Abstract
Estrogen receptors, comprised of ERα and ERβ isoforms in mammals, act as ligandmodulated transcription factors and orchestrate a plethora of cellular functions from sexual development and reproduction to metabolic homeostasis. Herein, I revisit the structural basis of the binding of ERα to DNA and estradiol in light of the recent discoveries and emerging trends in the field of nuclear receptors. A particular emphasis of this review is on the chemical and structural diversity of an everincreasing repertoire of physiological, environmental and synthetic ligands of estrogen receptors that ultimately modulate their interactions with cognate DNA located within the promoters of estrogenresponsive genes. In particular, modulation of estrogen receptors by small molecule ligands represents an important therapeutic goal toward the treatment of a wide variety of human pathologies including breast cancer, cardiovascular disease, osteoporosis and obesity. Collectively, this article provides an overview of a wide array of small organic and inorganic molecules that can fine-tune the physiological function of estrogen receptors, thereby bearing a direct impact on human health and disease.
Keywords: Endoestrogens, Estrogen receptors, Metalloestrogens, Phytoestrogens, SERMs, Xenoestrogens.
Current Topics in Medicinal Chemistry
Title:Structural and Functional Diversity of Estrogen Receptor Ligands
Volume: 15 Issue: 14
Author(s): Amjad Farooq
Affiliation:
Keywords: Endoestrogens, Estrogen receptors, Metalloestrogens, Phytoestrogens, SERMs, Xenoestrogens.
Abstract: Estrogen receptors, comprised of ERα and ERβ isoforms in mammals, act as ligandmodulated transcription factors and orchestrate a plethora of cellular functions from sexual development and reproduction to metabolic homeostasis. Herein, I revisit the structural basis of the binding of ERα to DNA and estradiol in light of the recent discoveries and emerging trends in the field of nuclear receptors. A particular emphasis of this review is on the chemical and structural diversity of an everincreasing repertoire of physiological, environmental and synthetic ligands of estrogen receptors that ultimately modulate their interactions with cognate DNA located within the promoters of estrogenresponsive genes. In particular, modulation of estrogen receptors by small molecule ligands represents an important therapeutic goal toward the treatment of a wide variety of human pathologies including breast cancer, cardiovascular disease, osteoporosis and obesity. Collectively, this article provides an overview of a wide array of small organic and inorganic molecules that can fine-tune the physiological function of estrogen receptors, thereby bearing a direct impact on human health and disease.
Export Options
About this article
Cite this article as:
Farooq Amjad, Structural and Functional Diversity of Estrogen Receptor Ligands, Current Topics in Medicinal Chemistry 2015; 15 (14) . https://dx.doi.org/10.2174/1568026615666150413154841
DOI https://dx.doi.org/10.2174/1568026615666150413154841 |
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
-
Simple and Convenient Synthesis of (±)-Bakuchiol
Letters in Organic Chemistry Negative Regulation of NEDD8 Conjugation Pathway by Novel Molecules and Agents for Anticancer Therapy
Current Pharmaceutical Design The Application of X-ray, NMR, and Molecular Modeling in the Design of MMP Inhibitors
Current Topics in Medicinal Chemistry Hepato and Cardiotoxicity of Chemotherapeutic Treatment Evaluated by Means of Small Animal Imaging
Anti-Cancer Agents in Medicinal Chemistry Targeted Nanostructured Lipid Carriers for Delivery of Paclitaxel to Cancer Cells: Preparation, Characterization, and Cell Toxicity
Current Drug Delivery Molecular Field Analysis (MFA) and Other QSAR Techniques in Development of Phosphatase Inhibitors
Anti-Cancer Agents in Medicinal Chemistry Targeting the PI3K/Akt/mTOR Axis by Apigenin for Cancer Prevention
Anti-Cancer Agents in Medicinal Chemistry Ethosomes as Vesicles for Effective Transdermal Delivery: From Bench to Clinical Implementation
Current Clinical Pharmacology CD147 Promotes Melanoma Progression Through Hypoxia-Induced MMP2 Activation
Current Molecular Medicine Biosimilars Regulation in the United States and FDA Approved Biosimilars from 2015-2018
Applied Clinical Research, Clinical Trials and Regulatory Affairs Design of multifunctional nanocarriers for delivery of anti-cancer therapy
Current Pharmaceutical Design CD147: A Novel Modulator of Inflammatory and Immune Disorders
Current Medicinal Chemistry Etiopathogenesis, Classical Immunotherapy and Innovative Nanotherapeutics for Inflammatory Neurological Disorders
Current Nanoscience The Circulating Endothelial Cell in Cancer: Towards Marker and Target Identification
Current Pharmaceutical Design Caring for HIV-Infected Patients in the ICU in The Highly Active Antiretroviral Therapy Era
Current HIV Research Radionuclide-Labeled Peptides for Imaging and Treatment of CXCR4- Overexpressing Malignant Tumors
Current Topics in Medicinal Chemistry Brain Tumor Segmentation Using Deep Belief Networks and Pathological Knowledge
CNS & Neurological Disorders - Drug Targets TNF-α/Cycloheximide-Induced Oxidative Stress and Apoptosis in Murine Intestinal Epithelial MODE-K Cells
Current Pharmaceutical Design Meet Our Associate Editor:
Current Molecular Medicine The Tumor Suppressor Role of the Ras Association Domain Family 10
Anti-Cancer Agents in Medicinal Chemistry