11β-Hydroxysteroid dehydrogenase type 1, a target for development of oral antidiabetic drugs (Review)

被引：0
|
作者：
V. V. Lipson
M. G. Shirobokova
O. N. Petrova
机构：
[1] National Academy of Medical Sciences of Ukraine,Danilevsky Institute of Endocrine Pathology Problems
[2] National Academy of Sciences of Ukraine,Institute for Single Crystals
[3] Karazin Kharkiv National University,undefined
来源：
Pharmaceutical Chemistry Journal | 2013年 / 47卷
关键词：
11β-hydroxysteroid dehydrogenase; cortisol; metabolic syndrome; obesity; drug discovery;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
11β-Hydroxysteroid dehydrogenase (11β-HSD1) is an enzyme that catalyses the transformation of the inactive glucocorticoid cortisone into active cortisol. A chronically elevated level of cortisol as a result of 11β-HSD1 hyperexpression in the liver and fatty tissue leads to the development of metabolic syndrome, obesity, insulin-resistance, type 2 diabetes mellitus (DM2), and cardiovascular complications. Inhibition of 11β-HSD1 is recognized as a promising strategy for reducing the activity of glucocorticoids on a tissue-specific level. Herein inhibitors of 11β-HSD1, representatives of several types of N-containing heterocycles at various research stages, are reviewed as potential drugs influencing metabolic syndrome, DM2, and obesity.
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页码：80 / 86
页数：6
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