Inhibitors of 11β-HSD1: A Potential Treatment for the Metabolic Syndrome

Author(s): David J. St. Jean Jr., Minghan Wang, Christopher Fotsch

Journal Name: Current Topics in Medicinal Chemistry

Volume 8 , Issue 17 , 2008

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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

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Article Details

Year: 2008
Page: [1508 - 1523]
Pages: 16
DOI: 10.2174/156802608786413528
Price: $65

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