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 |
- 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
-
Cardiovascular Effects of Flavonoids
Current Medicinal Chemistry Postpartum Haemorrhage, A Persisting Killer Around the Globe, Road Ahead
Current Women`s Health Reviews Effect of a Dihydropyridine-Type Calcium Channel Blocker on Vascular Remodelling after Experimental Balloon Angioplasty
Cardiovascular & Hematological Agents in Medicinal Chemistry Pharmacologic Therapy for Cardiovascular Risk Reduction in Patients with the Metabolic Syndrome
Current Pharmaceutical Design Efficacy and Safety of the Combination of Docetaxel (Taxotere®) with Targeted Therapies in the Treatment of Solid Malignancies
Current Drug Targets Phenotypes of Obstructive Sleep Apnea and Direct Targeted Therapy: A Literature Review
Current Respiratory Medicine Reviews Combining Diffusion-Weighted Imaging Patterns with ABCD2 Score Predicts Stroke Risk after Transient Ischemic Attack
Current Neurovascular Research Is It Possible to Apply Secondary Stroke Prevention Guidelines to Very Old Populations?
Cardiovascular & Hematological Disorders-Drug Targets Patent Selections
Recent Patents on Biomarkers Extensive Coronary Calcification: A Clinically Unrecognised Condition
Current Vascular Pharmacology Curcumin Nanomicelle Improves Lipid Profile, Stress Oxidative Factors and Inflammatory Markers in Patients Undergoing Coronary Elective Angioplasty; A Randomized Clinical Trial
Endocrine, Metabolic & Immune Disorders - Drug Targets Clinical Experience with Specific COX-2 Inhibitors in Arthritis
Current Pharmaceutical Design Diuretics: From Classical Carbonic Anhydrase Inhibitors to Novel Applications of the Sulfonamides
Current Pharmaceutical Design Expression, Purification, and Characterization of an Enzymatically Active Truncated Human Rho-Kinase I (ROCK I) Domain Expressed in Sf-9 Insect Cells
Protein & Peptide Letters Preface: Facing New Challenges in Cardiovascular Disease, When the Pressure Goes Up and the Pump Goes Astray
Recent Advances in Cardiovascular Drug Discovery (Discontinued) Classic β-Amyloid Deposits Cluster Around Large Diameter Blood Vessels Rather than Capillaries in Sporadic Alzheimers Disease
Current Neurovascular Research Childhood Hypertension and Effects on Cognitive Functions: Mechanisms and Future Perspectives
CNS & Neurological Disorders - Drug Targets Cell-free DNA: Characteristics, Detection and its Applications in Myocardial Infarction
Current Pharmaceutical Design High Serum Alkaline Phosphatase Levels in Relation to Multi-Cerebral Microbleeds in Acute Ischemic Stroke Patients with Atrial Fibrillation and/or Rheumatic Heart Disease
Current Neurovascular Research Depression and its Relation with Uncontrolled Hypertension and Increased Cardiovascular Risk
Current Hypertension Reviews