Abstract
The 17β-hydroxysteroid dehydrogenases (17β-HSDs) are involved in the regulation of estrogens and androgens by catalyzing the reduction of 17-ketosteroids or the oxidation of 17β-hydroxysteroids. The enzyme activities associated with the different 17β-HSD isoforms are widespread in human tissues, not only in classic steroidogenic tissues but also in a large series of peripheral intracrine tissues. Being involved at the end of steroidogenesis, the numerous members of 17β-HSD family constitute interesting therapeutic targets for controlling the concentration of estrogens and androgens. Thus, inhibitors of reductive 17β-HSD isoforms are attractive to block the formation of hydroxysteroids that stimulate estrogeno-sensitive pathologies (breast, ovarian, and endometrium cancers) and androgenosensitive pathologies (prostate cancer, benign prostatic hyperplasia, acne, and hirsutism). The inhibitors could be used to block the degradation of estradiol, an attractive strategy for treating osteoporosis and Alzheimers disease. In addition to their classical use as anti-cancer agents and therapeutic agents, inhibitors of 17β-HSDs are also useful tools to elucidate the role of these enzymes in particular biological systems. The present review article gives a description of novel inhibitors of 17β-HSDs that were published in 2003-2006.
Keywords: Hydroxysteroid dehydrogenase, 17β-HSD, enzyme, inhibitor, steroid, estrogen, androgen, cancer
Anti-Cancer Agents in Medicinal Chemistry
Title: Advances in Development of Inhibitors of 17β-Hydroxysteroid Dehydrogenases
Volume: 9 Issue: 6
Author(s): Donald Poirier
Affiliation:
Keywords: Hydroxysteroid dehydrogenase, 17β-HSD, enzyme, inhibitor, steroid, estrogen, androgen, cancer
Abstract: The 17β-hydroxysteroid dehydrogenases (17β-HSDs) are involved in the regulation of estrogens and androgens by catalyzing the reduction of 17-ketosteroids or the oxidation of 17β-hydroxysteroids. The enzyme activities associated with the different 17β-HSD isoforms are widespread in human tissues, not only in classic steroidogenic tissues but also in a large series of peripheral intracrine tissues. Being involved at the end of steroidogenesis, the numerous members of 17β-HSD family constitute interesting therapeutic targets for controlling the concentration of estrogens and androgens. Thus, inhibitors of reductive 17β-HSD isoforms are attractive to block the formation of hydroxysteroids that stimulate estrogeno-sensitive pathologies (breast, ovarian, and endometrium cancers) and androgenosensitive pathologies (prostate cancer, benign prostatic hyperplasia, acne, and hirsutism). The inhibitors could be used to block the degradation of estradiol, an attractive strategy for treating osteoporosis and Alzheimers disease. In addition to their classical use as anti-cancer agents and therapeutic agents, inhibitors of 17β-HSDs are also useful tools to elucidate the role of these enzymes in particular biological systems. The present review article gives a description of novel inhibitors of 17β-HSDs that were published in 2003-2006.
Export Options
About this article
Cite this article as:
Poirier Donald, Advances in Development of Inhibitors of 17β-Hydroxysteroid Dehydrogenases, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (6) . https://dx.doi.org/10.2174/187152009788680000
DOI https://dx.doi.org/10.2174/187152009788680000 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Genetics of the First Seven Proprotein Convertase Enzymes in Health and Disease
Current Genomics High Mobility Group Box 1 Protein as a Potential Drug Target for Infection- and Injury-Elicited Inflammation
Inflammation & Allergy - Drug Targets (Discontinued) Understanding Tumor-Antigen Presentation in the New Era of Cancer Immunotherapy
Current Pharmaceutical Design Inhibition of Histone Deacetylases: A Pharmacological Approach to the Treatment of Non-Cancer Disorders
Current Topics in Medicinal Chemistry Novel Nanotechnology Approaches for Targeted Cancer Therapy
Recent Patents on Nanomedicine Target Acquired: Progress and Promise of Targeted Therapeutics in the Treatment of Prostate Cancer
Current Cancer Drug Targets Trends in Utilization of the Pharmacological Potential of Chalcones
Current Clinical Pharmacology The Role of Tumor Suppressor Dysregulation in Prostate Cancer Progression
Current Drug Targets In Vivo Pharmacokinetic and Tissue Distribution Studies in Mice of Alternative Formulations for Local and Systemic Delivery of Paclitaxel: Gel, Film, Prodrug, Liposomes and Micelles
Current Drug Delivery Planning of External Beam Radiotherapy for Prostate Cancer Guided by PET/CT
Current Radiopharmaceuticals An Overview of Bioactive Peptides for in vivo Imaging and Therapy in Human Diseases
Mini-Reviews in Medicinal Chemistry The Use of Cytokines and Chemokines in the Cancer Immunotherapy
Recent Patents on Anti-Cancer Drug Discovery Artificial Intelligence, Big Data and Machine Learning Approaches in Precision Medicine & Drug Discovery
Current Drug Targets Mechanisms of Tubulin Binding Ligands to Target Cancer Cells: Updates on their Therapeutic Potential and Clinical Trials
Current Cancer Drug Targets Synthesis and Biological Evaluation of Macamides Derivatives as Potent Inhibitors of Breast Cancer Cell MCF-7
Letters in Drug Design & Discovery Plastid Molecular Pharming II. Production of Biopharmaceuticals by Plastid Transformation
Mini-Reviews in Medicinal Chemistry Fetal Mesenchymal Stem Cells in Cancer Therapy
Current Stem Cell Research & Therapy Iron Chelators: Development of Novel Compounds with High and Selective Anti-Tumour Activity
Current Drug Delivery Anticancer Drug Discovery from the Marine Environment
Recent Patents on Anti-Cancer Drug Discovery Estrogen Receptors: Mechanism of Action and Relevance to Schizophrenia
Current Psychiatry Reviews