Best Practice & Research Clinical Endocrinology & Metabolism
Volume 21, Issue 4 , Pages 607-619 , December 2007

Modulation of glucocorticoid action and the treatment of type-2 diabetes

References 

  1. Fraser R, Ingram MC, Anderson NH, et al. Cortisol effects on body mass, blood pressure, and cholesterol in the general population. Hypertension. 1999;33(6):1364–1368
  2. Giguere V, Hollenberg SM, Rosenfeld MG, et al. Functional domains of the human glucocorticoid receptor. Cell. 1986;46(5):645–652
  3. Hollenberg SM, Weinberger C, Ong ES, et al. Primary structure and expression of a functional human glucocorticoid receptor cDNA. Nature. 1985;318:635–641
  4. Oakley RH, Sar M, Cidlowski JA. The human glucocorticoid receptor beta isoform. Expression, biochemical properties, and putative function. The Journal of Biological Chemistry. 1996;271(16):9550–9559
  5. Beato M, Truss M, Chavez S. Control of transcription by steroid hormones. Annals of the New York Academy of Sciences. 1996;784:93–123
  6. Beato M, Chalepakis G, Schauer M, et al. DNA regulatory elements for steroid hormones. Journal of Steroid Biochemistry. 1989;32(5):737–747
  7. Charron J, Drouin J. Glucocorticoid inhibition of transcription from episomal proopiomelanocortin gene promoter. Proceedings of the National Academy of Sciences of the United States of America. 1986;83(23):8903–8907
  8. Kullmann M, Schneikert J, Moll J, et al. RAP46 is a negative regulator of glucocorticoid receptor action and hormone-induced apoptosis. The Journal of Biological Chemistry. 1998;273(23):14620–14625
  9. White PC, Mune T, Agarwal AK. 11 beta-Hydroxysteroid dehydrogenase and the syndrome of apparent mineralocorticoid excess. Endocrine Reviews. 1997;18(1):135–156
  10. Tomlinson JW, Walker EA, Bujalska IJ, et al. 11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response. Endocrine Reviews. 2004;25(5):831–866
  11. Agarwal AK, Tusie-Luna MT, Monder C, et al. Expression of 11b-hydroxysteroid dehydrogenase using recombinant vaccinia virus. Molecular Endocrinology. 1990;4:1827–1832
  12. Lavery GG, Walker EA, Draper N, et al. Hexose-6-phosphate dehydrogenase knockout mice lack 11beta -hydroxysteroid dehydrogenase type 1-mediated glucocorticoid generation. The Journal of Biological Chemistry. 2006;281:6546–6551
  13. Bujalska IJ, Draper N, Michailidou Z, et al. Hexose-6-phosphate dehydrogenase confers oxo-reductase activity upon 11 beta-hydroxysteroid dehydrogenase type 1. Journal of Molecular Endocrinology. 2005;34(3):675–684
  14. Kotelevtsev Y, Holmes MC, Burchell A, et al. 11beta-hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist hyperglycemia on obesity or stress. Proceedings of the National Academy of Sciences of the United States of America. 1997;94(26):14924–14929
  15. Masuzaki H, Yamamoto H, Kenyon CJ, et al. Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice. The Journal of Clinical Investigation. 2003;112(1):83–90
  16. Masuzaki H, Paterson J, Shinyama H, et al. A transgenic model of visceral obesity and the metabolic syndrome. Science. 2001;294(5549):2166–2170
  17. Kershaw EE, Morton NM, Dhillon H, et al. Adipocyte-specific glucocorticoid inactivation protects against diet-induced obesity. Diabetes. 2005;54(4):1023–1031
  18. Paterson JM, Morton NM, Fievet C, et al. Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice. Proceedings of the National Academy of Sciences of the United States of America. 2004;101(18):7088–7093
  19. Livingstone DE, Jones GC, Smith K, et al. Understanding the role of glucocorticoids in obesity: tissue-specific alterations of corticosterone metabolism in obese Zucker rats. Endocrinology. 2000;141(2):560–563
  20. Morton NM, Ramage L, Seckl JR. Down-regulation of adipose 11beta-hydroxysteroid dehydrogenase type 1 by high-fat feeding in mice: a potential adaptive mechanism counteracting metabolic disease. Endocrinology. 2004;145(6):2707–2712
