Abstract
The estrogen receptor is a regulator of a wide range of physiological functions, including the female reproductive system, in addition to bone, cardiovascular and CNS function. ER ligands have been approved for the treatment of menopausal symptoms, breast cancer and osteoporosis, however the search continues for new modulators of ER function with improved properties. Progress in medicinal chemistry programs has resulted in the identification of structurally diverse molecules with unique biological properties. Recent advances in the design and synthesis of these non-steroidal and steroidal estrogen receptor ligands is reviewed. The relationship between the structural features of the ligand and receptor function is also discussed.
Keywords: estrogen receptor modulators, steroidal estrogen receptor ligands, menopausal symptoms, estrogen receptor
Current Topics in Medicinal Chemistry
Title: Estrogen Receptor Modulators: Relationships of Ligand Structure, Receptor Affinity and Functional Activity
Volume: 3 Issue: 14
Author(s): Owen B. Wallace, Timothy I. Richardson and Jeffrey A. Dodge
Affiliation:
Keywords: estrogen receptor modulators, steroidal estrogen receptor ligands, menopausal symptoms, estrogen receptor
Abstract: The estrogen receptor is a regulator of a wide range of physiological functions, including the female reproductive system, in addition to bone, cardiovascular and CNS function. ER ligands have been approved for the treatment of menopausal symptoms, breast cancer and osteoporosis, however the search continues for new modulators of ER function with improved properties. Progress in medicinal chemistry programs has resulted in the identification of structurally diverse molecules with unique biological properties. Recent advances in the design and synthesis of these non-steroidal and steroidal estrogen receptor ligands is reviewed. The relationship between the structural features of the ligand and receptor function is also discussed.
Export Options
About this article
Cite this article as:
Wallace B. Owen, Richardson I. Timothy and Dodge A. Jeffrey, Estrogen Receptor Modulators: Relationships of Ligand Structure, Receptor Affinity and Functional Activity, Current Topics in Medicinal Chemistry 2003; 3 (14) . https://dx.doi.org/10.2174/1568026033451727
DOI https://dx.doi.org/10.2174/1568026033451727 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Novel Mechanisms of Anticancer Activities of Green Tea Component Epigallocatechin- 3-Gallate
Anti-Cancer Agents in Medicinal Chemistry Role of EGFR Inhibitors in the Treatment of Central Nervous System Metastases from Non-Small Cell Lung Cancer
Current Cancer Drug Targets Thirty Years of Polyamine-Related Approaches to Cancer Therapy. Retrospect and Prospect. Part 1. Selective Enzyme Inhibitors
Current Drug Targets MUC Glycoproteins: Potential Biomarkers and Molecular Targets for Cancer Therapy
Current Cancer Drug Targets Molecular Approach to Targeted Therapy for Multiple Sclerosis
CNS & Neurological Disorders - Drug Targets SIRT1 as a Promising Novel Therapeutic Target for Myocardial Ischemia Reperfusion Injury and Cardiometabolic Disease
Current Drug Targets Increasing Testosterone Levels and Effects on Cognitive Functions in Elderly Men and Women: A Review
Current Drug Targets - CNS & Neurological Disorders Drug Transport Across the Placenta
Current Pharmaceutical Biotechnology Adjuvant Hormonal Therapy in Women with Early-stage Breast Cancer
Medicinal Chemistry Caring for HIV-Infected Patients in the ICU in The Highly Active Antiretroviral Therapy Era
Current HIV Research Insights into the Role of Matrix Metalloproteinases and Tissue Inhibitor of Metalloproteinases in Health and Disease
Current Chemical Biology Cardiovascular Risk in Patients with Primary Hyperparathyroidism
Current Pharmaceutical Design Treatment of Lung Cancer Using Nanoparticle Drug Delivery Systems
Current Drug Discovery Technologies Natural Terpenoids Against Female Breast Cancer: A 5-year Recent Research
Current Medicinal Chemistry Predicting Targeted Polypharmacology for Drug Repositioning and Multi- Target Drug Discovery
Current Medicinal Chemistry The Role of Microbiota and Probiotics in Stress-Induced Gastrointestinal Damage
Current Molecular Medicine 7-prenyloxi-6-methoxycoumarin from Polygala sabulosa A.W. Bennett Regulates p38 MAPK and NF-kB Pathways Inhibiting the Inflammation Induced by Carrageenan in the Mouse Model of Pleurisy
Inflammation & Allergy - Drug Targets (Discontinued) Clinical Pharmacology of Trastuzumab
Current Clinical Pharmacology Present Drug Therapy of Demyelinating Disorders
Current Drug Therapy Resistance to Radiotherapy and Targeted Molecular Therapies in Squamous Cell Carcinomas of the Head and Neck, Preclinical Data and New Approaches
Current Signal Transduction Therapy