Multiple mechanisms of GW-9508, a selective G protein-coupled receptor 40 agonist, in the regulation of glucose homeostasis and insulin sensitivity

American Journal of Physiology - Endocrinology and Metabolism

Volumn 304, Issue 6, 2013, Pages

  Ou, Horng Yih ^a   Wu, Hung Tsung ^b   Hung, Hao Chang ^a   Yang, Yi Ching ^a   Wu, Jin Shang ^a   Chang, Chih Jen ^a,b  

^a NATIONAL CHENG KUNG UNIVERSITY   (Taiwan)

^b NATIONAL CHENG KUNG UNIVERSITY   (Taiwan)

Author keywords

Diabetes; Fetuin A; G protein coupled receptor 40; Insulin resistance; Partial agonist

Indexed keywords

AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; FETUIN A; G PROTEIN COUPLED RECEPTOR 40; GLUCOSE; GLYCOGEN; GLYCOGEN SYNTHASE KINASE 3BETA; GW 9508; INSULIN; PALMITIC ACID; PHOSPHOLIPASE C; PROTEIN KINASE B; PROTEIN KINASE C; SMALL INTERFERING RNA; UNCLASSIFIED DRUG; AHSG PROTEIN, MOUSE; ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR; GPR40 PROTEIN, MOUSE; GW9508; METHYLAMINE; PROPIONIC ACID DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DIABETES MELLITUS; DRUG MECHANISM; GLUCOSE BLOOD LEVEL; GLUCOSE HOMEOSTASIS; GLUCOSE INTOLERANCE; GLYCOGEN ANALYSIS; HUMAN; HUMAN CELL; INSULIN BLOOD LEVEL; INSULIN RESISTANCE; INSULIN SENSITIVITY; LIPID DIET; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; SIGNAL TRANSDUCTION; ANIMAL; BLOOD; C57BL MOUSE; CELL STRAIN HEPG2; DRUG ANTAGONISM; DRUG EFFECT; DRUG POTENTIATION; GENETICS; GLYCOGEN LIVER LEVEL; HYPERGLYCEMIA; LIVER; METABOLISM; NON INSULIN DEPENDENT DIABETES MELLITUS; RNA INTERFERENCE;

ALPHA-2-HS-GLYCOPROTEIN; ANIMALS; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DIET, HIGH-FAT; HEP G2 CELLS; HUMANS; HYPERGLYCEMIA; HYPOGLYCEMIC AGENTS; INSULIN; INSULIN RESISTANCE; LIVER; LIVER GLYCOGEN; MALE; METHYLAMINES; MICE; MICE, INBRED C57BL; PROPIONATES; RECEPTORS, G-PROTEIN-COUPLED; RNA INTERFERENCE; SIGNAL TRANSDUCTION;

MLCS; MLOWN;

EID: 84877272337     PISSN: 01931849     EISSN: 15221555     Source Type: Journal    
DOI: 10.1152/ajpendo.00419.2012     Document Type: Article

References (33)

