Effects of selective and non-selective glucocorticoid receptor II antagonists on rapid-onset diabetes in young rats

PLoS ONE

Volumn 9, Issue 3, 2014, Pages

  Beaudry, Jacqueline L ^a   Dunford, Emily C ^a   Teich, Trevor ^a   Zaharieva, Dessi ^a   Hunt, Hazel ^b   Belanoff, Joseph K ^b   Riddell, Michael C ^a  

^a YORK UNIVERSITY   (Canada)

^b Corcept Therapeutics ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

C 108297; C 113176; GLUCOCORTICOID RECEPTOR ANTAGONIST; GLUCOSE; MIFEPRISTONE; UNCLASSIFIED DRUG; CORTICOSTERONE; GLUCOCORTICOID RECEPTOR; GLUCOSE BLOOD LEVEL; HORMONE ANTAGONIST; INSULIN; MOLECULAR LIBRARY;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BODY COMPOSITION; BODY MASS; CONTROLLED STUDY; DIABETES MELLITUS; DIET RESTRICTION; DRUG EFFECT; DRUG EFFICACY; GLUCOSE BLOOD LEVEL; GLUCOSE INTOLERANCE; GLUCOSE TOLERANCE; INSULIN RELEASE; INSULIN RESISTANCE; INTRAABDOMINAL FAT; LIPID STORAGE; MALE; NONHUMAN; PANCREAS ISLET BETA CELL; PROTEIN CONTENT; RAPID ONSET DIABETES; RAT; TREATMENT DURATION; WEIGHT GAIN; WEIGHT REDUCTION; ANIMAL; ANTAGONISTS AND INHIBITORS; BLOOD; BODY WEIGHT; CHEMICALLY INDUCED; DIABETES MELLITUS, EXPERIMENTAL; DRUG EFFECTS; LIPID DIET; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY; SPRAGUE DAWLEY RAT;

ANIMALS; BLOOD GLUCOSE; BODY WEIGHT; CORTICOSTERONE; DIABETES MELLITUS, EXPERIMENTAL; DIET, HIGH-FAT; HORMONE ANTAGONISTS; INSULIN; INSULIN RESISTANCE; MALE; MIFEPRISTONE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GLUCOCORTICOID; SMALL MOLECULE LIBRARIES;

EID: 84898657978     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0091248     Document Type: Article

References (61)

