Naproxen and cromolyn as new glycogen synthase kinase 3β inhibitors for amelioration of diabetes and obesity: An investigation by docking simulation and subsequent in vitro/in vivo biochemical evaluation

Journal of Biochemical and Molecular Toxicology

Volumn 27, Issue 9, 2013, Pages 425-436

  Motawi, Tarek M K ^a   Bustanji, Yasser ^b   El Maraghy, Shohda A ^a   Taha, Mutasem O ^b   Al Ghussein, Mohamed A S ^c  

^a CAIRO UNIVERSITY   (Egypt)

^b UNIVERSITY OF JORDAN   (Jordan)

^c AL AZHAR UNIVERSITY   (Palestine)

Author keywords

Cromolyn; Docking simulation; Glycogen; Glycogen synthase kinase 3 ; Naproxen; Resistin

Indexed keywords

ADIPONECTIN; C PEPTIDE; CROMOGLYCATE DISODIUM; GLUCOSE; GLYCOGEN; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; GLYCOGEN SYNTHASE KINASE 3BETA; INSULIN; NAPROXEN; RESISTIN; GLYCOGEN SYNTHASE KINASE 3; GLYCOGEN SYNTHASE KINASE 3 BETA; PROTEIN BINDING;

ARTICLE; BODY WEIGHT; DRUG PROTEIN BINDING; ENZYME INHIBITION; ENZYME LINKED IMMUNOSORBENT ASSAY; GLUCOSE BLOOD LEVEL; GLYCOGEN ANALYSIS; IN VITRO STUDY; IN VIVO STUDY; INSULIN BLOOD LEVEL; MOLECULAR DOCKING; NON INSULIN DEPENDENT DIABETES MELLITUS; OBESITY; PROTEIN BLOOD LEVEL; WEIGHT REDUCTION; ANIMAL; ANTAGONISTS AND INHIBITORS; BINDING SITE; CHEMISTRY; DIABETES MELLITUS; ENZYMOLOGY; HUMAN; MOUSE; PROTEIN CONFORMATION;

ANIMALIA; MUS;

ANIMALS; BINDING SITES; CROMOLYN SODIUM; DIABETES MELLITUS; GLYCOGEN SYNTHASE KINASE 3; HUMANS; MICE; MOLECULAR DOCKING SIMULATION; NAPROXEN; OBESITY; PROTEIN BINDING; PROTEIN CONFORMATION;

EID: 84883450764     PISSN: 10956670     EISSN: 10990461     Source Type: Journal    
DOI: 10.1002/jbt.21503     Document Type: Article

References (37)

