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
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...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
- 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
-
New Immunosuppressants: Immunosuppression and Immunomodulation
Medicinal Chemistry Reviews - Online (Discontinued) Anti-Cancer Effect of Gingerol in Cancer Prevention and Treatment
Anti-Cancer Agents in Medicinal Chemistry Transglutaminase-Mediated Activation of Nuclear Transcription Factor-κB in Cancer Cells: A New Therapeutic Opportunity
Current Cancer Drug Targets Receptor Tyrosine Kinases Take a Direct Route to Mitochondria: An Overview
Current Protein & Peptide Science Meet Our Editorial Board Member:
Current Cancer Drug Targets Anticancer Drugs Discovery and Development from Marine Organisms
Current Topics in Medicinal Chemistry Omega-3 Fatty Acids for Nutrition and Medicine: Considering Microalgae Oil as a Vegetarian Source of EPA and DHA
Current Diabetes Reviews 13-lncRNAs Signature to Improve Diagnostic and Prognostic Prediction of Hepatocellular Carcinoma
Combinatorial Chemistry & High Throughput Screening Current Status and Future of Target-Based Therapeutics
Current Cancer Drug Targets Surgical Staging for Cervical Cancer
Current Women`s Health Reviews STAT Inhibition in the Treatment of Cancer: Transcription Factors as Targets for Molecular Therapy
Current Cancer Therapy Reviews New Benzothiazole/thiazole-Containing Hydroxamic Acids as Potent Histone Deacetylase Inhibitors and Antitumor Agents
Medicinal Chemistry Synthetic and Medicinal Perspective of Fused-Thiazoles as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Separation of Ginseng Active Ingredients and their Roles in Cancer Metastasis Supplementary Therapy
Current Drug Metabolism Mitochondria Damage in the Pathogenesis of Diabetic Retinopathy and in the Metabolic Memory Associated with its Continued Progression
Current Medicinal Chemistry Novel Drugs Targeting Microtubules: the Role of Epothilones
Current Pharmaceutical Design Microenvironment and Brain Tumor Stem Cell Maintenance: Impact of the Niche
Anti-Cancer Agents in Medicinal Chemistry Anthocyanins As Modulators of Cell Redox-Dependent Pathways in Non-Communicable Diseases
Current Medicinal Chemistry Mechanisms of Drug-Induced Mitotic Catastrophe in Cancer Cells
Current Pharmaceutical Design Experimental Validation of an Assembly of Optimized Curved Rectangular Coils for the Use in Dynamic Field Free Line Magnetic Particle Imaging
Current Medical Imaging