alpha, estrogen receptor-beta, estrogen signaling, phytoestrogens, xenoestrogens, selective estrogen receptor modulators.
Current Medicinal Chemistry
Title:Exogenous Hormonal Regulation in Breast Cancer Cells by Phytoestrogens and Endocrine Disruptors
Volume: 21 Issue: 9
Author(s): A. Albini, C. Rosano, G. Angelini, A. Amaro, A.I. Esposito, S. Maramotti, D.M. Noonan and U. Pfeffer
Affiliation:
Keywords: Breast cancer, estrogen receptor-alpha, estrogen receptor-beta, estrogen signaling, phytoestrogens, xenoestrogens, selective estrogen receptor modulators.
Abstract: Observations on the role of ovarian hormones in breast cancer growth, as well as interest in contraception, stimulated research into the biology of estrogens. The identification of the classical receptors ERα and ERβ and the transmembrane receptor GPER and the resolution of the structure of the ligand bound to its receptor established the principal molecular mechanisms of estrogen action. The presence of estrogen-like compounds in many plants used in traditional medicine or ingested as food ingredients, phytoestrogens, as well as the estrogenic activities of many industrial pollutants and pesticides, xenoestrogens, have prompted investigations into their role in human health. Phyto- and xenoestrogens bind to the estrogen receptors with a lower affinity than the endogenous estrogens and can compete or substitute the hormone. Xenoestrogens, which accumulate in the body throughout life, are believed to increase breast cancer risk, especially in cases of prenatal and prepuberal exposure whereas the role of phytoestrogens is still a matter of debate. At present, the application of phytoestrogens appears to be limited to the treatment of post-menopausal symptoms in women where the production of endogenous estrogens has ceased. In this review we discuss chemistry, structure and classification, estrogen signaling and the consequences of the interactions of estrogens, phytoestrogens and xenoestrogens with their receptors, the complex interactions of endogenous and exogenous ligands, the evaluation of the health risks related to xenoestrogens, and the perspectives toward the synthesis of potent third generation selective estrogen receptor modulators (SERMs).
Export Options
About this article
Cite this article as:
Albini A., Rosano C., Angelini G., Amaro A., Esposito A.I., Maramotti S., Noonan D.M. and Pfeffer U., Exogenous Hormonal Regulation in Breast Cancer Cells by Phytoestrogens and Endocrine Disruptors, Current Medicinal Chemistry 2014; 21 (9) . https://dx.doi.org/10.2174/0929867321666131129124640
DOI https://dx.doi.org/10.2174/0929867321666131129124640 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Dysfunction of Mitochondrial ATP Production As a Target for Personalized Cancer Therapy
Current Pharmacogenomics and Personalized Medicine Mucoadhesive Nanoparticulate System for Oral Drug Delivery: A Review
Current Drug Therapy Hepatitis B Virus X Protein Modulates Chemokine CCL15 Upregulation in Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Evolution of Novel Non-Steroidal Anti-Inflammatory Drugs with Reduced Gastrointestinal Adverse Effects
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Liposomes and Lipid Envelope-Type Systems for Systemic siRNA Delivery
Current Pharmaceutical Design Combined Treatment with PPAR-γ Agonists in Pancreatic Cancer: A Glimmer of Hope for Cancer Therapy?
Current Cancer Drug Targets Influence of Tumor Microenvironment on the Distribution and Elimination of Nano-formulations
Current Drug Metabolism Computational Approaches for the Identification and Optimization of Src Family Kinases Inhibitors
Current Medicinal Chemistry Immune Receptors, Cadherins and their Interactions
Current Immunology Reviews (Discontinued) Heregulin in Breast Cancer: Old Story, New Paradigm
Current Pharmaceutical Design Inflammatory Bowel Disease and Celiac Disease: Overlaps in the Pathology and Genetics, and their Potential Drug Targets
Endocrine, Metabolic & Immune Disorders - Drug Targets Multifunctional Thio-Stabilized Gold Nanoparticles for Near-Infrared Fluorescence Detection and Imaging of Activated Caspase-3
Current Analytical Chemistry ARRDC3 Inhibits the Progression of Human Prostate Cancer Through ARRDC3-ITGβ4 Pathway
Current Molecular Medicine A Simplified Protocol Employing Elacridar in Rodents: A Screening Model in Drug Discovery to Assess P-gp Mediated Efflux at the Blood Brain Barrier
Drug Metabolism Letters Protection of Blood Brain Barrier Integrity and Modulation of Inflammatory Mediators During Treatment of Pneumococcal Meningitis with Daptomycin or Ceftriaxone
Current Neurovascular Research Armed Oncolytic Adenoviruses and Polymer-shielded Nanocomplex for Systemic Delivery
Current Cancer Therapy Reviews Next Generation Antineoplastic Agents: A Review on Structurally Modified Vinblastine (VBL) Analogues
Current Medicinal Chemistry Recent Patents on Proteases and Kinases as Anti-Infective Agents: A Review
Recent Patents on Anti-Infective Drug Discovery Editorial [Hot Topic: Modulation, Absorption and Delivery of Xenobiotics: The Synergic Role of CYP450 and P-gp Activities (Guest Editor: Nicola Antonio Colabufo)]
Current Drug Metabolism Heat Shock Protein 90 Inhibitors as Broad Spectrum Anti-Infectives
Current Pharmaceutical Design