  21. Kerstens MN, Riemens SC, Sluiter WJ, et al. Lack of relationship between 11beta-hydroxysteroid dehydrogenase setpoint and insulin sensitivity in the basal state and after 24h of insulin infusion in healthy subjects and type 2 diabetic patients. Clinical Endocrinology. 2000;52(4):403–411
  22. Valsamakis G, Anwar A, Tomlinson JW, et al. 11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus. The Journal of Clinical Endocrinology and Metabolism. 2004;89(9):4755–4761
  23. Sandeep TC, Andrew R, Homer NZ, et al. Increased in vivo regeneration of cortisol in adipose tissue in human obesity and effects of the 11beta-hydroxysteroid dehydrogenase type 1 inhibitor carbenoxolone. Diabetes. 2005;54(3):872–879
  24. Tomlinson JW, Sinha B, Bujalska I, et al. Expression of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue is not increased in human obesity. The Journal of Clinical Endocrinology and Metabolism. 2002;87(12):5630–5635
  25. Rask E, Olsson T, Soderberg S, et al. Tissue-specific dysregulation of cortisol metabolism in human obesity. The Journal of Clinical Endocrinology and Metabolism. 2001;86(3):1418–1421
  26. Rask E, Walker BR, Soderberg S, et al. Tissue-specific changes in peripheral cortisol metabolism in obese women: increased adipose 11beta-hydroxysteroid dehydrogenase type 1 activity. The Journal of Clinical Endocrinology and Metabolism. 2002;87(7):3330–3336
  27. Wake DJ, Rask E, Livingstone DE, et al. Local and systemic impact of transcriptional up-regulation of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue in human obesity. The Journal of Clinical Endocrinology and Metabolism. 2003;88(8):3983–3988
  28. Paulmyer-Lacroix O, Boullu S, Oliver C, et al. Expression of the mRNA Coding for 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue from obese patients: an in situ hybridization study. The Journal of Clinical Endocrinology and Metabolism. 2002;87(6):2701–2705
  29. Westerbacka J, Yki-Jarvinen H, Vehkavaara S, et al. Body fat distribution and cortisol metabolism in healthy men: enhanced 5beta-reductase and lower cortisol/cortisone metabolite ratios in men with fatty liver. The Journal of Clinical Endocrinology and Metabolism. 2003;88(10):4924–4931
  30. Lindsay RS, Wake DJ, Nair S, et al. Subcutaneous adipose 11beta-hydroxysteroid dehydrogenase type 1 activity and messenger ribonucleic Acid levels are associated with adiposity and insulinemia in Pima Indians and Caucasians. The Journal of Clinical Endocrinology and Metabolism. 2003;88(6):2738–2744
  31. Kannisto K, Pietilainen KH, Ehrenborg E, et al. Overexpression of 11beta-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of insulin resistance: studies in young adult monozygotic twins. The Journal of Clinical Endocrinology and Metabolism. 2004;89(9):4414–4421
  32. Drake AJ, Livingstone DE, Andrew R, et al. Reduced adipose glucocorticoid reactivation and increased hepatic glucocorticoid clearance as an early adaptation to high-fat feeding in Wistar rats. Endocrinology. 2005;146(2):913–919
  33. Bujalska IJ, Kumar S, Stewart PM. Does central obesity reflect ‘Cushing's disease of the omentum'?. Lancet. 1997;349(August 26):1210–1213
  34. Andrew R, Smith K, Jones GC, et al. Distinguishing the activities of 11beta-hydroxysteroid dehydrogenases in vivo using isotopically labeled cortisol. The Journal of Clinical Endocrinology and Metabolism. 2002;87(1):277–285
  35. Basu R, Singh RJ, Basu A, et al. Splanchnic cortisol production occurs in humans: evidence for conversion of cortisone to cortisol via the 11-beta hydroxysteroid dehydrogenase (11beta-hsd) type 1 pathway. Diabetes. 2004;53(8):2051–2059
  36. Andrew R, Westerbacka J, Wahren J, et al. The contribution of visceral adipose tissue to splanchnic cortisol production in healthy humans. Diabetes. 2005;54(5):1364–1370
  37. Basu R, Singh RJ, Basu A, et al. Obesity and type 2 diabetes do not alter splanchnic cortisol production in humans. The Journal of Clinical Endocrinology and Metabolism. 2005;90(7):3919–3926
