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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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

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

Volume 8, Issue 17, 2008

Page: [1508 - 1523] Pages: 16

DOI: 10.2174/156802608786413528

Price: $65

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


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