Abstract
In the last twenty years the efforts to design and optimize new drugs have been based on the three dimensional structure of the selected target proteins. In this regard, useful information has been achieved mainly by protein crystallography, which has recently turned from a low into a high-throughput process thanks to the improvement in robot technologies, automation procedure and the use of synchrotron radiation facilities [1-3]. This review examines the impact of Structure Based Drug Design (SBDD) on the discovery of ligands as the selective estrogen receptor modulators (SERMs) of the Estrogen Receptor (ER)α, which is involved in the regulation of several physiological and pathological processes.
Keywords: Structure based drug design, estrogen, estrogen receptor, lasofoxifene, raloxifene, tamoxifen, SERMs, ADME, DNA, ligand binding domain
Current Medicinal Chemistry
Title: Structure-Based Approach for the Discovery of Novel Selective Estrogen Receptor Modulators
Volume: 18 Issue: 8
Author(s): C. Rosano, E. Stec-Martyna, R. Lappano and M. Maggiolini
Affiliation:
Keywords: Structure based drug design, estrogen, estrogen receptor, lasofoxifene, raloxifene, tamoxifen, SERMs, ADME, DNA, ligand binding domain
Abstract: In the last twenty years the efforts to design and optimize new drugs have been based on the three dimensional structure of the selected target proteins. In this regard, useful information has been achieved mainly by protein crystallography, which has recently turned from a low into a high-throughput process thanks to the improvement in robot technologies, automation procedure and the use of synchrotron radiation facilities [1-3]. This review examines the impact of Structure Based Drug Design (SBDD) on the discovery of ligands as the selective estrogen receptor modulators (SERMs) of the Estrogen Receptor (ER)α, which is involved in the regulation of several physiological and pathological processes.
Export Options
About this article
Cite this article as:
Rosano C., Stec-Martyna E., Lappano R. and Maggiolini M., Structure-Based Approach for the Discovery of Novel Selective Estrogen Receptor Modulators, Current Medicinal Chemistry 2011; 18 (8) . https://dx.doi.org/10.2174/092986711795029645
DOI https://dx.doi.org/10.2174/092986711795029645 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Detection of Predictive Markers for Therapeutic Stratification of Salivary Glands Tumors
Current Drug Targets Emerging Indications for Statins: A Pluripotent Family of Agents with Several Potential Applications
Current Pharmaceutical Design The Emergence of Immune-checkpoint Inhibitors in Colorectal Cancer Therapy
Current Drug Targets Epigenetic Remodeling of Chromatin Architecture: Exploring Tumor Differentiation Therapies in Mesenchymal Stem Cells and Sarcomas
Current Stem Cell Research & Therapy Silencing Human Cancer: Identification and Uses of MicroRNAs
Recent Patents on Anti-Cancer Drug Discovery Induction of Tumour Cell Senescence: A New Strategy in Anticancer Treatment
Medicinal Chemistry Reviews - Online (Discontinued) Bacterial Biotransformation and Anticancer Activities of Betulin against A549, HepG2 and 5RP7 Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Using Pharmacologic Data to Plan Clinical Treatments for Patients with Peritoneal Surface Malignancy
Current Drug Discovery Technologies Computational and Synthetic Biology Approaches for the Biosynthesis of Antiviral and Anticancer Terpenoids from <i>Bacillus subtilis</i>
Medicinal Chemistry Synthesis and In vitro/In vivo Characterization of Raloxifene Grafted Poly(Styrene Maleic Acid)-Poly(Amide-Ether-Ester-Imide) Micelles for Targeted Delivery of Docetaxel in G Protein-Coupled Estrogen Receptor Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry Exogenous Hormonal Regulation in Breast Cancer Cells by Phytoestrogens and Endocrine Disruptors
Current Medicinal Chemistry The Antiprogestogen Mifepristone: A Review
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Decreased lncRNA SNHG16 Accelerates Oxidative Stress Induced Pathological Angiogenesis in Human Retinal Microvascular Endothelial Cells by Regulating miR-195/mfn2 Axis
Current Pharmaceutical Design DNA Methylation, An Epigenetic Mode of Gene Expression Regulation in Reproductive Science
Current Pharmaceutical Design Exogenous Expression of WNT7A in Leukemia-Derived Cell Lines Induces Resistance to Chemotherapeutic Agents
Anti-Cancer Agents in Medicinal Chemistry Perioperative Management of Female Hormone Medications
Current Clinical Pharmacology Role of Androgens in Womens Sexual Function & Dysfunction: What Have We Learned in Six Decades?
Current Women`s Health Reviews Peptides Targeting Estrogen Receptor Alpha-Potential Applications for Breast Cancer Treatment
Current Pharmaceutical Design Ellipticines as DNA-Targeted Chemotherapeutics
Current Medicinal Chemistry Microenvironmental Regulation of Cancer Stem Cell Phenotypes
Current Stem Cell Research & Therapy