1. Funder JW (1997) Glucocorticoid and mineralocorticoid receptors: Biology and clinical (Pubitemid 27101827)
2. De Kloet ER, Vreugdenhil E, Oitzl MS, Joels M (1998) Brain corticosteroid receptor balance in health and disease. Endocr Rev 19: 269-301. (Pubitemid 29117816)
3. Zhou J, Cidlowski JA (2005) The human glucocorticoid receptor: One gene, multiple proteins and diverse responses. Steroids 70: 407-417. (Pubitemid 40616039)
4. Rhen T, Cidlowski JA (2005) Antiinflammatory action of glucocorticoids-new mechanisms for old drugs. N Engl J Med 353: 1711-1723.
5. Andrews RC, Walker BR (1999) Glucocorticoids and insulin resistance: Old hormones, new targets. Clin Sci (Lond) 96: 513-523. (Pubitemid 29237902)
6. McMahon M, Gerich J, Rizza R (1988) Effects of glucocorticoids on carbohydrate metabolism. Diabetes Metab Rev 4: 17-30. (Pubitemid 18072099)
7. Shibli-Rahhal A, Van Beek M, Schlechte JA (2006) Cushing's syndrome. Clin Dermatol 24: 260-265. (Pubitemid 43975261)
8. Kelly HW, Sternberg AL, Lescher R, Fuhlbrigge AL, Williams P, et al. (2012) Effect of inhaled glucocorticoids in childhood on adult height. N Engl J Med 367: 904-912.
9. Schacke H, Docke WD, Asadullah K (2002) Mechanisms involved in the side effects of glucocorticoids. Pharmacol Ther 96: 23-43. (Pubitemid 35346616)
10. Nielsen MF, Caumo A, Chandramouli V, Schumann WC, Cobelli C, et al. (2004) Impaired basal glucose effectiveness but unaltered fasting glucose release and gluconeogenesis during short-term hypercortisolemia in healthy subjects. Am J Physiol Endocrinol Metab 286: E102-10. (Pubitemid 38036615)
11. Hoes JN, van der Goes MC, van Raalte DH, van der Zijl NJ, den Uyl D, et al. (2011) Glucose tolerance, insulin sensitivity and beta-cell function in patients with rheumatoid arthritis treated with or without low-to-medium dose glucocorticoids. Ann Rheum Dis 70: 1887-1894.
12. Lansang MC, Hustak LK (2011) Glucocorticoid-induced diabetes and adrenal suppression: How to detect and manage them. Cleve Clin J Med 78: 748-756.
13. Simmons LR, Molyneaux L, Yue DK, Chua EL (2012) Steroid-induced diabetes: Is it just unmasking of type 2 diabetes? ISRN Endocrinol 2012: 910905.
14. Chan O, Inouye K, Riddell MC, Vranic M, Matthews SG (2003) Diabetes and the hypothalamo-pituitary-adrenal (HPA) axis. Minerva Endocrinol 28: 87-102.
15. Matthews LC, Hanley NA (2011) The stress of starvation: Glucocorticoid restraint of beta cell development. Diabetologia 54: 223-226.
16. Wang Y, Nakagawa Y, Liu L, Wang W, Ren X, et al. (2011) Tissue-specific dysregulation of hexose-6-phosphate dehydrogenase and glucose-6-phosphate transporter production in db/db mice as a model of type 2 diabetes. Diabetologia 54: 440-450.
17. Anagnostis P, Athyros VG, Tziomalos K, Karagiannis A, Mikhailidis DP (2009) Clinical review: The pathogenetic role of cortisol in the metabolic syndrome: A hypothesis. J Clin Endocrinol Metab 94: 2692-2701.
18. Rosmond R (2005) Role of stress in the pathogenesis of the metabolic syndrome. Psychoneuroendocrinology 30: 1-10. (Pubitemid 39195039)
19. Stewart PM (1996) 11 beta-hydroxysteroid dehydrogenase: Implications for clinical medicine. Clin Endocrinol (Oxf) 44: 493-499. (Pubitemid 26168766)
20. Bujalska IJ, Draper N, Michailidou Z, Tomlinson JW, White PC, et al. (2005) Hexose-6-phosphate dehydrogenase confers oxo-reductase activity upon 11 beta-hydroxysteroid dehydrogenase type 1. J Mol Endocrinol 34: 675-684. (Pubitemid 40903593)
21. Johanssen S, Allolio B (2007) Mifepristone (RU 486) in cushing's syndrome. Eur J Endocrinol 157: 561-569. (Pubitemid 350187372)
22. Belavic JM (2013) Drug updates and approvals: 2012 in review. Nurse Pract 38: 24-42.
23. [Anonymous]. (2012) Mifepristone (korlym) for cushing's syndrome. Med Lett Drugs Ther 54: 46-47.
