Inhibitors of 11β-HSD1: A Potential Treatment for the Metabolic Syndrome
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 Amgen's 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; Cushing's syndrome; HPA axis; cortisol; glucocorticoid excess; metabolic syndrome
Document Type: Research Article
Affiliations: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Mail Stop 29-1-B, Thousand Oaks, CA 91320-1799.
Publication date: 01 November 2008
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