11β-hydroxysteroid dehydrogenase type 1 - Second part selective inhibition for the management of metabolic abnormalities associated with obesity;La 11β-hydroxystéroïde déshydrogénase de type 1 - 2e Partie inhibition sélective pour traiter les anomalies métaboliques associées à l'obésité

Medecine des Maladies Metaboliques

Volumn 3, Issue 6, 2009, Pages 595-600

  Iovino, A ^a   Scheen, André J ^a  

^a UNIVERSITY OF LIÈGE   (Belgium)

Author keywords

11 hydroxysteroid dehydrogenase type 1; Abdominal obesity; Cortisol; Metabolic syndrome; Selective inhibition; Type 2 diabetes

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; ANTIDIABETIC AGENT; CARBENOXOLONE; CORTISONE; INCB 13739; METFORMIN; MIFEPRISTONE; ORAL ANTIDIABETIC AGENT; PF 00915275; PREDNISOLONE; PREDNISONE; UNCLASSIFIED DRUG;

ABDOMINAL OBESITY; DRUG INHIBITION; GLUCOSE TOLERANCE; HUMAN; HYPOKALEMIA; HYPOTENSION; IMMUNOHISTOCHEMISTRY; IN VIVO STUDY; INSULIN RESISTANCE; METABOLIC DISORDER; METABOLIC SYNDROME X; NON INSULIN DEPENDENT DIABETES MELLITUS; REVIEW;

EID: 77949386560     PISSN: 19572557     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1957-2557(09)73624-7     Document Type: Article

References (38)