24. Fleseriu M, Biller BM, Findling JW, Molitch ME, Schteingart DE, et al. (2012) Mifepristone, a glucocorticoid receptor antagonist, produces clinical and metabolic benefits in patients with cushing's syndrome. J Clin Endocrinol Metab 97: 2039-2049.
25. Goldberg JR, Plescia MG, Anastasio GD (1998) Mifepristone (RU 486): Current knowledge and future prospects. Arch Fam Med 7: 219-222. (Pubitemid 128433243)
26. Zalachoras I, Houtman R, Atucha E, Devos R, Tijssen AM, et al. (2013) Differential targeting of brain stress circuits with a selective glucocorticoid receptor modulator. Proc Natl Acad Sci 110:7910-7915.
27. Asagami T, Belanoff JK, Azuma J, Blasey CM, Clark RD, et al. (2011) Selective glucocorticoid receptor (GR-II) antagonist reduces body weight gain in mice. J Nutr Metab 2011: 235389. 10.1155/2011/235389.
28. Belanoff JK, Blasey CM, Clark RD, Roe RL (2011) Selective glucocorticoid receptor (type II) antagonists prevent weight gain caused by olanzapine in rats. Eur J Pharmacol 655: 117-120.
29. Shpilberg Y, Beaudry JL, D'Souza A, Campbell JE, Peckett A, et al. (2012) A rodent model of rapid-onset diabetes induced by glucocorticoids and high-fat feeding. Dis Model Mech. doi:10.1242/dmm.008912
30. Beaudry JL, D'Souza A, Teich T, Tsushima R, Riddell MC (2013) Exogenous glucocorticoids and a high-fat diet cause severe hyperglycemia and hyperinsulinemia and limit islet glucose responsiveness in young male sprague-dawley rats. Endocrinology 154: 3197-3208.
31. Holness MJ, Smith ND, Greenwood GK, Sugden MC (2005) Interactive influences of peroxisome proliferator-activated receptor alpha activation and glucocorticoids on pancreatic beta cell compensation in insulin resistance induced by dietary saturated fat in the rat. Diabetologia 48: 2062-2068. (Pubitemid 41416917)
32. Wallace TM, Levy JC, Matthews DR (2004) Use and abuse of HOMA modeling. Diabetes Care 27: 1487-1495. (Pubitemid 38680001)
33. Hoffman RP (2008) Indices of insulin action calculated from fasting glucose and insulin reflect hepatic, not peripheral, insulin sensitivity in african-american and caucasian adolescents. Pediatr Diabetes 9: 57-61. (Pubitemid 351784996)
34. Koopman R, Schaart G, Hesselink MK (2001) Optimisation of oil red O staining permits combination with immunofluorescence and automated quantification of lipids. Histochem Cell Biol 116: 63-68. (Pubitemid 32695819)
35. Campbell JE, Peckett AJ, D'souza AM, Hawke TJ, Riddell MC (2011) Adipogenic and lipolytic effects of chronic glucocorticoid exposure. Am J Physiol Cell Physiol 300: C198-209.
36. Taskinen MR (2003) Diabetic dyslipidaemia: From basic research to clinical practice. Diabetologia 46: 733-749.
37. Roy RR, Gardiner PF, Simpson DR, Edgerton VR (1983) Glucocorticoidinduced atrophy in different fibre types of selected rat jaw and hind-limb muscles. Arch Oral Biol 28: 639-643.
38. Chrousos GP (2004) Is 11beta-hydroxysteroid dehydrogenase type 1 a good therapeutic target for blockade of glucocorticoid actions? Proc Natl Acad Sci U S A 101: 6329-6330. (Pubitemid 38585971)
39. D'souza AM, Beaudry JL, Szigiato AA, Trumble SJ, Snook LA, et al. (2012) Consumption of a high-fat diet rapidly exacerbates the development of fatty liver disease that occurs with chronically elevated glucocorticoids. Am J Physiol Gastrointest Liver Physiol 302: G850-863.
40. Gross C, Blasey CM, Roe RL, Allen K, Block TS, et al. (2009) Mifepristone treatment of olanzapine-induced weight gain in healthy men. Adv Ther 26: 959-969.
41. Beebe KL, Block T, Debattista C, Blasey C, Belanoff JK (2006) The efficacy of mifepristone in the reduction and prevention of olanzapine-induced weight gain in rats. Behav Brain Res 171: 225-229. (Pubitemid 43946497)
42. Belanoff JK, Blasey CM, Clark RD, Roe RL (2010) Selective glucocorticoid receptor (type II) antagonist prevents and reverses olanzapine-induced weight gain. Diabetes Obes Metab 12: 545-547.
