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
-
Clomiphene for the Treatment of Male Infertility: A Case Report of Mood Change and a Literature Overview
Current Drug Safety Methods to Access 2-aminobenzimidazoles of Medicinal Importance
Current Organic Chemistry Integrin αvβ3 as a Therapeutic Target for Blocking Tumor-Induced Angiogenesis
Current Drug Targets A Survey on Machine Learning Based Medical Assistive Systems in Current Oncological Sciences
Current Medical Imaging Frailty of Older Age: The Role of the Endocrine - Immune Interaction
Current Pharmaceutical Design Identification of the ZAK-MKK4-JNK-TGFβ Signaling Pathway as a Molecular Target for Novel Synthetic Iminoquinone Anticancer Compound BA-TPQ
Current Cancer Drug Targets Thymoquinone: Major Molecular Targets, Prominent Pharmacological Actions and Drug Delivery Concerns
Current Bioactive Compounds From Chemical Graphs in Computer-Aided Drug Design to General Markov-Galvez Indices of Drug-Target, Proteome, Drug-Parasitic Disease, Technological, and Social-Legal Networks
Current Computer-Aided Drug Design Bioinformatics Tools for Mass Spectrometry-Based High-Throughput Quantitative Proteomics Platforms
Current Proteomics Wasp Venom Toxins as a Potential Therapeutic Agent
Protein & Peptide Letters Biofunctional Peptides from Milk Proteins: Mineral Binding and Cytomodulatory Effects
Current Pharmaceutical Design Epigenetic Regulators Governing Cancer Stem Cells and Epithelial- Mesenchymal Transition in Oral Squamous Cell Carcinoma
Current Stem Cell Research & Therapy Combined Chemotherapy or Biotherapy with Jasmonates: Targeting Energy Metabolism for Cancer Treatment
Current Pharmaceutical Biotechnology Recent Advances in Substrate Identification of Protein Kinases in Plants and Their Role in Stress Management
Current Genomics Genito-Urological Cancers in Elderly Patients
Anti-Cancer Agents in Medicinal Chemistry Update on Evidence that Support a Role of Solar Ultraviolet-B Irradiance in Reducing Cancer Risk
Anti-Cancer Agents in Medicinal Chemistry Radiation-Induced Neuroinflammation and Radiation Somnolence Syndrome
CNS & Neurological Disorders - Drug Targets Tissue Biomarkers for Prostate Cancer Radiation Therapy
Current Molecular Medicine Is There a Clinical Future for Spermatogonial Stem Cells?
Current Stem Cell Research & Therapy Next Generation Tyrosine Kinase Inhibitor (TKI): Afatinib
Recent Patents on Anti-Cancer Drug Discovery