David J. St. Jean Jr., Minghan Wang and Christopher Fotsch Pages 1508 - 1523 ( 16 )
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.
11β-hydroxysteroid dehydrogenase, glucocorticoid excess, cortisol, Cushing's syndrome, HPA axis, metabolic syndrome
Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Mail Stop 29-1-B, Thousand Oaks, CA 91320-1799.