Chronic glucokinase activation reduces glycaemia and improves glucose tolerance in high-fat diet fed mice

European Journal of Pharmacology

Volumn 663, Issue 1-3, 2011, Pages 80-86

  Winzell, Maria Sörhede ^a   Coghlan, Matthew ^b   Leighton, Brendan ^b   Frangioudakis, Georgia ^c   Smith, David M ^b   Storlien, Leonard H ^d   Ahrén, Bo ^a  

^a LUND UNIVERSITY   (Sweden)

^b ASTRAZENECA   (United Kingdom)

^c GARVAN INSTITUTE OF MEDICAL RESEARCH   (Australia)

^d UNIVERSITY OF SYDNEY   (Australia)

Author keywords

Glucokinase; Glucose tolerance; High fat diet; Insulin resistance; Insulin secretion; Islet

Indexed keywords

3 (2 METHOXY 1 METHYL ETHOXY) 5 (4 METHYLSULFONYLPHENOXY) N (3 METHYL 1,2,4 THIADIAZOL 5 YL)BENZAMIDE; AGENTS AFFECTING CARBOHYDRATE METABOLISM; GKA 71; GLUCOKINASE; GLUCOSE; GLYCOGEN; INSULIN; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; ENZYME ACTIVATION; FEMALE; GLUCOSE BLOOD LEVEL; GLUCOSE OXIDATION; GLUCOSE TOLERANCE; GLYCEMIC CONTROL; IN VITRO STUDY; IN VIVO STUDY; INSULIN BLOOD LEVEL; INSULIN RELEASE; INSULIN RESISTANCE; INSULIN SENSITIVITY; LIPID DIET; MOUSE; NONHUMAN; PANCREAS ISLET CELL FUNCTION; PRIORITY JOURNAL; TREATMENT DURATION;

ADMINISTRATION, ORAL; ANIMALS; BLOOD GLUCOSE; DIETARY FATS; ENZYME ACTIVATION; FEMALE; GLUCOKINASE; GLUCOSE TOLERANCE TEST; HUMANS; INSULIN; ISLETS OF LANGERHANS; LIVER; MICE; RATS; SULFONES; THIADIAZOLES; TIME FACTORS;

EID: 79959308013     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2011.05.009     Document Type: Article

References (37)

