The protein encoded by this gene is a microsomal enzyme that catalyzes the conversion of the stress hormone cortisol to the inactive metabolitecortisone. In addition, the encoded protein can catalyze the reverse reaction, the conversion of cortisone to cortisol. Too much cortisol can lead to central obesity, and a particular variation in this gene has been associated with obesity and insulin resistance in children. Two transcript variants encoding the same protein have been found for this gene.[5]
Clinical significance[]
11β-HSD1 is inhibited by carbenoxolone, a drug typically used in the treatment of peptic ulcers. Moreover, 18alpha-glycyrrhizic acid from the root of glycyrrhiza glabra was discovered as an inhibitor.[6]
Salicylate downregulates 11β-HSD1 expression in adipose tissue in obese mice and hence may explain why aspirin improves glycemic control in type 2 diabetes.[7]Epigallocatechin gallate from green tea can also potently inhibit this enzyme;[8] green tea is a complex mixture of various phenolics with contents varying with production and processing, and some of the phenolics are known HDAC inhibitors that alter genetic expression. EGCG as usually consumed in green tea is poorly absorbed into the bloodstream. More research is needed to reach firm conclusions.[citation needed]
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White PC, Mune T, Agarwal AK (February 1997). "11 beta-Hydroxysteroid dehydrogenase and the syndrome of apparent mineralocorticoid excess". Endocrine Reviews. 18 (1): 135–56. doi:10.1210/er.18.1.135. PMID9034789.
Agarwal AK (November 2003). "Cortisol metabolism and visceral obesity: role of 11beta-hydroxysteroid dehydrogenase type I enzyme and reduced co-factor NADPH". Endocrine Research. 29 (4): 411–8. doi:10.1081/ERC-120026947. PMID14682470. S2CID32163545.
Whorwood CB, Mason JI, Ricketts ML, Howie AJ, Stewart PM (April 1995). "Detection of human 11 beta-hydroxysteroid dehydrogenase isoforms using reverse-transcriptase-polymerase chain reaction and localization of the type 2 isoform to renal collecting ducts". Molecular and Cellular Endocrinology. 110 (1–2): R7–12. doi:10.1016/0303-7207(95)03546-J. PMID7545619. S2CID25070635.
Mune T, Rogerson FM, Nikkilä H, Agarwal AK, White PC (August 1995). "Human hypertension caused by mutations in the kidney isozyme of 11 beta-hydroxysteroid dehydrogenase". Nature Genetics. 10 (4): 394–9. doi:10.1038/ng0895-394. PMID7670488. S2CID30848352.
Ricketts ML, Verhaeg JM, Bujalska I, Howie AJ, Rainey WE, Stewart PM (April 1998). "Immunohistochemical localization of type 1 11beta-hydroxysteroid dehydrogenase in human tissues". The Journal of Clinical Endocrinology and Metabolism. 83 (4): 1325–35. doi:10.1210/jc.83.4.1325. PMID9543163.
Cooper MS, Walker EA, Bland R, Fraser WD, Hewison M, Stewart PM (September 2000). "Expression and functional consequences of 11beta-hydroxysteroid dehydrogenase activity in human bone". Bone. 27 (3): 375–81. doi:10.1016/S8756-3282(00)00344-6. PMID10962348.