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 |
- 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
-
Pharmacological Strategies to Increase the Antitumor Activity of Methylating Agents
Current Medicinal Chemistry Phage Displayed Biomolecules As Preventive and Therapeutic Agents
Current Pharmaceutical Biotechnology Molecular Mechanisms of Inflammation. Anti-Inflammatory Benefits of Virgin Olive Oil and the Phenolic Compound Oleocanthal
Current Pharmaceutical Design Predicting Cancer-Related MiRNAs Using Expression Profiles in Tumor Tissue
Current Pharmaceutical Biotechnology Phosphotyrosine Phosphatases in Cancer Diagnostic and Treatment
Recent Patents on DNA & Gene Sequences Adenocarcinoma of the Appendix in Elderly: Diagnostic Dilemma
New Emirates Medical Journal The Effects of Probiotics and Prebiotics on Gastrointestinal and Behavioural Symptoms in Autism Spectrum Disorder
Current Reviews in Clinical and Experimental Pharmacology Nanoparticle Systems Modulating Myeloid-Derived Suppressor Cells for Cancer Immunotherapy
Current Topics in Medicinal Chemistry The Toxicogenetics of Antirretroviral Therapy: The Evil Inside
Current Medicinal Chemistry Inflammation in Ischemic Stroke: Mechanisms, Consequences and Possible Drug Targets
CNS & Neurological Disorders - Drug Targets Circular RNAs and Glioma: Small Molecule with Big Actions
Current Molecular Medicine Identification of Novel IRAK-4 Inhibitors Through Pharmacophore Modeling, Atom-based 3D-QSAR, Docking Strategies and Molecular Dynamics Simulation
Letters in Drug Design & Discovery 99mTc-(tricine)-HYNIC-Lys-FROP Peptide for Breast Tumor Targeting
Anti-Cancer Agents in Medicinal Chemistry Insulin-Like Growth Factor 2 - The Oncogene and its Accomplices
Current Pharmaceutical Design Modifying Radiation Damage
Current Drug Targets Status of Flavonols as P-Glycoprotein Inhibitors in Cancer Chemotherapy
Current Cancer Therapy Reviews Preface
Current Cancer Drug Targets Atopic Dermatitis and Cytokines: Recent Patents in Immunoregulatory and Therapeutic Implications of Cytokines in Atopic Dermatitis - Part I: Cytokines in Atopic Dermatitis
Recent Patents on Inflammation & Allergy Drug Discovery Active Metabolites Resulting from Decarboxylation, Reduction and Ester Hydrolysis of Parent Drugs
Current Drug Metabolism Boswellic Acids: Biological Actions and Molecular Targets
Current Medicinal Chemistry