  38. Maser E, Bannenberg G. 11 beta-hydroxysteroid dehydrogenase mediates reductive metabolism of xenobiotic carbonyl compounds. Biochemical Pharmacology. 1994;47(10):1805–1812
  39. Szotakova B, Skalova L, Wsol V, et al. Reduction of the potential anticancer drug oracin in the rat liver in-vitro. The Journal of Pharmacy and Pharmacology. 2000;52(5):495–500
  40. Hult M, Nobel CS, Abrahmsen L, et al. Novel enzymological profiles of human 11beta-hydroxysteroid dehydrogenase type 1. Chemico-Biological Interactions. 2001;130–132(1–3):805–814
  41. Oppermann UC, Maser E. Molecular and structural aspects of xenobiotic carbonyl metabolizing enzymes. Role of reductases and dehydrogenases in xenobiotic phase I reactions. Toxicology. 2000;144(1–3):71–81
  42. Bannenberg G, Martin HJ, Belai I, et al. 11beta-Hydroxysteroid dehydrogenase type 1: tissue-specific expression and reductive metabolism of some anti-insect agent azole analogues of metyrapone. Chemico-Biological Interactions. 2003;143-144:449–457
  43. Maser E. 11Beta-hydroxysteroid dehydrogenase responsible for carbonyl reduction of the tobacco-specific nitrosamine 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone in mouse lung microsomes. Cancer Research. 1998;58(14):2996–3003
  44. Finckh C, Atalla A, Nagel G, et al. Expression and NNK reducing activities of carbonyl reductase and 11beta-hydroxysteroid dehydrogenase type 1 in human lung. Chemico-Biological Interactions. 2001;130–132(1–3):761–773
  45. Monder C, White PC. 11b-Hydroxysteroid dehydrogenase. Vitamins and Hormones. 1993;47:187–271
  46. Walker BR, Connacher AA, Lindsay RM, et al. Carbenoxolone increases hepatic insulin sensitivity in man: a novel role for 11-oxosteroid reductase in enhancing glucocorticoid receptor activation. The Journal of Clinical Endocrinology and Metabolism. 1995;80(11):3155–3159
  47. Andrews RC, Rooyackers O, Walker BR. Effects of the 11 beta-hydroxysteroid dehydrogenase inhibitor carbenoxolone on insulin sensitivity in men with type 2 diabetes. The Journal of Clinical Endocrinology and Metabolism. 2003;88(1):285–291
  48. Tomlinson JW, Sherlock M, Hughes B, et al. Inhibition of 11{beta}-HSD1 activity in vivo limits glucocorticoid exposure to human adipose tissue and decreases lipolysis. The Journal of Clinical Endocrinology and Metabolism. 2007;92:857–864
  49. Morris DJ, Souness GW, Latif SA, et al. Effect of chenodeoxycholic acid on 11beta-hydroxysteroid dehydrogenase in various target tissues. Metabolism. 2004;53(6):811–816
  50. Shimoyama Y, Hirabayashi K, Matsumoto H, et al. Effects of glycyrrhetinic acid derivatives on hepatic and renal 11beta-hydroxysteroid dehydrogenase activities in rats. The Journal of Pharmacy and Pharmacology. 2003;55(6):811–817
  51. Hult M, Jornvall H, Oppermann UC. Selective inhibition of human type 1 11beta-hydroxysteroid dehydrogenase by synthetic steroids and xenobiotics. FEBS Letters. 1998;441(1):25–28
  52. Schweizer RA, Atanasov AG, Frey BM, et al. A rapid screening assay for inhibitors of 11beta-hydroxysteroid dehydrogenases (11beta-HSD): flavanone selectively inhibits 11beta-HSD1 reductase activity. Molecular and Cellular Endocrinology. 2003;212(1-2):41–49
  53. Barf T, Vallgarda J, Emond R, et al. Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. Journal of Medicinal Chemistry. 2002;45(18):3813–3815
  54. Koch MA, Wittenberg LO, Basu S, et al. Compound library development guided by protein structure similarity clustering and natural product structure. Proceedings of the National Academy of Sciences of the United States of America. 2004;101(48):16721–16726
  55. Diederich S, Grossmann C, Hanke B, et al. In the search for specific inhibitors of human 11beta-hydroxysteroid-dehydrogenases (11beta-HSDs): chenodeoxycholic acid selectively inhibits 11beta-HSD-I. European Journal of Endocrinology. 2000;142(2):200–207
