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.
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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 |
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