1. Lichtenberger LM, Romero JJ, Dial EJ, Moore JE. Naproxen-PC: A GI safe and highly effective anti-inflammatory. Inflammopharmacology 2008;16:1-5.
2. Foreman JC, Haliett MB, Mongar JL. Site of action of the anti-allergic drugs cromoglycate and doxantrazole. Br J Pharmacol 1981;11:473-3610.
3. Whiting B, Williams RL, Lorenzi M, Varady JC, Robins DS. Effect of naproxen on glucose metabolism and tolbutamide kinetics and dynamics in maturity onset diabetics. Br J Clin Pharmacol 1981;11:295-302.
4. Wang J, Shi G-P. Mast cell stabilization: novel medication for obesity and diabetes. Diabetes Metab Res Rev 2011;27(8):919-924.
5. Srinivas S, Feldman D. A phase II trial of calcitriol and naproxen in recurrent prostate cancer. Anticancer Res 2009;29:3605-3610.
6. Arumugam T, Ramachandran V, Logsdon CD. Effect of cromolyn on S100P interactions with RAGE and pancreatic cancer growth and invasion in mouse models. J Natl Canc Inst 2006;98:1806-1818.
7. Ali A, Hoeflich KP, Woodgett JR. Glycogen synthase kinase-3: properties, functions, and regulation. Chem Rev 2001;101:2527-2540.
8. Frame S, Cohen P. GSK3 takes centre stage more than 20 years after its discovery. Biochem J 2001;359:1-16.
9. Saltiel AR. New perspectives into the molecular pathogenesis and treatment of type 2 diabetes. Cell 2001;104:517-529.
10. Bullock WH, Magnuson SR, Choi S, Gunn DE, Rudolph J. Prospects for kinase activity modulators in the treatment of diabetes and diabetic complications. Curr Top Med Chem 2002;2:915-938.
11. Nikoulina SE, Ciaraldi TP, Mudaliar S, Mohideen P, Carter L, Henry RR. Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes. Diabetes 2000;49:263-271.
12. Tang QQ, Gronborg M, Huang H, Kim JW, Otto TC, Pandey A, Lane MD. Sequential phosphorylation of CCAAT enhancer-binding protein beta by MAPK and glycogen synthase kinase 3beta is required for adipogenesis. Proc Natl Acad Sci USA 2005;102:9766-9771.
13. Shakoori A, Ougolkov A, Yu ZW, Zhang B, Modarressi MH, Billadeau DD, Mai M, Takahashi Y, Minamoto T. Deregulated GSK3 beta activity in colorectal cancer: its association with tumor cell survival and proliferation. Biochem Biophys Res Commun 2005;334:1365-1373.
14. Wulfkuhle JD, Aquino JA, Calvert VS, Fishman DA, Coukos G, Liotta LA, Petricoin III EF. Signal pathway profiling of ovarian cancer from human tissue specimens using reverse-phase protein microarrays. Proteomics 2003;3:2085-2090.
15. Liao X, Thrasher JB, Holzbeierlein J, Stanley S, Benyili. Glycogen synthase kinase-3 activity is required for androgen-stimulated gene expression in prostate cancer. Endocrinology 2004;145(6):2941-2949.
16. Eldar-Finkelman H. Glycogen synthase kinase 3: an emerging therapeutic target. Trends Mol Med 2002;8:126-132.
17. Meijer L, Flajolet, M, Greengard P. Pharmacological inhibitors of glycogen synthase kinase 3. Trends Pharmacol Sci 2004;25:471-480.
18. Wagman AS, Johnson KW, Bussiere DE. Discovery and development of GSK3 inhibitors for the treatment of type 2 diabetes. Curr Pharm Des 2004;10:1105-1137.
19. Dokken BB, Sloniger JA, Henriksen EJ. Acute selective glycogen synthase kinase-3 inhibition enhances insulin signaling in prediabetic insulin-resistant rat skeletal muscle. Am J Physiol Endocrinol Metab 2005;288:E1188-E1194.
20. Taha MO, Bustanji Y, Al-Ghussein MA, Mohammad M, Zalloum H, Al-Masri IM. Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin. J Med Chem 2008;51:2062-2077.
21. Bustanji Y, Taha MO, Almasri IM, Al Ghussein MA, Mohammad MK, Alkhatib HS. Inhibition of glycogen synthase kinase by curcumin: Investigation by simulated molecular docking and subsequent in vitro/in vivo evaluation. J Enzyme Inhib Med Chem 2009;24:771-778.
22. Mohammad MK, Al-Masri IM, Taha MO, Al-Ghussein MA, Alkhatib HS, Najjar S, Bustanji Y. Olanzapine inhibits glycogen synthase kinase-3beta: an investigation by docking simulation and experimental validation. Eur J Pharmacol 2008;584:185-191.
23. Bhat R, Xue Y, Berg S, Hellberg S, Ormö M, Nilsson Y. Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem 2003;278:45937-45945.
24. Taha MO, Habash M, Al-Hadidi Z, Al-Bakri A, Younis K, Sisan S. Docking-Based comparative intermolecular Contacts Analysis as New 3-D QSAR concept for validating docking studies and in silico screening: NMT and GP inhibitors as case studies. J Chem Inf Model 2011;51:647-669.
25. Martinez A, Alonso M, Castro A, Pérez C, Moreno FJ. First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. J Med Chem 2002;45:1292-1299.
26. Carroll NV, Longley RW, Roe JH. The determination of glycogen in liver and muscle by use of anthrone reagent. J Biol Chem 1956;220:583-593.
27. Nowicki MT, Aleksunes LM, Sawant SP, Dnyanmote AV, Mehendale HM, Manautou JM. Renal and hepatic transporter expression in type 2 diabetic rats. Drug Metab Lett 2008;2:11-17.
28. Frier BM, Ashby JP, Narin IM, Baris JD. Plasma insulin, C-peptide and glucagon concentrations in patients with insulin independent diabetes treated with chlorpropamide. Diabete Metab 1981;7(1):45-49.
29. Meijer L, Flajolet M, Greengard P. Pharmacological inhibitors of glycogen synthase kinase 3. Trends Pharmacol Sci 2004;25:471-480.
30. Morfini G, Szebenyi G, Elluru R, Ratner N, Brady ST. Glycogen synthase kinase 3 phosphorylates kinesin light chains and negatively regulates kinesin-based motility. EMBO J 2002;21:281-293.
31. Emoto M, Langille SE, Czech MP. A role for kinesin in insulin stimulated GLUT4 glucose transporter translocation in 3T3-L1 adipocytes. J Biol Chem 2001;276:10677-10682.
32. Welsh GI, Proud CG. Glycogen synthase kinase-3 is rapidly inactivated in response to insulin and phosphorylates eukaryotic initiation factor eIF-2B. Biochem J 1993;94(Part 3):625-629.
33. Moule SK, Welsh GI, Edgell NJ, Foulstone EJ, Proud CG, Denton RM. Regulation of protein kinase B and glycogen synthase kinase-3 by insulin and beta-adrenergic agonists in rat epididymal fat cells: activation of protein kinase B by wortmannin-sensitive and -insensitive mechanisms. J Biol Chem 1997;272:7713-7719.
34. Summers SA, Kao AW, Kohn AD, Backus GS, Roth RA, Pessin JE, Birnbaum MJ. The role of glycogen synthase kinase 3beta in insulin-stimulated glucose metabolism. J Biol Chem 1999;274:17934-17940.
35. Tang QQ, Gronborg M, Huang H, Kim JW, Otto TC, Pandey A, Lane MD. Sequential phosphorylation of CCAAT enhancer-binding protein beta by MAPK and glycogen synthase kinase 3beta is required for adipogenesis. Proc Natl Acad Sci USA 2005;102:9766-9771.
36. Kusminski MC, McTernan PG, Kumar S. Role of resistin in obesity, insulin resistance and type II diabetes. Clin Sci (Lond) 2005;109:243-256.
37. Fasshauer M, Paschke R, Stumvoll M. Adiponectin, obesity, and cardiovascular disease. Biochimie 2004;86:779-784.