Anti-obesity effects of 3-hydroxychromone derivative, a novel small-molecule inhibitor of glycogen synthase kinase-3

Biochemical Pharmacology

Volumn 85, Issue 7, 2013, Pages 965-976

  Lee, Sooho ^a   Yang, Woo Kyeom ^a   Song, Ji Ho ^b   Ra, Young Min ^b   Jeong, Jin Hyun ^b,c   Choe, Wonchae ^a   Kang, Insug ^a   Kim, Sung Soo ^a   Ha, Joohun ^a  

^a Kyung Hee University Hospital   (South Korea)

^b Kyung Hee University   (South Korea)

^c Yonsei University   (South Korea)

Author keywords

GSK 3; Lipid metabolism; Obesity; Protein kinase inhibitor

Indexed keywords

2 (3 CHLORO 4 HYDROXYANILINO) 3 (2 NITROPHENYL)MALEIMIDE; 3 HYDROXYCHROMONE DERIVATIVE; ANTIOBESITY AGENT; BETA CATENIN; CHROMONE DERIVATIVE; GLYCOGEN SYNTHASE; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; GLYCOGEN SYNTHASE KINASE 3BETA; LITHIUM CHLORIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CELL DIFFERENTIATION; CELL STRAIN 3T3; CELL STRAIN HEK293; CELL STRAIN HEPG2; CONTROLLED STUDY; DOWN REGULATION; DRUG POTENCY; DRUG SCREENING; DYSLIPIDEMIA; EMBRYO; ENZYME INACTIVATION; ENZYME INHIBITION; FATTY LIVER; GENE EXPRESSION REGULATION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIPID METABOLISM; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROADIPOCYTE; PROTEIN STABILITY; UPREGULATION; WEIGHT GAIN;

3T3-L1 CELLS; ADIPOCYTES; ADIPOGENESIS; ADIPOSITY; AMINOPHENOLS; ANIMALS; ANTI-OBESITY AGENTS; BETA CATENIN; BODY WEIGHT; CELL DIFFERENTIATION; CHROMONES; GLYCOGEN SYNTHASE KINASE 3; HEK293 CELLS; HEP G2 CELLS; HUMANS; LIPID METABOLISM; LITHIUM CHLORIDE; MALE; MALEIMIDES; MICE; MICE, INBRED C57BL; OBESITY; PROTEIN STABILITY; THIAZOLES;

EID: 84874654896     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2012.12.023     Document Type: Article

References (46)

