Xu Rongda, Sang Bi-Ching, Navre Marc, Kassel Daniel B
Takeda San Diego, Inc., 10410 Science Center Dr., San Diego, CA 92121, USA.
Rapid Commun Mass Spectrom. 2006;20(11):1643-7. doi: 10.1002/rcm.2484.
Cortisol is an important glucocorticoid that regulates many physiological pathways by activating various intracellular receptors. The type 1 isozyme of 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) functions in vivo predominantly as a reductase by converting cortisone into cortisol. A high-throughput liquid chromatography/tandem mass spectrometry (LC/MS/MS) method has been developed to screen for inhibitors of 11beta-HSD1 by monitoring cortisol and cortisone simultaneously. The injection cycle time can be as fast as 1 min/sample, making it amenable to the analysis of large numbers of the cell-assay samples in the screening of 11beta-HSD inhibitors. The reductase and dehydrogenase activities of 11beta-HSD1 are assessed separately.
皮质醇是一种重要的糖皮质激素，通过激活各种细胞内受体来调节多种生理途径。11β-羟基类固醇脱氢酶1型同工酶（11β-HSD1）在体内主要作为还原酶发挥作用，将可的松转化为皮质醇。已开发出一种高通量液相色谱/串联质谱（LC/MS/MS）方法，通过同时监测皮质醇和可的松来筛选11β-HSD1抑制剂。进样循环时间可快至1分钟/样品，适用于在筛选11β-HSD抑制剂时分析大量细胞测定样品。11β-HSD1的还原酶和脱氢酶活性分别进行评估。
