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

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2008年 / 8卷 / 17期

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

页码：1508 / 1523

页数：16

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