Olanzapine inhibits glycogen synthase kinase-3β: An investigation by docking simulation and experimental validation
作者： Mohammad K Mohammad , Ihab M Al-Masri , Mutasem O Taha , Mohamed AS Al-Ghussein , Hatim S AlKhatib
DOI: 10.1016/J.EJPHAR.2008.01.019
关键词: Atypical antipsychotic 、 GSK-3 、 Glycogen 、 Olanzapine 、 Thienobenzodiazepine 、 Glycogen synthase 、 Endocrinology 、 GSK3B 、 Internal medicine 、 In vivo 、 Chemistry 、 Pharmacology
摘要: Olanzapine was investigated as an inhibitor of glycogen synthase kinase-3beta (GSK-3beta) in attempt to evaluate its effect on blood glucose level. The investigation included simulated docking experiments fit olanzapine within the binding pocket GSK-3beta followed by vitro enzyme inhibition assay well vivo subchronic animal treatment. found readily a low energy orientation characterized with optimal attractive interactions bridging tricyclic thienobenzodiazepine nitrogen and sulfur atoms residue VAL-135 GSK-3beta. In showed significant decrease fasting level Balb/c mice at 1.0, 2.0 3.0 mg/kg dose levels (P<0.05) 6 fold increase liver 3 (P<0.001). Moreover; potently inhibit recombinant (IC(50) value=91.0 nM). Our findings strongly suggest that has activity could justify some pharmacological effects metabolic disturbances.
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