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
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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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  • [11] Grossman AB(2003)undefined Mol. Cell. Endocrinol. 201 177-692
  • [12] Tomlinson JW(2000)undefined J. Endocrinol. 165 685-1210
  • [13] Stewart PM(2002)undefined J. Clin. Endocrinol. Metab. 87 1205-133
  • [14] Amelung D(2004)undefined FEBS Lett. 571 129-91
  • [15] Huebner HJ(1996)undefined Lancet 347 88-520
  • [16] Roka L(2007)undefined Drug Discovery Today 12 504-4421
  • [17] Seckl JR(2004)undefined J. Clin. Endocrinol. Metab. 89 4414-1027
  • [18] Walker BR(1999)undefined J. Clin. Endocrinol. Metab. 84 1022-1960
  • [19] Stewart PM(2007)undefined Obesity 15 1954-12636
  • [20] Krozowski ZS(2001)undefined J. Biol. Chem. 276 12629-299