1. e partie : Rôle de l'exposition tissulaire au cortisol dans le risque métabolique lié à l'obésité. Médecine des maladies Métaboliques, 2009;3:507-13.
2. Anagnostis P, Athyros VG, Tziomalos K, et al. Clinical review. The pathogenetic role of cortisol in the metabolic syndrome: a hypothesis. J Clin Endocrinol Metab 2009;94:2692-701.
3. Boyle CD, Kowalski TJ. 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: a review of recent patents. Exp Opin Ther Pat 2009;19:801-25.
4. Tomlinson JW, Stewart PM. Modulation of glucocorticoid action and the treatment of type-2 diabetes. Best Pract Res Clin Endocrinol Metab 2007;21:607-19.
5. Bujalska IJ, Kumar S, Stewart PM. Does central obesity reflect "Cushing's disease of the omentum"? Lancet 1997;349:1210-3.
6. Basu R, Singh RJ, Basu A, et al. Obesity and type 2 diabetes do not alter splanchnic cortisol production in humans. J Clin Endocrinol Metab 2005;90:3919-26.
7. Sandeep TC, Andrew R, Homer NZM, et al. Increased in vivo regeneration of cortisol in adipose tissue in human obesity and effects of the 11â-hydroxysteroid dehydrogenase type 1 inhibitor carbenoxolone. Diabetes 2005;54:872-9.
8. Alberti L, Girola A, Gilardini L, et al. Type 2 diabetes and metabolic syndrome are associated with increased expression of 11beta-hydroxysteroid dehydrogenase type 1 in obese subjects. Int J Obes 2007;31:1826-31.
9. Paulsen SK, Pedersen SB, Fisker S, et al. 11β-HSD type 1 expression in human adipose tissue: impact of gender, obesity, and fat localization. Obesity 2007;15:1954-60.
10. Desbriere R, Vuaroqueaux V, Achard V, et al. 11β-hydroxysteroid dehydrogenase type 1 mRNA is increased in both visceral and subcutaneous adipose tissue of obese patients. Obesity 2006;14:794-8.
11. Munoz R, Carvajal C, Escalona A, et al. 11β-hydroxysteroid dehydrogenase type 1 is overexpressed in subcutaneous adipose tissue of morbidly obese patients. Obes Surg 2009;19:764-70.
12. Tomlinson JW, Walker EA, Bujalska IJ, et al. 11β-hydroxysteroïd dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response. Endocr Rev 2004;25:831-66.
13. Veilleux A, Rhéaume C, Daris M, et al. Omental adipose tissue type 1 11beta-hydroxysteroid dehydrogenase oxoreductase activity, body fat distribution, and metabolic alterations in women. J Clin Endocrinol Metab 2009;94:3550-7.
14. Stimson RH, Andersson J, Andrew R, et al. Cortisol release from adipose tissue by 11β-hydroxysteroid dehydrogenase type 1 in humans. Diabetes 2009;58:46-53.
15. Andrew R, Westerbacka J, Wahren J, et al. The contribution of visceral adipose tissue to splanchnic cortisol production in healthy humans. Diabetes 2005;54:1364-70.
16. Basu R, Basu A, Grudzien M, et al. Liver is the site of splanchnic cortisol production in obese nondiabetic humans. Diabetes 2009;58:39-45.
17. Rask E, Olsson T, Söderberg S, et al. Tissue-specific dysregulation of cortisol metabolism in human obesity. J Clin Endocrinol Metab 2001;86:1418-21.
18. Stewart PM, Boulton A, Kumar S, et al. Cortisol metabolism in human obesity: impaired cortisone→cortisol conversion in subjects with central adiposity. J Clin Endocrinol Metab 1999;84:1022-7.
19. Rask E, Walker BR, Söderberg S, et al. Tissue-specific changes in peripheral cortisol metabolism in obese women: increased adipose 11β-hydroxysteroid dehydrogenase type 1 activity. J Clin Endocrinol Metab 2002;87:3330-6.
20. Stewart PM, Tomlinson JW. Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 for patients with metabolic syndrome, is the target liver, fat, or both? (commentary). Diabetes 2009;58:14-5.
21. Tomlinson JW, Finney J, Gay C, et al. Impaired glucose tolerance and insulin resistance are associated with increased adipose 11beta-hydroxysteroid dehydrogenase type 1 expression and elevated hepatic 5alpha-reductase activity. Diabetes 2008;57:2652-60.
22. Purnell JQ, Kahn SE, Samuels MH, et al. Enhanced cortisol production rates, free cortisol, and 11 Beta HSD-1 expression correlate with visceral fat and insulin resistance in men: effect of weight loss. Am J Physiol Endocrinol Metab 2009;296:E351-7.
23. Valsamakis G, Anwar A, Tomlinson JW, et al. 11β-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus. J Clin Endocrinol Metab 2004;89:4755-61.
24. Swali A, Walker EA, Lavery GG, et al. 11beta-hydroxysteroid dehydrogenase type 1 regulates insulin and glucagon secretion in pancreatic islets. Diabetologia 2008;51:2003-11.
25. Nieman LK, Chrousos GP, Kellner C, et al. Successful treatment of Cushing's syndrome with the glucocorticoid antagonist RU 486. J Clin Endocrinol Metab 1985;61:536-40.
26. Walker BR, Andrew R. Tissue production of cortisol by 11β-hydroxysteroid dehydrogenase type 1 and metabolic disease. Ann NY Acad Sci 2006;1083:165-84.
27. Friedman JE, Sun Y, Ishizuka T, et al. Phosphoenolpyruvate carboxykinase (GTP) gene transcription and hyperglycemia are regulated by glucocorticoids in genetically obese db/db transgenic mice. J Biol Chem 1997;272:31475 -81.
28. 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. J Clin Endocrinol Metab 1995;80:3155-9.
29. Andrews RC, Rooyackers O, Walker B. Effects of the 11β- hydroxysteroid dehydrogenase inhibitor carbenoxolone on insulin sensitivity in men with type 2 diabetes. J Clin Endocrinol Metab 2003;88:285-91.
30. Wamil M, Seckl JR. Inhibition of 11β-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Discov Today 2007;12:504-20.
31. Bujalska IJ, Gathercole LL, Tomlinson JW, et al. A novel selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor prevents human adipogenesis. J Endocrinol 2008;197:297-307.
32. Courtney R, Stewart PM, Toh M, et al. Modulation of 11β- hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J Clin Endocrinol Metab 2008;93:550-6.
33. Gumy C, Thurnbichler C, Aubry EM, et al. Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 by plant extracts used as traditional antidiabetic medicines. Fitoterapia 2009; Jan 23 [Epub ahead of print].
34. Hawkins M, Hunter D, Kishore P, et al. INCB013739, a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1), improves insulin sensitivity and lowers plasma cholesterol over 28 days in patients with type 2 diabetes mellitus. Diabetes 2008;57(Suppl.1): A99-A100 [Abstract 344-OR].
35. Rosenstock J, Banarer S, Fonseca V, et al. Efficacy and safety of the 11-B-HSD1 inhibitor, INCB13739, added to metformin therapy in patients with type 2 diabetes. Diabetes 2009;58(Suppl.1): LB3 [Late breaking abstract 7-LB].
36. Ye YL, Zhou Z, Zou HJ, et al. Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes. Bioorg Med Chem 2009;17:5722-32.
37. Vantyghem MC, Marcelli-Tourvieille S, Defrance F, et al. 11β-hydroxystéroïde déshydrogénases. Avancées récentes. Ann Endocrinol (Paris) 2007;68:349-56.
38. Strachan MWJ, Reynolds RM, Frier BM, et al. The role of metabolic derangements and glucocorticoid excess in the aetiology of cognitive impairment in type 2 diabetes. Implications for future therapeutic strategies. Diabetes Obes Metab 2009;11:407-14.