Abstract
Aromatase inhibitors are class of drugs that inhibit aromatase, a rate limiting enzyme in the biosynthesis of estrogens from their corresponding androgens. Estrogens play a vital role in the development and growth of breast tumors especially in postmenopausal women apart from their important functions in cell homeostasis. The reduction of estrogen physiological concentration through aromatase inhibition is one of the most important therapeutic strategies against this cancer type. The third-generation aromatase inhibitors are now used as first-line therapy in the treatment of early and metastatic breast cancer in postmenopausal women. However the quest for new class of drugs still stays indispensable to evade the danger of conceivable rising resistances to existing drugs, toxicity and unwanted side effects due to chronic treatment. The current review deals with recent advances in understanding of aromatase, its mechanism and research in the development of various novel chemotypes as aromatase inhibitors. The new challenges and the fast changing trends in bringing rational approach in aromatase inhibitors to a different level like research in dual/multiple target enzyme inhibition strategies, radiolabeling of aromatase inhibitors as theranostic agents; the development of new computational models for complete understanding of aromatase enzyme and its substrate/ligand interactions will bring in holistic approach to comprehensive inhibition of aromatase and other relevant enzymes for effective treatment and monitoring of postmenopausal breast cancer.
Keywords: Aromatase inhibitors, estrogen, breast cancer, dual inhibitors, molecular modeling, radiolabeling.
Mini-Reviews in Medicinal Chemistry
Title:Aromatase Inhibitors Evolution as Potential Class of Drugs in the Treatment of Postmenopausal Breast Cancer Women
Volume: 18 Issue: 7
Author(s): Stephen Paul Avvaru, Malleshappa N. Noolvi*, Tejraj M. Aminbhavi, Sudipta Chkraborty, Ashutosh Dash and Shyam S. Shukla
Affiliation:
- Department of Pharmaceutical Chemistry, Shree Dhanvantary Pharmacy College, Kim, Surat, 394110,India
Keywords: Aromatase inhibitors, estrogen, breast cancer, dual inhibitors, molecular modeling, radiolabeling.
Abstract: Aromatase inhibitors are class of drugs that inhibit aromatase, a rate limiting enzyme in the biosynthesis of estrogens from their corresponding androgens. Estrogens play a vital role in the development and growth of breast tumors especially in postmenopausal women apart from their important functions in cell homeostasis. The reduction of estrogen physiological concentration through aromatase inhibition is one of the most important therapeutic strategies against this cancer type. The third-generation aromatase inhibitors are now used as first-line therapy in the treatment of early and metastatic breast cancer in postmenopausal women. However the quest for new class of drugs still stays indispensable to evade the danger of conceivable rising resistances to existing drugs, toxicity and unwanted side effects due to chronic treatment. The current review deals with recent advances in understanding of aromatase, its mechanism and research in the development of various novel chemotypes as aromatase inhibitors. The new challenges and the fast changing trends in bringing rational approach in aromatase inhibitors to a different level like research in dual/multiple target enzyme inhibition strategies, radiolabeling of aromatase inhibitors as theranostic agents; the development of new computational models for complete understanding of aromatase enzyme and its substrate/ligand interactions will bring in holistic approach to comprehensive inhibition of aromatase and other relevant enzymes for effective treatment and monitoring of postmenopausal breast cancer.
Export Options
About this article
Cite this article as:
Avvaru Paul Stephen , Noolvi N. Malleshappa*, Aminbhavi M. Tejraj , Chkraborty Sudipta , Dash Ashutosh and Shukla S. Shyam , Aromatase Inhibitors Evolution as Potential Class of Drugs in the Treatment of Postmenopausal Breast Cancer Women, Mini-Reviews in Medicinal Chemistry 2018; 18 (7) . https://dx.doi.org/10.2174/1389557517666171101100902
DOI https://dx.doi.org/10.2174/1389557517666171101100902 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Probiotics in Curing Allergic and Inflammatory Conditions - Research Progress and Futuristic Vision
Recent Patents on Inflammation & Allergy Drug Discovery Fibroblast Growth Factors/Fibroblast Growth Factor Receptors as Targets for the Development of Anti-Angiogenesis Strategies
Current Pharmaceutical Design Recent Advances of Natural and Synthetic β-Carbolines as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Eliminating Ovarian Cancer Stem Cells: A Potential Therapeutic Target for Ovarian Cancer Chemoresistance
Current Protein & Peptide Science Applications of X-Ray Diffraction Imaging to Mammography
Recent Patents on Medical Imaging ENaC in the Brain - Future Perspectives and Pharmacological Implications
Current Molecular Pharmacology Foreword
Current Pharmaceutical Design Anti-inflammatory and Antitumor Properties of Eriobotrya Japonica Lindl: Mini-Review
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Post-translational and Post-transcriptional Modifications of Pregnane X Receptor (PXR) in Regulation of the Cytochrome P450 Superfamily
Current Drug Metabolism Multidrug-Resistance (MDR) Proteins Develops Refractory Epilepsy Phenotype:Clinical and Experimental Evidences
Current Drug Therapy Smart Triggered Release in Controlled Drug Delivery
Current Drug Targets Systems Biology: A Powerful Tool for Drug Development
Current Topics in Medicinal Chemistry Multifunctional Anti-Cancer Nano-Platforms are Moving to Clinical Trials
Current Drug Metabolism New Insight in LPS Antagonist
Mini-Reviews in Medicinal Chemistry Small Heat Shock Proteins and the Endoplasmic Reticulum: Potential Attractive Therapeutic Targets?
Current Molecular Medicine The Clinical Prognostic Value of LRG1 in Esophageal Squamous Cell Carcinoma
Current Cancer Drug Targets Combined Cancer Therapy with Non-Conventional Drugs: All Roads Lead to AMPK
Mini-Reviews in Medicinal Chemistry Synthesis and Anticancer Activity of 2,4,5-triaryl Imidazole Derivatives
Letters in Drug Design & Discovery Therapeutic Targeting of Endothelial Dysfunction in Chronic Diabetic Complications
Recent Patents on Cardiovascular Drug Discovery An Antileukemic Glutaminase Free L-Asparaginase from Bacillus brevis
Current Biotechnology