1. C. Canto, and J. Auwerx PGC-1alpha, SIRT1 and AMPK, an energy sensing network that controls energy expenditure Curr Opin Lipidol 20 2009 98 105
2. M.J. Khandekar, P. Cohen, and B.M. Spiegelman Molecular mechanisms of cancer development in obesity Nat Rev Cancer 11 2011 886 895
3. Y. Cao Adipose tissue angiogenesis as a therapeutic target for obesity and metabolic diseases Nat Rev Drug Discov 9 2010 107 115
4. P.J. Havel Control of energy homeostasis and insulin action by adipocyte hormones: leptin, acylation stimulating protein, and adiponectin Curr Opin Lipidol 13 2002 51 59 (Pubitemid 34174629)
5. B.M. Spiegelman, and J.S. Flier Obesity and the regulation of energy balance Cell 104 2001 531 543 (Pubitemid 32201948)
6. N. Ouchi, J.L. Parker, J.J. Lugus, and K. Walsh Adipokines in inflammation and metabolic disease Nat Rev Immunol 11 2011 85 97
7. J.P. Despres, and I. Lemieux Abdominal obesity and metabolic syndrome Nature 444 2006 881 887 (Pubitemid 46024995)
8. H. Eldar-Finkelman Glycogen synthase kinase 3: an emerging therapeutic target Trends Mol Med 8 2002 126 132 (Pubitemid 34532638)
9. J. Manchester, A.V. Skurat, P. Roach, S.D. Hauschka, and J.C. Lawrence Jr. Increased glycogen accumulation in transgenic mice overexpressing glycogen synthase in skeletal muscle Proc Natl Acad Sci USA 93 1996 10707 10711
10. E.E. Benarroch Glycogen metabolism: metabolic coupling between astrocytes and neurons Neurology 74 2010 919 923
11. P. Cohen, and S. Frame The renaissance of GSK3 Nat Rev Mol Cell Biol 2 2001 769 776 (Pubitemid 33679839)
12. L. Meijer, M. Flajolet, and P. Greengard Pharmacological inhibitors of glycogen synthase kinase 3 Trends Pharmacol Sci 25 2004 471 480 (Pubitemid 39149703)
13. G.V. Rayasam, V.K. Tulasi, R. Sodhi, J.A. Davis, and A. Ray Glycogen synthase kinase 3: more than a namesake Br J Pharmacol 156 2009 885 898
14. L.K. Chico, L.J. Van Eldik, and D.M. Watterson Targeting protein kinases in central nervous system disorders Nat Rev Drug Discov 8 2009 892 909
15. A. Wada GSK-3 inhibitors and insulin receptor signaling in health, disease, and therapeutics Front Biosci 14 2009 1558 1570
16. J. Bain, H. McLauchlan, M. Elliott, and P. Cohen The specificities of protein kinase inhibitors: an update Biochem J 371 2003 199 204 (Pubitemid 36458094)
17. S.P. Davies, H. Reddy, M. Caivano, and P. Cohen Specificity and mechanism of action of some commonly used protein kinase inhibitors Biochem J 351 2000 95 105
18. A. Martinez Preclinical efficacy on GSK-3 inhibitors: towards a future generation of powerful drugs Med Res Rev 28 2008 773 796
19. J.B. Kim, and B.M. Spiegelman ADD1/SREBP1 promotes adipocyte differentiation and gene expression linked to fatty acid metabolism Genes Dev 10 1996 1096 1107 (Pubitemid 26152851)
20. M.P. Coghlan, A.A. Culbert, D.A. Cross, S.L. Corcoran, J.W. Yates, and N.J. Pearce Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription Chem Biol 7 2000 793 803
21. F. Zhang, C.J. Phiel, L. Spece, N. Gurvich, and P.S. Klein Inhibitory phosphorylation of glycogen synthase kinase-3 (GSK-3) in response to lithium. Evidence for autoregulation of GSK-3 J Biol Chem 278 2003 33067 33077 (Pubitemid 37055753)
22. N. Horike, H. Sakoda, A. Kushiyama, H. Ono, M. Fujishiro, and H. Kamata AMP-activated protein kinase activation increases phosphorylation of glycogen synthase kinase 3beta and thereby reduces cAMP-responsive element transcriptional activity and phosphoenolpyruvate carboxykinase C gene expression in the liver J Biol Chem 283 2008 33902 33910
23. S.L. Longnus, C. Segalen, J. Giudicelli, M.P. Sajan, R.V. Farese, and E. Van Obberghen Insulin signalling downstream of protein kinase B is potentiated by 5′AMP-activated protein kinase in rat hearts in vivo Diabetologia 48 2005 2591 2601 (Pubitemid 41738227)
24. L.E. Zaragosi, B. Wdziekonski, C. Fontaine, P. Villageois, P. Peraldi, and C. Dani Effects of GSK3 inhibitors on in vitro expansion and differentiation of human adipose-derived stem cells into adipocytes BMC Cell Biol 9 2008 11
25. S.E. Ross, N. Hemati, K.A. Longo, C.N. Bennett, P.C. Lucas, and R.L. Erickson Inhibition of adipogenesis by Wnt signaling Science 289 2000 950 953 (Pubitemid 30659947)
26. B. Sen, Z. Xie, N. Case, M. Ma, C. Rubin, and J. Rubin Mechanical strain inhibits adipogenesis in mesenchymal stem cells by stimulating a durable beta-catenin signal Endocrinology 149 2008 6065 6075
