Abstract
Estrogen plays vital roles in human health and diseases. Estrogen mediates its actions almost entirely by binding to estrogen receptors (ER), alpha and beta which further function as transcription factors. Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to ER and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers and is also approved as the first chemo-preventive agent for lowering breast cancer incidence in high risk women. The therapeutic and preventive efficacy of tamoxifen was initially proven by series of experiments in the laboratory which laid the foundation of its clinical use. Unfortunately, use of tamoxifen is associated with de-novo and acquired resistance and some undesirable side effects. The molecular study of the resistance provides an opportunity to precisely understand the mechanism of SERM action which may further help in designing new and improved SERMs. Recent clinical studies reveal that another SERM, raloxifene, which is primarily used to treat post-menopausal osteoporosis, is as efficient as tamoxifen in preventing breast cancers with fewer side effects. Overall, these findings open a new horizon for SERMs as a class of drug which not only can be used for therapeutic and preventive purposes of breast cancers but also for various other diseases and disorders. Major efforts are therefore directed to make new SERMs with a better therapeutic profile and fewer side effects.
Keywords: Breast cancer, osteoporosis, estrogen receptor, tamoxifen, raloxifene, SERMs, endocrine therapy, drug resistance
Anti-Cancer Agents in Medicinal Chemistry
Title: Potential of Selective Estrogen Receptor Modulators as Treatments and Preventives of Breast Cancer
Volume: 9 Issue: 5
Author(s): Jing Peng, Surojeet Sengupta and V. Craig Jordan
Affiliation:
Keywords: Breast cancer, osteoporosis, estrogen receptor, tamoxifen, raloxifene, SERMs, endocrine therapy, drug resistance
Abstract: Estrogen plays vital roles in human health and diseases. Estrogen mediates its actions almost entirely by binding to estrogen receptors (ER), alpha and beta which further function as transcription factors. Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to ER and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers and is also approved as the first chemo-preventive agent for lowering breast cancer incidence in high risk women. The therapeutic and preventive efficacy of tamoxifen was initially proven by series of experiments in the laboratory which laid the foundation of its clinical use. Unfortunately, use of tamoxifen is associated with de-novo and acquired resistance and some undesirable side effects. The molecular study of the resistance provides an opportunity to precisely understand the mechanism of SERM action which may further help in designing new and improved SERMs. Recent clinical studies reveal that another SERM, raloxifene, which is primarily used to treat post-menopausal osteoporosis, is as efficient as tamoxifen in preventing breast cancers with fewer side effects. Overall, these findings open a new horizon for SERMs as a class of drug which not only can be used for therapeutic and preventive purposes of breast cancers but also for various other diseases and disorders. Major efforts are therefore directed to make new SERMs with a better therapeutic profile and fewer side effects.
Export Options
About this article
Cite this article as:
Peng Jing, Sengupta Surojeet and Jordan Craig V., Potential of Selective Estrogen Receptor Modulators as Treatments and Preventives of Breast Cancer, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (5) . https://dx.doi.org/10.2174/187152009788451833
DOI https://dx.doi.org/10.2174/187152009788451833 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Current Evidence and Potential Mechanisms of Therapeutic Action of PEDF in Cervical Cancer Treatment
Current Molecular Medicine Fyn Kinase in Brain Diseases and Cancer: The Search for Inhibitors
Current Medicinal Chemistry Silibinin – A Promising New Treatment for Cancer
Anti-Cancer Agents in Medicinal Chemistry Pharmacological Modulation of Caspase Activation
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Tumor Stroma as a Target in Cancer
Current Cancer Drug Targets Reviewing the Role of Resveratrol as a Natural Modulator of Microglial Activities
Current Pharmaceutical Design Intestinal Absorption Enhancement Via the Paracellular Route by Fatty Acids, Chitosans and Others: A Target for Drug Delivery
Current Drug Delivery Kruppel-Like Factors 4 and 5: Unity in Diversity
Current Genomics Microwave-Assisted Synthesis and Evaluation of Substituted Aryl Propyl Acridone-4-Carboxamides as Potential Chemosensitizing Agents for Cancer
Letters in Drug Design & Discovery Pharmacoproteomics Applications for Drug Target Discovery in CNS Disorders
Current Pharmacogenomics and Personalized Medicine RNA Splicing Manipulation: Strategies to Modify Gene Expression for a Variety of Therapeutic Outcomes
Current Gene Therapy Alpha-Emitters for Immuno-Therapy: A Review of Recent Developments from Chemistry to Clinics
Current Topics in Medicinal Chemistry Chemoradiotherapy in Locally Advanced, Unresectable Non-Small Cell Lung Cancer
Reviews on Recent Clinical Trials The Role of Metabolism in Toxicity of Polycyclic Aromatic Hydrocarbons and their Non-genotoxic Modes of Action
Current Drug Metabolism The Efficacy and Safety of Additional Anti-HER2-Targeting Drugs in the Treatment of HER2-Positive Advanced Breast Cancer: A Meta-Analysis
Anti-Cancer Agents in Medicinal Chemistry Review of the Contribution of Radiolabelled Tracers for Tumour Cell Status Imaging
Current Medical Imaging Triazene Compounds in the Treatment of Acute Myeloid Leukemia: A Short Review and a Case Report
Current Medicinal Chemistry Recent Advances in Drug Design of Epidermal Growth Factor Receptor Inhibitors
Current Medicinal Chemistry PARP Inhibitor Development for Systemic Cancer Targeting
Anti-Cancer Agents in Medicinal Chemistry Specific Targeted Therapy: A New Tool for the Destruction of Cancer
Current Drug Therapy