1. Agius L. Glucokinase and molecular aspects of liver glycogen metabolism. Biochem J 414: 1-18, 2008.
2. Araki T, Hirayama M, Hiroi S, Kaku K. GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Diabetes Obes Metab 14: 271-278, 2012.
3. Binkert C, Demetriou M, Sukhu B, Szweras M, Tenenbaum HC, Dennis JW. Regulation of osteogenesis by fetuin. J Biol Chem 274: 28514-28520, 1999.
4. Briscoe CP, Peat AJ, McKeown SC, Corbett DF, Goetz AS, Littleton TR, McCoy DC, Kenakin TP, Andrews JL, Ammala C, Fornwald JA, Ignar DM, Jenkinson S. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol 148: 619-628, 2006.
5. Briscoe CP, Tadayyon M, Andrews JL, Benson WG, Chambers JK, Eilert MM, Ellis C, Elshourbagy NA, Goetz AS, Minnick DT, Murdock PR, Sauls HR Jr, Shabon U, Spinage LD, Strum JC, Szekeres PG, Tan KB, Way JM, Ignar DM, Wilson S, Muir AI. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 278: 11303-11311, 2003.
6. Burant CF, Viswanathan P, Marcinak J, Cao C, Vakilynejad M, Xie B, Leifke E. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet 379: 1403-1411, 2012.
7. Cintron VJ, Ko MS, Chi KD, Gross JP, Srinivas PR, Goustin AS, Grunberger G. Genetic mapping and functional studies of a natural inhibitor of the insulin receptor tyrosine kinase: the mouse ortholog of human alpha2-HS glycoprotein. Int J Exp Diabetes Res 1: 249-263, 2001.
8. Dasgupta S, Bhattacharya S, Biswas A, Majumdar SS, Mukhopadhyay S, Ray S, Bhattacharya S. NF-kappaB mediates lipid-induced fetuin-A expression in hepatocytes that impairs adipocyte function effecting insulin resistance. Biochem J 429: 451-462, 2010.
9. Edfalk S, Steneberg P, Edlund H. Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion. Diabetes 57: 2280-2287, 2008.
10. Gehrmann W, Elsner M, Lenzen S. Role of metabolically generated reactive oxygen species for lipotoxicity in pancreatic beta-cells. Diabetes Obes Metab 12, Suppl 2: 149-158, 2010.
11. Grimes CA, Jope RS. The multifaceted roles of glycogen synthase kinase 3beta in cellular signaling. Prog Neruobiol 65: 391-426, 2001.
12. Hara T, Hirasawa A, Ichimura A, Kimura I, Tsujimoto G. Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders. J Pharm Sci 100: 3594-3601, 2011.
13. Itoh Y, Kawamata Y, Harada M, Kobayashi M, Fujii R, Fukusumi S, Ogi K, Hosoya M, Tanaka Y, Uejima H, Tanaka H, Maruyama M, Satoh R, Okubo S, Kizawa H, Komatsu H, Matsumura F, Noguchi Y, Shinohara T, Hinuma S, Fujisawa Y, Fujino M. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 422: 173-176, 2003.
14. Kamei N, Tobe K, Suzuki R, Ohsugi M, Watanabe T, Kubota N, Ohtsuka-Kowatari N, Kumagai K, Sakamoto K, Kobayashi M, Yamauchi T, Ueki K, Oishi Y, Nishimura S, Manabe I, Hashimoto H, Ohnishi Y, Ogata H, Tokuyama K, Tsunoda M, Ide T, Murakami K, Nagai R, Kadowaki T. Overexpression of monocyte chemoattractant protein-1 in adipose tissues causes macrophage recruitment and insulin resistance. J Biol Chem 281: 26602-26614, 2006.
15. Le Floch JP, Escuyer P, Baudin E, Baudon D, Perlemuter L. Blood glucose area under the curve. Methodological aspects. Diabetes Care 13: 172-175, 1990.
16. Liu XJ, He AB, Chang YS, Fang FD. Atypical protein kinase C in glucose metabolism. Cell Signal 18: 2071-2076, 2006.
17. Mathews ST, Singh GP, Ranalletta M, Cintron VJ, Qiang X, Goustin AS, Jen KL, Charron MJ, Jahnen-Dechent W, Grunberger G. Improved insulin sensitivity and resistance to weight gain in mice null for the Ahsg gene. Diabetes 51: 2450-2458, 2002.
