11β-hydroxysteroid dehydrogenase 1 human tissue distribution, selective inhibitor, and role in doxorubicin metabolism

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Abstract

11β-Hydroxysteroid dehydrogenase 1 (11β-HSD1) is distributed mainly in the human liver, with no detectable levels in the intestine or kidney, based on a newly developed proteomic approach. 11β-HSD1 is mostly membrane-bound and retained in the liver microsomal fraction. Interindividual variability of 11β-HSD1 is relatively low, with about a 3-fold difference. A significant correlation was not observed between various demographic variables (ethnicity, gender, age, weight, smoking, and alcohol use) and 11β-HSD1 protein expression or activity based on data from 31 donors. PF-915275 has been identified as a selective 11β-HSD1 inhibitor with minimal effects on carbonyl reductase 1 and major cytochrome P450 enzymes. 11β-HSD1 has been shown, for the first time, to be involved in doxorubicin metabolism, accounting for approximately 30% of doxorubicinol formation in human hepatocytes.

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Yang, X., Hua, W., Ryu, S., Yates, P., Chang, C., Zhang, H., & Di, L. (2018). 11β-hydroxysteroid dehydrogenase 1 human tissue distribution, selective inhibitor, and role in doxorubicin metabolism. Drug Metabolism and Disposition, 46(7), 1023–1029. https://doi.org/10.1124/dmd.118.081083

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