43. Bourgeois S, Pfahl M, Baulieu EE (1984) DNA binding properties of glucocorticosteroid receptors bound to the steroid antagonist RU-486. EMBO J 3: 751-755.
44. Heikinheimo O, Kontula K, Croxatto H, Spitz I, Luukkainen T, et al. (1987) Plasma concentrations and receptor binding of RU 486 and its metabolites in humans. J Steroid Biochem 26: 279-284. (Pubitemid 17040134)
45. Sartor O, Cutler GB Jr (1996) Mifepristone: Treatment of cushing's syndrome. Clin Obstet Gynecol 39: 506-510. (Pubitemid 26143728)
46. Dallman MF (2003) Fast glucocorticoid feedback favors 'the munchies'. Trends Endocrinol Metab 14: 394-396. (Pubitemid 37392209)
47. Okada S, York DA, Bray GA (1992) Mifepristone (RU 486), a blocker of type II glucocorticoid and progestin receptors, reverses a dietary form of obesity. Am J Physiol 262: R1106-10.
48. Langley SC, York DA (1990) Effects of antiglucocorticoid RU 486 on development of obesity in obese fa/fa zucker rats. Am J Physiol 259: R539-44.
49. Taylor AI, Frizzell N, McKillop AM, Flatt PR, Gault VA (2009) Effect of RU486 on hepatic and adipocyte gene expression improves diabetes control in obesity-type 2 diabetes. Horm Metab Res 41: 899-904.
50. Friedman JE, Yun JS, Patel YM, McGrane MM, Hanson RW (1993) Glucocorticoids regulate the induction of phosphoenolpyruvate carboxykinase (GTP) gene transcription during diabetes. J Biol Chem 268: 12952-12957. (Pubitemid 23182469)
51. Vander Kooi BT, Onuma H, Oeser JK, Svitek CA, Allen SR, et al. (2005) The glucose-6-phosphatase catalytic subunit gene promoter contains both positive and negative glucocorticoid response elements. Mol Endocrinol 19: 3001-3022. (Pubitemid 41697718)
52. Debono M, Chadarevian R, Eastell R, Ross RJ, Newell-Price J (2013) Mifepristone reduces insulin resistance in patient volunteers with adrenal incidentalomas that secrete low levels of cortisol: A pilot study. PLoS One 8: e60984. doi:10.1371/journal.pone.0060984
53. Haller J, Mikics E, Makara GB (2008) The effects of non-genomic glucocorticoid mechanisms on bodily functions and the central neural system. A critical evaluation of findings. Front Neuroendocrinol 29: 273-291. (Pubitemid 351467120)
54. Peckett AJ, Wright DC, Riddell MC (2011) The effects of glucocorticoids on adipose tissue lipid metabolism. Metabolism 60: 1500-1510.
55. Spiga F, Harrison LR, Wood SA, Atkinson HC, MacSweeney CP, et al. (2007) Effect of the glucocorticoid receptor antagonist org 34850 on basal and stressinduced corticosterone secretion. J Neuroendocrinol 19: 891-900. (Pubitemid 47555234)
56. Deschoolmeester J, Palming J, Persson T, Pereira MJ, Wallerstedt E, et al. (2013) Differences between men and women in the regulation of adipose 11beta-HSD1 and in its association with adiposity and insulin resistance. Diabetes Obes Metab 15:1056-60.
57. Dallman MF, la Fleur SE, Pecoraro NC, Gomez F, Houshyar H, et al. (2004) Minireview: Glucocorticoids-food intake, abdominal obesity, and wealthy nations in 2004. Endocrinology 145: 2633-2638. (Pubitemid 38686208)
58. Linssen MM, van Raalte DH, Toonen EJ, Alkema W, van der Zon GC, et al. (2011) Prednisolone-induced beta cell dysfunction is associated with impaired endoplasmic reticulum homeostasis in INS-1E cells. Cell Signal 23: 1708-1715.
59. Koizumi M, Yada T (2008) Sub-chronic stimulation of glucocorticoid receptor impairs and mineralocorticoid receptor protects cytosolic Ca2+ responses to glucose in pancreatic beta-cells. J Endocrinol 197: 221-229. (Pubitemid 351696235)
60. van Raalte DH, Ouwens DM, Diamant M (2009) Novel insights into glucocorticoid-mediated diabetogenic effects: Towards expansion of therapeutic options? Eur J Clin Invest 39: 81-93.
61. Mohler ML, He Y, Wu Z, Hong SS, Miller DD (2007) Non-steroidal glucocorticoid receptor antagonists: The race to replace RU-486 for antiglucocorticoid therapy. Expert Opin Ther Pat 17: 59-81. (Pubitemid 46075653)