1. Ahrén, B., Pacini, G., 2002. Insufficient islet compensation to insulin resistance vs. reduced glucose effectiveness in glucose-intolerant mice. Am. J. Physiol. Endocrinol. Metab. 283, E738-E744.
2. Ahrén, B., Pacini, G., 2005. Islet adaptation to insulin resistance: mechanisms and implications for intervention. Diabetes Obes. Metab. 7, 2-8.
3. Bessesen, D.H., Bull, S., Cornier, M.A., 2008. Trafficking of dietary fat and resistance to obesity. Physiol. Behav. 94, 681-688.
4. Brocklehurst, K.J., Payne, V.A., Davies, R.A., Carroll, D., Vertigan, H.L., Wightman, H.J., Aiston, S., Waddell, I.D., Leighton, B., Coghlan, M.P., Agius, L., 2004. Stimulation of hepatocyte glucose metabolism by novel small molecule glucokinase activators. Diabetes 53, 535-541. (Pubitemid 38270620)
5. Coghlan, M., Leighton, B., 2008. Glucokinase activators in diabetes management. Expert Opin. Investig. Drugs 17, 145-167.
6. Coope, G.J., Atkinson, A.M., Allott, C., McKerrecher, D., Johnstone, C., Pike, K.G., Holme, P.C., Vertigan, H., Gill, D., Coghlan, M.P., Leighton, B., 2006. Predictive blood glucose lowering efficacy by glucokinase activators in high fat fed female Zucker rats. Br. J. Pharmacol. 149, 328-335.
7. Cuesta-Munoz, A.L., Huopio, H., Otonkoski, T., Gomez-Zumaquero, J.M., Näntö-Salonen, K., Rahier, J., Lopez-Enriquez, S., Garcia-Gimeno, M.A., Sanz, P., Soriguer, F., Laakso, M., 2004. Severe persistent hyperinsulinemic hypoglycemia due to a de novo glucokinase mutation. Diabetes 53, 2164-2168. (Pubitemid 38970771)
8. Desai, U.J., Slosberg, E.D., Boettcher, B.R., Caplan, S.L., Fanelli, B., Stephan, Z., Gunther, V.J., Kaleko, M., Connelly, S., 2001. Phenotypic correction of diabetic mice by adenovirus-mediated glucokinase expression. Diabetes 50, 2287-2295. (Pubitemid 33641913)
9. Dunne, M.J., Cosgrove, K.E., Shepherd, R.M., Aynsley-Green, A., Lindley, K.J., 2004. Hyperinsulinism in infancy: from basic science to clinical disease. Physiol. Rev. 84, 239-275.
10. Dunning, B.E., Gerich, J.E., 2007. The role of alpha-cell dysregulation in fasting and postprandial hyperglycemia in type 2 diabetes and therapeutic implications. Endocr. Rev. 28, 253-283.
11. Efanov, A.M., Barrett, D.G., Brenner, M.B., Briggs, S.L., Delaunois, A., Durbin, J.D., Giese, U., Guo, H., Radloff, M., Gil, G.S., Sewing, S., Wang, Y., Weichart, A., Zaliani, A., Gromada, J., 2005. A novel glucokinase activator modulates pancreatic islet and hepatocyte function. Endocrinology 146, 3696-3701. (Pubitemid 41175734)
12. Gomis, R.R., Ferrer, J.C., Guinovart, J.J., 2000. Shared control of hepatic glycogen synthesis by glycogen synthase and glucokinase. Biochem. J. 351 (Pt 3), 811-816.
13. Gorman, T., Hope, D.C., Brownlie, R., Yu, A., Gill, D., Löfvenmark, J., Wedin, M., Mayers, R.M., Snaith, M.R., Smith, D.M., 2008. Effect of high-fat diet on glucose homeostasis and gene expression in glucokinase knockout mice. Diabetes Obes. Metab. 10, 885-897.
14. Grimsby, J., Sarabu, R., Corbett, W.L., Haynes, N.E., Bizzarro, F.T., Coffey, J.W., Guertin, K.R., Hilliard, D.W., Kester, R.F., Mahaney, P.E., Marcus, L., Qi, L., Spence, C.L., Tengi, J., Magnuson, M.A., Chu, C.A., Dvorozniak, M.T., Matschinsky, F.M., Grippo, J.F., 2003. Allosteric activators of glucokinase: potential role in diabetes therapy. Science 301, 370-373. (Pubitemid 36877072)
15. Grupe, A., Hultgren, B., Ryan, A., Ma, Y.H., Bauer, M., Stewart, T.A., 1995. Transgenic knockouts reveal a critical requirement for pancreatic beta cell glucokinase in maintaining glucose homeostasis. Cell 83, 69-78.
16. Hariharan, N., Farrelly, D., Hagan, D., Hillyer, D., Arbeeny, C., Sabrah, T., Treloar, A., Brown, K., Kalinowski, S., Mookhtiar, K., 1997. Expression of human hepatic glucokinase in transgenic mice liver results in decreased glucose levels and reduced body weight. Diabetes 46, 11-16. (Pubitemid 27009942)
17. Home, P.D., Pacini, G., 2008. Hepatic dysfunction and insulin insensitivity in type 2 diabetes mellitus: a critical target for insulin-sensitizing agents. Diabetes Obes. Metab. 10, 699-718.
18. Johnson, D., Shepherd, R.M., Gill, D., Gorman, T., Smith, D.M., Dunne, M.J., 2007. Glucose-dependent modulation of insulin secretion and intracellular calcium ions by GKA50, a glucokinase activator. Diabetes 56, 1694-1702. (Pubitemid 46842608)
