Abstract
Estrogen receptors (ERs) are proteins that mediate the action of estradiol and a series of natural and synthetic chemicals that mimic the estradiol structure. Estrogenic action was initially attributed to a single type of ER, now known as ERα, but ERβ was discovered in 1995. Tissue specific distribution and the intensity of expression of these proteins determine the first response of tissues to estrogenic compounds. Estrogens and ERs play a major role in the origin and progression of breast cancer, and antiestrogens that block ER function are useful for breast cancer prevention and treatment. Estrogen mimetics, however, do not fall into distinct categories of agonists and antagonists, since their action is regulated by tissue-specific expression of a number of auxiliary proteins called coactivators or corepressors. In addition, small molecules such as polyamines, fattyacids, and thioredoxin may modulate ER function. Estrogenic functions encompass multiple organ systems, including the reproductive, skeletal, cardiovascular, and nervous system. Estrogens are critical for bone remodeling and mineralization so that estrogen replacement therapy is proven to strengthen bone health in post-menopausal women. Ideally, selective blockade of ER function in breast epithelial cells should be accompanied by growth support on bone and cardiovascular systems. The details of estrogenic function in different organs are to be fully realized, in order to better utilize selective estrogen receptor modulators (SERMs) to fight not only breast cancer but also osteoporosis and cardiovascular diseases. Current research on SERMs points toward accomplishing this goal by exploiting ER as a versatile target against multiple diseases.
Keywords: estrogens, estrogen receptor, selective estrogen receptor modulator, breast cancer, osteoporosis, cardiovascular diseases, hormone replacement therapy
Current Cancer Drug Targets
Title: Estrogen Receptors as Targets for Drug Development for Breast Cancer, Osteoporosis and Cardiovascular Diseases
Volume: 4 Issue: 6
Author(s): Thresia Thomas, Michael A. Gallo and T. J. Thomas
Affiliation:
Keywords: estrogens, estrogen receptor, selective estrogen receptor modulator, breast cancer, osteoporosis, cardiovascular diseases, hormone replacement therapy
Abstract: Estrogen receptors (ERs) are proteins that mediate the action of estradiol and a series of natural and synthetic chemicals that mimic the estradiol structure. Estrogenic action was initially attributed to a single type of ER, now known as ERα, but ERβ was discovered in 1995. Tissue specific distribution and the intensity of expression of these proteins determine the first response of tissues to estrogenic compounds. Estrogens and ERs play a major role in the origin and progression of breast cancer, and antiestrogens that block ER function are useful for breast cancer prevention and treatment. Estrogen mimetics, however, do not fall into distinct categories of agonists and antagonists, since their action is regulated by tissue-specific expression of a number of auxiliary proteins called coactivators or corepressors. In addition, small molecules such as polyamines, fattyacids, and thioredoxin may modulate ER function. Estrogenic functions encompass multiple organ systems, including the reproductive, skeletal, cardiovascular, and nervous system. Estrogens are critical for bone remodeling and mineralization so that estrogen replacement therapy is proven to strengthen bone health in post-menopausal women. Ideally, selective blockade of ER function in breast epithelial cells should be accompanied by growth support on bone and cardiovascular systems. The details of estrogenic function in different organs are to be fully realized, in order to better utilize selective estrogen receptor modulators (SERMs) to fight not only breast cancer but also osteoporosis and cardiovascular diseases. Current research on SERMs points toward accomplishing this goal by exploiting ER as a versatile target against multiple diseases.
Export Options
About this article
Cite this article as:
Thomas Thresia, Gallo A. Michael and Thomas J. T., Estrogen Receptors as Targets for Drug Development for Breast Cancer, Osteoporosis and Cardiovascular Diseases, Current Cancer Drug Targets 2004; 4 (6) . https://dx.doi.org/10.2174/1568009043332880
DOI https://dx.doi.org/10.2174/1568009043332880 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
Related Articles
-
Genetic Polymorphism and Tumor Immunotherapy
Current Pharmacogenomics Systemic Fungal Infections Caused by Candida Species: Epidemiology, Infection Process and Virulence Attributes
Current Drug Targets DNA Recognition by a Novel Bis-Intercalator, Potent Anticancer Drug XR5944
Current Topics in Medicinal Chemistry Anticancer Potential of Calli <i>Versus</i> Seedling Extracts Derived from <i>Rosmarinus officinalis</i> and <i>Coleus hybridus</i>
Current Pharmaceutical Biotechnology Dietary Interventions for Atopic Disorders
Current Pharmaceutical Design A Role of Immunotherapy in Metastatic Malignant Melanoma
Central Nervous System Agents in Medicinal Chemistry Potent New Weapons in the Oncology Arsenal (Antibody-Drug Conjugates) Require Unique Biological Manufacturing Expertise
Current Organic Chemistry Editorial (Thematic Issue: Treatment of Cancer in the Elderly)
Anti-Cancer Agents in Medicinal Chemistry The SCF-type E3 Ubiquitin Ligases as Cancer Targets
Current Cancer Drug Targets Synthesis, Molecular Docking Study and in vitro Anticancer Activity of Tetrazole Linked Benzochromene Derivatives
Anti-Cancer Agents in Medicinal Chemistry Calcium Phosphate System for Gene Delivery: Historical Background and Emerging Opportunities
Current Pharmaceutical Design WT1 Peptide Vaccine as a Paradigm for “Cancer Antigen-Derived Peptide”-Based Immunotherapy for Malignancies: Successful Induction of Anti-Cancer Effect by Vaccination with a Single Kind of WT1 Peptide
Anti-Cancer Agents in Medicinal Chemistry miR-221/222 Confers Radioresistance in Glioblastoma Cells Through Activating Akt Independent of PTEN Status
Current Molecular Medicine Biologic Therapy in Inflammatory and Immunomediated Skin Diseases: Safety Profile
Current Drug Safety Increasing Sensitivity to Radiotherapy and Chemotherapy by Using Novel Biological Agents that Alter the Tumor Microenvironment
Current Molecular Medicine Apixaban - Metabolism, Pharmacologic Properties and Drug Interactions
Current Drug Metabolism Low Dose of Acacetin Promotes Breast Cancer MCF-7 Cells Proliferation Through the Activation of ERK/ PI3K /AKT and Cyclin Signaling Pathway
Recent Patents on Anti-Cancer Drug Discovery Enhancement of the Antiproliferative Activity of Gemcitabine by Modulation of c-Met Pathway in Pancreatic Cancer
Current Pharmaceutical Design Tackling Cardiovascular Risk: New Evidence from Personalized Medicine
Current Pharmacogenomics and Personalized Medicine MYC-Mediated Synthetic Lethality for Treating Tumors
Current Cancer Drug Targets