Cell‐based assay for screening 11β‐hydroxysteroid dehydrogenase inhibitors using liquid chromatography/tandem mass spectrometry detection

Abstract Cortisol is an important glucocorticoid that regulates many physiological pathways by activating various intracellular receptors. The type 1 isozyme of 11 β ‐hydroxysteroid dehydrogenase (11 β ‐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 11 β ‐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 11 β ‐HSD inhibitors. The reductase and dehydrogenase activities of 11 β ‐HSD1 are assessed separately. Copyright © 2006 John Wiley & Sons, Ltd.