  56. Alberts P, Engblom L, Edling N, et al. Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice. Diabetologia. 2002;45(11):1528–1532
  57. Alberts P, Nilsson C, Selen G, et al. Selective inhibition of 11{beta}-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains. Endocrinology. 2003;144(11):4755–4762
  58. Hermanowski-Vosatka A, Balkovec JM, Cheng K, et al. 11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice. The Journal of Experimental Medicine. 2005;202(4):517–527
  59. Berthiaume M, Laplante M, Festuccia W, et al. Depot-specific modulation of rat intraabdominal adipose tissue lipid metabolism by pharmacological inhibition of 11beta-hydroxysteroid dehydrogenase type 1. Endocrinology. 2007;148(5):2391–2397
  60. Davani B, Khan A, Hult M, et al. Type 1 11beta -hydroxysteroid dehydrogenase mediates glucocorticoid activation and insulin release in pancreatic islets. The Journal of Biological Chemistry. 2000;275(45):34841–34844
  61. Davani B, Portwood N, Bryzgalova G, et al. Aged transgenic mice with increased glucocorticoid sensitivity in pancreatic beta-cells develop diabetes. Diabetes. 2004;53(Suppl 1):S51–S59
  62. Draper N, Walker EA, Bujalska IJ, et al. Mutations in the genes encoding 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase interact to cause cortisone reductase deficiency. Nature Genetics. 2003;34(4):434–439
  63. Atanasov AG, Nashev LG, Schweizer RA, et al. Hexose-6-phosphate dehydrogenase determines the reaction direction of 11beta-hydroxysteroid dehydrogenase type 1 as an oxoreductase. FEBS Letters. 2004;571(1–3):129–133
  64. Banhegyi G, Benedetti A, Fulceri R, et al. Cooperativity between 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase in the lumen of the endoplasmic reticulum. The Journal of Biological Chemistry. 2004;279(26):27017–27021
  65. Bitar MS. Co-administration of etomoxir and RU-486 mitigates insulin resistance in hepatic and muscular tissues of STZ-induced diabetic rats. Hormone and Metabolic Research. 2001;33(10):577–584
  66. Gettys TW, Watson PM, Taylor IL, et al. RU-486 (Mifepristone) ameliorates diabetes but does not correct deficient beta-adrenergic signalling in adipocytes from mature C57BL/6J-ob/ob mice. International Journal of Obesity and Related Metabolic Disorders. 1997;21(10):865–873
  67. Liang Y, Osborne MC, Monia BP, et al. Antisense oligonucleotides targeted against glucocorticoid receptor reduce hepatic glucose production and ameliorate hyperglycemia in diabetic mice. Metabolism. 2005;54(7):848–855
  68. von Geldern TW, Tu N, Kym PR, et al. Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. Journal of Medicinal Chemistry. 2004;47(17):4213–4230
  69. Jacobson PB, von Geldern TW, Ohman L, et al. Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes. The Journal of Pharmacology and Experimental Therapeutics. 2005;314(1):191–200
  70. Zinker B, Mika A, Nguyen P, et al. Liver-selective glucocorticoid receptor antagonism decreases glucose production and increases glucose disposal, ameliorating insulin resistance. Metabolism. 2007;56(3):380–387
  71. Edgerton DS, Jacobson PB, Opgenorth TJ, et al. Selective antagonism of the hepatic glucocorticoid receptor reduces hepatic glucose production. Metabolism. 2006;55(9):1255–1262
  72. Morgan BP, Liu KK, Dalvie DK, et al. Discovery of potent, non-steroidal and highly selective glucocorticoid receptor antagonists with anti-obesity activity. Letters in Drug Design and Discovery. 2004;1:1–5
  73. Morgan BP, Swick AG, Hargrove DM, et al. Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. Journal of Medicinal Chemistry. 2002;45(12):2417–2424
  74. Link JT, Sorensen B, Patel J, et al. Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators. Journal of Medicinal Chemistry. 2005;48(16):5295–5304

PII: S1521-690X(07)00060-7

doi: 10.1016/j.beem.2007.07.003

Best Practice & Research Clinical Endocrinology & Metabolism
Volume 21, Issue 4 , Pages 607-619 , December 2007

Article Tools

* Image Usage & Resolution