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

被引:19
|
作者
Jean, David J. St., Jr. [1 ]
Wang, Minghan [1 ]
Fotsch, Christopher [1 ]
机构
[1] Amgen Inc, Dept Med Chem, Thousand Oaks, CA 91320 USA
关键词
11 beta-hydroxysteroid dehydrogenase; glucocorticoid excess; cortisol; Cushing's syndrome; HPA axis; metabolic syndrome;
D O I
10.2174/156802608786413528
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) is the enzyme that converts cortisone to cortisol. A growing body of evidence suggests that selective inhibition of 11 beta-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 11 beta-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.
引用
收藏
页码:1508 / 1523
页数:16
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