19. Kahn, S.E., 2003. The relative contributions of insulin resistance and beta-cell dysfunction to the pathophysiology of type 2 diabetes. Diabetologia 46, 3-19. (Pubitemid 36237741)
20. Matschinsky, F.M., 1996. Banting Lecture 1995. A lesson in metabolic regulation inspired by the glucokinase glucose sensor paradigm. Diabetes 45, 223-241.
21. Matschinsky, F.M., 2002. Regulation of pancreatic beta-cell glucokinase: from basics to therapeutics. Diabetes 51 (Suppl 3), S394-S404. (Pubitemid 35403423)
22. Matschinsky, F.M., 2009. Assessing the potential of glucokinase activators in diabetes therapy. Nat. Rev. Drug Discov. 8, 399-416.
23. O'Doherty, R.M., Lehman, D.L., Telemaque-Potts, S., Newgard, C.B., 1999. Metabolic impact of glucokinase overexpression in liver: lowering of blood glucose in fed rats is accompanied by hyperlipidemia. Diabetes 48, 2022-2027. (Pubitemid 29458366)
24. Pacini, G., Thomaseth, K., Ahrén, B., 2001. Contribution to glucose tolerance of insulin-independent vs. insulin-dependent mechanisms in mice. Am. J. Physiol. Endocrinol. Metab. 281, E693-E703.
25. Pacini, G., Ahrén, M., Ahrén, B., 2009. Reappraisal of the intravenous glucose tolerance index for a simple assessment of insulin sensitivity in mice. Am. J. Physiol. Regul. Integr. Comp. Physiol. 296, R1316-R1324.
26. Postic, C., Shiota, M., Niswender, K.D., Jetton, T.L., Chen, Y., Moates, J.M., Shelton, K.D., Lindner, J., Cherrington, A.D., Magnuson, M.A., 1999. Dual roles for glucokinase in glucose homeostasis as determined by liver and pancreatic beta cell-specific gene knock-outs using Cre recombinase. J. Biol. Chem. 274, 305-315.
27. Schuit, F.C., Huypens, P., Heimberg, H., Pipeleers, D.G., 2001. Glucose sensing in pancreatic beta-cells: a model for the study of other glucose-regulated cells in gut, pancreas, and hypothalamus. Diabetes 50, 1-11. (Pubitemid 32047973)
28. Seoane, J., Gomez-Foix, A.M., O'Doherty, R.M., Gomez-Ara, C., Newgard, C.B., Guinovart, J.J., 1996. Glucose 6-phosphate produced by glucokinase, but not hexokinase I, promotes the activation of hepatic glycogen synthase. J. Biol. Chem. 271, 23756-23760.
29. Shiota, M., Postic, C., Fujimoto, Y., Jetton, T.L., Dixon, K., Pan, D., Grimsby, J., Grippo, J.F., Magnuson, M.A., Cherrington, A.D., 2001. Glucokinase gene locus transgenic mice are resistant to the development of obesity-induced type 2 diabetes. Diabetes 50, 622-629. (Pubitemid 32195228)
30. Terauchi, Y., Takamoto, I., Kubota, N., Matsui, J., Suzuki, R., Komeda, K., Hara, A., Toyoda, Y., Miwa, I., Aizawa, S., Tsutsumi, S., Tsubamoto, Y., Hashimoto, S., Eto, K., Nakamura, A., Noda, M., Tobe, K., Aburatani, H., Nagai, R., Kadowaki, T., 2007. Glucokinase and IRS-2 are required for compensatory beta cell hyperplasia in response to high-fat diet-induced insulin resistance. J. Clin. Invest. 117, 246-257.
31. Valera, A., Bosch, F., 1994. Glucokinase expression in rat hepatoma cells induces glucose uptake and is rate limiting in glucose utilization. Eur. J. Biochem. 222, 533-539.
32. Waring, M.J., Brogan, I.J., Coghlan, M., Johnsatone, C., Jones, H.B., Leighton, B., McKerrecher, D., Pike, K.G., 2011. Overcoming retinoic acid receptor-alpha based testicular toxicology in the optimisation of glucokinase activators. Med. Chem. Comm., Accepted for publication.
33. Winzell, M.S., Ahrén, B., 2004. The high-fat diet-fed mouse: a model for studying mechanisms and treatment of impaired glucose tolerance and type 2 diabetes. Diabetes 53 (Suppl 3), S215-S219. (Pubitemid 39564546)
34. Winzell, M.S., Magnusson, C., Ahrén, B., 2007. Temporal and dietary fat content-dependent islet adaptation to high-fat feeding-induced glucose intolerance in mice. Metabolism 56, 122-128. (Pubitemid 44855020)
35. Wu, C., Kang, J.E., Peng, L.J., Li, H., Khan, S.A., Hillard, C.J., Okar, D.A., Lange, A.J., 2005. Enhancing hepatic glycolysis reduces obesity: differential effects on lipogenesis depend on site of glycolytic modulation. Cell Metab. 2, 131-140.
36. Xu, L.Z., Weber, I.T., Harrison, R.W., Gidh-Jain, M., Pilkis, S.J., 1995. Sugar specificity of human beta-cell glucokinase: correlation of molecular models with kinetic measurements. Biochemistry 34, 6083-6092.
37. Zierath, J.R., Kawano, Y., 2003. The effect of hyperglycaemia on glucose disposal and insulin signal transduction in skeletal muscle. Best Pract. Res. Clin. Endocrinol. Metab. 17, 385-398.