Yeast-based assays for screening 11β-HSD1 inhibitors

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• 作者：Rosario Vanella ; Roberta Callari ; Anna Weston ; Harald Heider…
• 关键词：11β ; HSD1 inhibition ; Metabolic syndrome ; Skin ageing ; Yeast based assay ; TEV protease ; TIPI mechanism ; Pdr5p ABC transporter
• 刊名：Microbial Cell Factories
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：15
• 期：1
• 全文大小：1,948 KB
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Biotechnology
  Applied Microbiology
  Environmental Engineering/Biotechnology
  
• 出版者：BioMed Central
• ISSN：1475-2859

文摘

Background Intracellular metabolism of glucocorticoid hormones plays an important role in the pathogenesis of metabolic syndrome and regulates, among many physiological processes, collagen metabolism in skin. At the peripheral level the concentration of active glucocorticoids is mainly regulated by the 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) enzyme, involved in the conversion of cortisone into the biologically active hormone cortisol. Cortisol interacts with the glucocorticoid receptor and regulates the expression of different classes of genes within the nucleus. Due to its implication in glucocorticoid metabolism, the inhibition of 11β-HSD1 activity has become a dominant strategy for the treatment of metabolic syndrome. Moreover, inhibitors of this target enzyme can be used for development of formulations to counteract skin ageing. Here we present the construction of two yeast cell based assays that can be used for the screening of novel 11β-HSD1 inhibitors.