Abstract
11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is the enzyme that converts cortisone to cortisol. A growing body of evidence suggests that selective inhibition of 11β-HSD1 could potentially treat the metabolic syndrome. This review provides an overview of compounds reported to have in vivo inhibitory activity against this enzyme. A major focus of this review is Amgens 11β-HSD1 program which includes a variety of in vivo data for a lead compound from our thiazolone class of inhibitors. Finally, an update on the current known clinical data is discussed.
Keywords: 11β-hydroxysteroid dehydrogenase, glucocorticoid excess, cortisol, Cushing's syndrome, HPA axis, metabolic syndrome
Current Topics in Medicinal Chemistry
Title: Inhibitors of 11β-HSD1: A Potential Treatment for the Metabolic Syndrome
Volume: 8 Issue: 17
Author(s): David J. St. Jean Jr., Minghan Wang and Christopher Fotsch
Affiliation:
Keywords: 11β-hydroxysteroid dehydrogenase, glucocorticoid excess, cortisol, Cushing's syndrome, HPA axis, metabolic syndrome
Abstract: 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is the enzyme that converts cortisone to cortisol. A growing body of evidence suggests that selective inhibition of 11β-HSD1 could potentially treat the metabolic syndrome. This review provides an overview of compounds reported to have in vivo inhibitory activity against this enzyme. A major focus of this review is Amgens 11β-HSD1 program which includes a variety of in vivo data for a lead compound from our thiazolone class of inhibitors. Finally, an update on the current known clinical data is discussed.
Export Options
About this article
Cite this article as:
Jean Jr. St. David J., Wang Minghan and Fotsch Christopher, Inhibitors of 11β-HSD1: A Potential Treatment for the Metabolic Syndrome, Current Topics in Medicinal Chemistry 2008; 8 (17) . https://dx.doi.org/10.2174/156802608786413528
DOI https://dx.doi.org/10.2174/156802608786413528 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Alpinia calcarata Roscoe: A Rich Source of Phytopharmaceuticals in Sri Lanka
The Natural Products Journal Cardiac and Renal Nitric Oxide in the Adaptation to Hypovolemic Shock
Current Enzyme Inhibition Conference Proceedings: Second International Conference on Novel Psychoactive Substances (NPS) Swansea, UK; September 12-13th, 2013
Current Drug Abuse Reviews Thienopyridines in Percutaneous Coronary Interventions: Standard Procedures and High Risk Subsets
Current Pharmaceutical Design Recent Advances in Antiarrhythmic Drug Treatment of Atrial Fibrillation
Recent Patents on Cardiovascular Drug Discovery Selective Neuronal Nitric Oxide Synthase Inhibitors
Current Topics in Medicinal Chemistry Endothelial Dysfunction in the Hypertensive State: Mechanisms of Hypertensive Cardiovascular Complications
Current Hypertension Reviews Hereditary Haemorrhagic Telangiectasia (HHT): Genetic and Molecular Aspects
Current Pharmaceutical Design Immune Thrombocytopenic Purpura: New Biological Therapy of an Old Disease
Current Medicinal Chemistry MMP Inhibitors in Cardiac Diseases: An Update
Recent Patents on Cardiovascular Drug Discovery Phosphodiesterase 4 Inhibitors in Immune-mediated Diseases: Mode of Action, Clinical Applications, Current and Future Perspectives
Current Medicinal Chemistry Chest Pain in Children
Current Pediatric Reviews On Some Physiological Aspects of Ethanol Repercussion on Neural and Cardiorenal Functions
Central Nervous System Agents in Medicinal Chemistry Inflammation, Atrial Fibrillation and Cardiac Surgery: Current Medical and Invasive Approaches for the Treatment of Atrial Fibrillation
Current Pharmaceutical Design Impact of Nutrition Transition and Resulting Morbidities on Economic and Human Development
Current Diabetes Reviews Adherence to Treatment, Arterial Stiffness and Cognitive Function in Irbesartan- Treated Newly Diagnosed Hypertensive Patients
Current Vascular Pharmacology Hypoglycemic and Hypolipidemic Effects of Aqueous Extracts of Ajuga iva and Centaurium erythreae on a Rodent Model of Metabolic Syndrome
The Natural Products Journal Releasing the Genie in the Bottle: Molecular Signaling with Hydrogen Sulfide
Current Neurovascular Research Angiotensin Converting Enzyme Inhibitor in Coronary Artery Bypass Surgery
Drug Design Reviews - Online (Discontinued) Hypertension in Diabetes: Optimal Pharmacotherapy
Cardiovascular & Hematological Agents in Medicinal Chemistry