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
-
Design, Synthesis and In vitro Cytotoxicity of New 1,2,3-triazol- and Nitrostyrene Hybrids as Potent Anticancer Agents
Letters in Drug Design & Discovery High Frequency of the Opioid Receptor µ-1 (OPRM1) A118G Polymorphism, an Opioid Drug Therapy Related Gene, in the Indonesian Population
Current Pharmacogenomics and Personalized Medicine Molecular and Biochemical Features in Alzheimers Disease
Current Pharmaceutical Design Correlation between Cancer Antigen 15.3 Value and Qualitative and Semiquantitative Parameters of Positron Emission Tomography/Computed Tomography in Breast Cancer Patients
Current Radiopharmaceuticals Novel Monocyte Biomarkers of Atherogenic Conditions
Current Pharmaceutical Design Aberrant Splicing, Hyaluronan Synthases and Intracellular Hyaluronan as Drivers of Oncogenesis and Potential Drug Targets
Current Cancer Drug Targets Radiolabelled Quinoline Derivaties for the PET Imaging of Peripheral Benzodiazepine Receptor
Current Medical Imaging Adipoparacrinology of Atherosclerosis: Evidence Updated
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) An Integrative Informatics Approach to Explain the Mechanism of Action of N1-(Anthraquinon-2-yl) Amidrazones as BCR/ABL Inhibitors
Current Computer-Aided Drug Design Anti-HER2 Cancer Therapy and Cardiotoxicity
Current Pharmaceutical Design The Role of Aryl Hydrocarbon Receptor-Regulated Cytochrome P450 Enzymes in Glioma
Current Pharmaceutical Design Advances in Spirocyclic Hybrids: Chemistry and Medicinal Actions
Current Medicinal Chemistry Therapeutic Potential of Endophytic Compounds: A Special Reference to Drug Transporter Inhibitors
Current Topics in Medicinal Chemistry Rabbit as an Animal Model for Pharmacokinetics Studies of Enteric Capsule Contains Recombinant Human Keratinocyte Growth Factor Loaded Chitosan Nanoparticles
Current Clinical Pharmacology Statins and Ischaemia Reperfusion Injury: A Molecular Biological Review
Current Vascular Pharmacology Potential Molecular Targets of Ampelopsin in Prevention and Treatment of Cancers
Anti-Cancer Agents in Medicinal Chemistry Discovery of Hybrid Purine-quinoline Molecules and Their Cytotoxic Evaluation
Letters in Drug Design & Discovery Dual Role of S100A8 and S100A9 in Inflammation-Associated Cancer
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Surface Modification of Nanocarriers for Cancer Therapy
Current Nanoscience Activation of Intrinsic Apoptosis and G1 Cell Cycle Arrest by a Triazole Precursor, N-(4-chlorophenyl)-2-(4-(3,4,5-trimethoxybenzyloxy)benzoyl)-hydrazinecarbothioamide in Breast Cancer Cell Line
Anti-Cancer Agents in Medicinal Chemistry