Famotidine inhibits glycogen synthase kinase-3β: an investigation by docking simulation and experimental validation.

作者: Mohammad Mohammad , Ihab M Al-Masri , Ala Issa , Mohamed AS Al-Ghussein , Mohammad Fararjeh

DOI: 10.3109/14756366.2012.672413

关键词:

摘要: Famotidine was investigated as an inhibitor of glycogen synthase kinase-3β (GSK-3β) in attempt to explain the molecular mechanism its hypoglycemic side effects. The investigation included simulated docking experiments, vitro enzyme inhibition assay, sparing studies using animal models and single dose oral glucose tolerance test (OGTT). Docking showed how famotidine is optimally fit within binding pocket GSK-3β via numerous attractive interactions with some specific amino acids. Experimentally, could inhibit (IC50 = 1.44 μM) increased significantly liver spares fasting models. Moreover, a shown decrease glycemic response curve after 75 g OGTT

参考文章(14)
G Støa-Birketvedt, PN Paus, R Ganss, OC Ingebretsen, J Florholmen, Cimetidine reduces weight and improves metabolic control in overweight patients with Type 2 diabetes International Journal of Obesity. ,vol. 22, pp. 1041- 1045 ,(1998) , 10.1038/SJ.IJO.0800721
Ana Martinez, Mercedes Alonso, Ana Castro, Concepción Pérez, Francisco J. Moreno, First Non-ATP Competitive Glycogen Synthase Kinase 3 β (GSK-3β) Inhibitors: Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer's Disease Journal of Medicinal Chemistry. ,vol. 45, pp. 1292- 1299 ,(2002) , 10.1021/JM011020U
Yasser Bustanji, Mutasem O Taha, Ihab M Almasri, Mohamed AS Al-Ghussein, Mohammad K Mohammad, Hatim S Alkhatib, None, Inhibition of glycogen synthase kinase by curcumin: Investigation by simulated molecular docking and subsequent in vitro/in vivo evaluation. Journal of Enzyme Inhibition and Medicinal Chemistry. ,vol. 24, pp. 771- 778 ,(2009) , 10.1080/14756360802364377
C. Scarpignato, F. Tirelli, R. Starcich, G. Bertaccini, Effect of acute and chronic cimetidine administration on glucose tolerance and insulin secretion in man. Hormone Research in Paediatrics. ,vol. 15, pp. 228- 236 ,(1981) , 10.1159/000179461
Mutasem O. Taha, Yasser Bustanji, Mohamed A. S. Al-Ghussein, Mohammad Mohammad, Hiba Zalloum, Ihab M. Al-Masri, Naji Atallah, Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin Journal of Medicinal Chemistry. ,vol. 51, pp. 2062- 2077 ,(2008) , 10.1021/JM7009765
Sandro Gentile, Riccardo Marmo, Andrea Costume, Cosimo Orlando, Rita D’Alessandro, Giuseppe Bellis, Mario Porcellini, Mario Coltorti, The role of ranitidine infusion on glucose, insulin and C-peptide serum levels induced by oral glucose tolerance test in healthy subjects. Acta Diabetologica. ,vol. 23, pp. 165- 170 ,(1986) , 10.1007/BF02624676
Mohammad K Mohammad, Ihab M Al-Masri, Mutasem O Taha, Mohamed AS Al-Ghussein, Hatim S AlKhatib, Samer Najjar, Yasser Bustanji, None, Olanzapine inhibits glycogen synthase kinase-3β: An investigation by docking simulation and experimental validation European Journal of Pharmacology. ,vol. 584, pp. 185- 191 ,(2008) , 10.1016/J.EJPHAR.2008.01.019
Kathy E Fit, Patrick C Williams, None, Use of Histamine2-Antagonists for the Treatment of Verruca Vulgaris Annals of Pharmacotherapy. ,vol. 41, pp. 1222- 1226 ,(2007) , 10.1345/APH.1H616
W. A. STUBBS, G. DELITALA, G. M. BESSER, C. R. W. EDWARDS, S. LABROOY, R. TAYLOR, J. J. MISIEWICZ, K. G. M. M. ALBERTI, THE ENDOCRINE AND METABOLIC EFFECTS OF CIMETIDINE Clinical Endocrinology. ,vol. 18, pp. 167- 178 ,(1983) , 10.1111/J.1365-2265.1983.TB03199.X