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

Xu Rongda | Zendy; Sang BiChing | Zendy; Navre Marc | Zendy; Kassel Daniel B. | Zendy

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

Author(s) -

Xu Rongda,

Sang BiChing,

Navre Marc,

Kassel Daniel B.

Publication year - 2006

Publication title -

rapid communications in mass spectrometry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.528

H-Index - 136

eISSN - 1097-0231

pISSN - 0951-4198

DOI - 10.1002/rcm.2484

Subject(s) - chemistry , cortisone , 11β hydroxysteroid dehydrogenase type 1 , dehydrogenase , chromatography , tandem mass spectrometry , mass spectrometry , in vivo , enzyme , steroid , liquid chromatography–mass spectrometry , reductase , biochemistry , endocrinology , hormone , medicine , microbiology and biotechnology , biology

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.

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