27. N. Sato, L. Meijer, L. Skaltsounis, P. Greengard, and A.H. Brivanlou Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor Nat Med 10 2004 55 63 (Pubitemid 38524699)
28. J. Liu, and S.R. Farmer Regulating the balance between peroxisome proliferator-activated receptor gamma and beta-catenin signaling during adipogenesis. A glycogen synthase kinase 3beta phosphorylation-defective mutant of beta-catenin inhibits expression of a subset of adipogenic genes J Biol Chem 279 2004 45020 45027 (Pubitemid 39430916)
29. R.T. Moon, A.D. Kohn, G.V. De Ferrari, and A. Kaykas WNT and beta-catenin signalling: diseases and therapies Nat Rev Genet 5 2004 691 701 (Pubitemid 39150127)
30. A.G. Powell, C.M. Apovian, and L.J. Aronne New drug targets for the treatment of obesity Clin Pharmacol Ther 90 2011 40 51
31. E.D. Rosen, and B.M. Spiegelman Molecular regulation of adipogenesis Annu Rev Cell Dev Biol 16 2000 145 171 (Pubitemid 32037503)
32. E.D. Rosen, C.H. Hsu, X. Wang, S. Sakai, M.W. Freeman, and F.J. Gonzalez C/EBPalpha induces adipogenesis through PPARgamma: a unified pathway Genes Dev 16 2002 22 26 (Pubitemid 34049634)
33. J. Liu, H. Wang, Y. Zuo, and S.R. Farmer Functional interaction between peroxisome proliferator-activated receptor gamma and beta-catenin Mol Cell Biol 26 2006 5827 5837 (Pubitemid 44134337)
34. K. MacAulay, A.S. Blair, E. Hajduch, T. Terashima, O. Baba, and C. Sutherland Constitutive activation of GSK3 down-regulates glycogen synthase abundance and glycogen deposition in rat skeletal muscle cells J Biol Chem 280 2005 9509 9518 (Pubitemid 40409646)
35. M.J. Brady, A.C. Nairn, and A.R. Saltiel The regulation of glycogen synthase by protein phosphatase 1 in 3T3-L1 adipocytes. Evidence for a potential role for DARPP-32 in insulin action J Biol Chem 272 1997 29698 29703
36. S. Mandard, R. Stienstra, P. Escher, N.S. Tan, I. Kim, and F.J. Gonzalez Glycogen synthase 2 is a novel target gene of peroxisome proliferator-activated receptors Cell Mol Life Sci 64 2007 1145 1157 (Pubitemid 46684553)
37. T.P. Ciaraldi, D.K. Oh, L. Christiansen, S.E. Nikoulina, A.P. Kong, and S. Baxi Tissue-specific expression and regulation of GSK-3 in human skeletal muscle and adipose tissue Am J Physiol Endocrinol Metab 291 2006 E891 E898
38. B.B. Dokken, J.A. Sloniger, and E.J. Henriksen Acute selective glycogen synthase kinase-3 inhibition enhances insulin signaling in prediabetic insulin-resistant rat skeletal muscle Am J Physiol Endocrinol Metab 288 2005 E1188 E1194
39. K. MacAulay, E. Hajduch, A.S. Blair, M.P. Coghlan, S.A. Smith, and H.S. Hundal Use of lithium and SB-415286 to explore the role of glycogen synthase kinase-3 in the regulation of glucose transport and glycogen synthase Eur J Biochem 270 2003 3829 3838 (Pubitemid 37123255)
40. S.E. Nikoulina, T.P. Ciaraldi, S. Mudaliar, L. Carter, K. Johnson, and R.R. Henry Inhibition of glycogen synthase kinase 3 improves insulin action and glucose metabolism in human skeletal muscle Diabetes 51 2002 2190 2198 (Pubitemid 34729024)
41. D.B. Ring, K.W. Johnson, E.J. Henriksen, J.M. Nuss, D. Goff, and T.R. Kinnick Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo Diabetes 52 2003 588 595 (Pubitemid 36323563)
42. M. Collino, M. Aragno, S. Castiglia, C. Tomasinelli, C. Thiemermann, and G. Boccuzzi Insulin reduces cerebral ischemia/reperfusion injury in the hippocampus of diabetic rats: a role for glycogen synthase kinase-3beta Diabetes 58 2009 235 242
43. Y.X. Wang PPARs: diverse regulators in energy metabolism and metabolic diseases Cell Res 20 2010 124 137
44. O. Kaidanovich-Beilin, and H. Eldar-Finkelman Long-term treatment with novel glycogen synthase kinase-3 inhibitor improves glucose homeostasis in ob/ob mice: molecular characterization in liver and muscle J Pharmacol Exp Ther 316 2006 17 24 (Pubitemid 41832576)
45. B.B. Dokken, and E.J. Henriksen Chronic selective glycogen synthase kinase-3 inhibition enhances glucose disposal and muscle insulin action in prediabetic obese Zucker rats Am J Physiol Endocrinol Metab 291 2006 E207 E213
46. S.E. Choi, H.J. Jang, Y. Kang, J.G. Jung, S.J. Han, and H.J. Kim Atherosclerosis induced by a high-fat diet is alleviated by lithium chloride via reduction of VCAM expression in ApoE-deficient mice Vascul Pharmacol 53 2010 264 272