Abstract
Glucocorticoids play an essential role in the regulation of multiple physiological processes, including energy metabolism, maintenance of blood pressure and stress responses, as well as cognitive functions. On a tissue-specific level, glucocorticoid action is controlled by 11beta-hydroxysteroid dehydrogenase enzymes. The type 1 enzyme (11beta-HSD1) is a NADP(H)-dependent bidirectional enzyme in vitro and reduces cortisone to active cortisol in vivo. 11beta-HSD1 is expressed in many tissues including the liver, adipose and skeletal muscles. Chronically elevated local glucocorticoid action as a result of increased 11beta-HSD1 activity has been associated with the metabolic syndrome, which is characterized by obesity, insulin resistance, type 2 diabetes and cardiovascular complications. Recent studies indicate that the inhibition of 11beta-HSD1 mitigates the adverse effects of excessive glucocorticoid levels on metabolic parameters and provides promising opportunities for the development of therapeutic interventions. This review discusses recently disclosed 11beta-HSD1 inhibitors and their potential for the treatment of metabolic disorders.
Keywords: 11beta-HSD1, glucocorticoid, metabolic syndrome, diabetes, obesity
Current Medicinal Chemistry
Title: The Role of 11Beta-Hydroxysteroid Dehydrogenase in Metabolic Disease and Therapeutic Potential of 11Beta-HSD1 Inhibitors
Volume: 15 Issue: 7
Author(s): Eddine Saiah
Affiliation:
Keywords: 11beta-HSD1, glucocorticoid, metabolic syndrome, diabetes, obesity
Abstract: Glucocorticoids play an essential role in the regulation of multiple physiological processes, including energy metabolism, maintenance of blood pressure and stress responses, as well as cognitive functions. On a tissue-specific level, glucocorticoid action is controlled by 11beta-hydroxysteroid dehydrogenase enzymes. The type 1 enzyme (11beta-HSD1) is a NADP(H)-dependent bidirectional enzyme in vitro and reduces cortisone to active cortisol in vivo. 11beta-HSD1 is expressed in many tissues including the liver, adipose and skeletal muscles. Chronically elevated local glucocorticoid action as a result of increased 11beta-HSD1 activity has been associated with the metabolic syndrome, which is characterized by obesity, insulin resistance, type 2 diabetes and cardiovascular complications. Recent studies indicate that the inhibition of 11beta-HSD1 mitigates the adverse effects of excessive glucocorticoid levels on metabolic parameters and provides promising opportunities for the development of therapeutic interventions. This review discusses recently disclosed 11beta-HSD1 inhibitors and their potential for the treatment of metabolic disorders.
Export Options
About this article
Cite this article as:
Saiah Eddine, The Role of 11Beta-Hydroxysteroid Dehydrogenase in Metabolic Disease and Therapeutic Potential of 11Beta-HSD1 Inhibitors, Current Medicinal Chemistry 2008; 15 (7) . https://dx.doi.org/10.2174/092986708783885264
DOI https://dx.doi.org/10.2174/092986708783885264 |
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
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...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
- 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
-
Transactivation of ErbB Receptors by Leptin in the Cardiovascular System: Mechanisms, Consequences and Target for Therapy
Current Pharmaceutical Design Acute Effects of Neutrophil-Derived Oxidative Stress on Pulmonary Microvasculature
Current Respiratory Medicine Reviews The Antioxidant Effects of Radix Astragali (Astragalus membranaceus and Related Species) in Protecting Tissues from Injury and Disease
Current Drug Targets Meet Our Editorial Board Member
Current Neuropharmacology Neuroprotection and Sex Steroid Hormones: Evidence of Estradiol- Mediated Protection in Hypertensive Encephalopathy
Mini-Reviews in Medicinal Chemistry Anti-atherosclerotic Effects of Spice-Derived Phytochemicals
Current Medicinal Chemistry Evolution of Copper Transporting ATPases in Eukaryotic Organisms
Current Genomics Advancement in Obesity Management: Leptin and Adiponectin Patents
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery The Role of Antiangiogenetic Agents in the Treatment of Breast Cancer
Current Medicinal Chemistry Monocytes, Macrophages and Other Inflammatory Mediators of Abdominal Aortic Aneurysm
Current Pharmaceutical Design Enhancement of Solubility and Permeability of Candesartan Cilexetil by Using Different Pharmaceutical Interventions
Current Drug Delivery Lack of Association between Genetic Polymorphism of Circadian Genes (PER2, PER3, CLOCK and OX2R) with Late Onset Depression and Alzheimer's Disease in a Sample of a Brazilian Population (Circadian Genes, Late-Onset Depression and Alzheimer's Disease)
Current Alzheimer Research The Role of Obesity in Cardiomyopathy and Nephropathy
Current Pharmaceutical Design Bioactivity and Pharmacological Actions of Carbon Monoxide-Releasing Molecules
Current Pharmaceutical Design Editorial: The Malignant Obesity Hypoventilation Syndrome (MOHS): An Unrecognized Critical Care Syndrome?
Current Respiratory Medicine Reviews Inhibition of the Calcineurin-NFAT Signalling Cascade in the Treatment of Heart Failure
Recent Patents on Cardiovascular Drug Discovery Pyrroles and Fused Pyrroles: Synthesis and Therapeutic Activities
Mini-Reviews in Organic Chemistry Meet Our Editorial Board Member
Current Pharmaceutical Design Associations between Alzheimer’s Disease and Blood Homocysteine, Vitamin B<sub>12</sub>, and Folate: A Case-Control Study
Current Alzheimer Research Contribution of ALDH2 Polymorphism to Alcoholism-Associated Hypertension
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery