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
-
Therapeutic Strategies for Targeting BRAF in Human Cancer
Reviews on Recent Clinical Trials Function and Regulation of Let-7 Family microRNAs
MicroRNA Design, Synthesis, and Biological Evaluation of New Azole Derivatives as Potent Aromatase Inhibitors with Potential Effects against Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry Preclinical and Clinical Studies of Novel Breast Cancer Drugs Targeting Molecules Involved in Protein Kinase C Signaling, the Putative Metastasis-Suppressor Gene Cap43 and the Y-box Binding Protein-1
Current Medicinal Chemistry Development of Novel Therapeutic Drugs in Humans from Plant Antimicrobial Peptides
Current Protein & Peptide Science HGF and RhoGTPases in Cancer Cell Motility
Current Signal Transduction Therapy IAPs as a Target for Anticancer Therapy
Current Cancer Drug Targets Pharmacological Strategies to Overcome HER2 Cross-Talk and Trastuzumab Resistance
Current Medicinal Chemistry Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings
Anti-Cancer Agents in Medicinal Chemistry Properties and Therapeutic Potential of Transient Receptor Potential Channels with Putative Roles in Adversity: Focus on TRPC5, TRPM2 and TRPA1
Current Drug Targets Saponins in Tumor Therapy
Mini-Reviews in Medicinal Chemistry Role of Tyrosine Kinase Inhibitor Molecules in Non Small Cell Lung Cancer:From Benchside to Bedside
Current Respiratory Medicine Reviews Cochlear Implants
Current Pharmaceutical Biotechnology Channel-Like Functions of the 18-kDa Translocator Protein (TSPO): Regulation of Apoptosis and Steroidogenesis as Part of the Host-Defense Response
Current Pharmaceutical Design Editorial (Thematic Issue: Novel Anticancer Drugs from Nature)
Current Medicinal Chemistry Study of Parasitic Infections, Cancer, and other Diseases with Mass-Spectrometry and Quantitative Proteome-Disease Relationships
Current Proteomics Sequential Bilateral Internal Jugular Vein Thrombosis: A Case Report and Review of this Rare Medical Entity
Vascular Disease Prevention (Discontinued) Melatonin Treatment Combined with TGF-β Silencing Inhibits Epithelial- Mesenchymal Transition in CF41 Canine Mammary Cancer Cell Line
Anti-Cancer Agents in Medicinal Chemistry Investigating Physical, Psychological and Social Well-being of Older Persons in Jordan
Current Aging Science Delivery Systems for Applications in siRNA Technology
Drug Delivery Letters