18. Ou HY, Wu HT, Hung HC, Yang YC, Wu JS, Chang CJ. Endoplasmic reticulum stress induces the expression of fetuin-a to develop insulin resistance. Endocrinology 153: 2974-2984, 2012.
19. Ou HY, Yang YC, Wu HT, Wu JS, Lu FH, Chang CJ. Increased fetuin-A concentrations in impaired glucose tolerance with or without nonalcoholic fatty liver disease, but not impaired fasting glucose. J Clin Endocrinol Metab 97: 4717-4723, 2012.
20. Ou HY, Yang YC, Wu HT, Wu JS, Lu FH, Chang CJ. Serum fetuin-A concentrations are elevated in subjects with impaired glucose tolerance and newly diagnosed type 2 diabetes. Clin Endocrinol (Oxf) 75: 450-455, 2011.
21. Rauth G, Pöschke O, Fink E, Eulitz M, Tippmer S, Kellerer M, Häring HU, Nawratil P, Haasemann M, Jahnen-Dechent W, Müller-Ester W. The nucleotide and partial amino acid sequences of rat fetuin. identity with the natural tyrosine kinase inhibitor of the rat insulin receptor. Eur J Biochem 204: 523-529, 1992.
22. Ricchi M, Odoardi MR, Carulli L, Anzivino C, Ballestri S, Pinetti A, Fantoni LI, Marra F, Bertolotti M, Banni S, Lonardo A, Carulli N, Loria P. Differential effect of oleic and palmitic acid on lipid accumulation and apoptosis in cultured hepatocytes. J Gastroenterol Hepatol 24: 830-840, 2009.
23. Salehi A, Flodgren E, Nilsson NE, Jimenez-Feltstrom J, Miyazaki J, Owman C, Olde B. Free fatty acid receptor 1 [FFA(1)R/GPR40] and its involvement in fatty-acid-stimulated insulin secretion. Cell Tissue Res 322: 207-215, 2005.
24. Saltiel AR, Kahn CR. Insulin signalling and the regulation of glucose and lipid metabolism. Nature 414: 799-806, 2001.
25. Srinivas PR, Wagner AS, Reddy LV, Deutsch DD, Leon MA, Goustin AS, Grunberger G. Serum alpha 2-HS-glycoprotein is an inhibitor of the human insulin receptor at the tyrosine kinase level. Mol Endocrinol 7: 1445-1455, 1993.
26. Stefan N, Hennige AM, Staiger H, Machann J, Schick F, Kröber SM, Machicao F, Fritsche A, Häring HU. Alpha2-Heremans-Schmid glycoprotein/ fetuin-A is associated with insulin resistance and fat accumulation in the liver in humans. Diabetes Care 29: 853-857, 2006.
27. Suh HN, Huong HT, Song CH, Lee JH, Han HJ. Linoleic acid stimulates gluconeogenesis via Ca2+/PLC, cPLA2, and PPAR pathways through GPR40 in primary cultured chicken hepatocytes. Am J Physiol Cell Physiol 295: C1518-C1527, 2008.
28. Toroian D, Price PA. The essential role of fetuin in the serum-induced calcification of collagen. Calcif Tissue Int 82: 116-126, 2008.
29. Wu HT, Chen CT, Cheng KC, Li YX, Yeh CH, Cheng JT. Pharmacological activation of peroxisome proliferator-activated receptor delta improves insulin resistance and hepatic steatosis in high fat diet-induced diabetic mice. Horm Metab Res 43: 631-635, 2011.
30. Wu HT, Chen W, Cheng KC, Ku PM, Yeh CH, Cheng JT. Oleic acid activates peroxisome proliferator-activated receptor to compensate insulin resistance in steatotic cells. J Nutr Biochem 23: 1264-1270, 2011.
31. Yang M, Chisholm JW, Soelaiman S, Shryock JC. Sulfonylureas uncouple glucose-dependence for GPR40-mediated enhancement of insulin secretion from INS-1E cells. Mol Cell Endocrinol 315: 308-313, 2010.
32. Zhang X, Yan G, Li Y, Zhu W, Wang H. DC260126, a small-molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats. Biomed Pharmacother 64: 647-651, 2010.
33. Zhang Y, Lee FY, Barrera G, Lee H, Vales C, Gonzalez FJ, Willson TM, Edwards PA. Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc Natl Acad Sci USA 103: 1006-1011, 2006.