Virtual Screening and Testing of GSK-3 Inhibitors Using Human SH-SY5Y Cells Expressing Tau Folding Reporter and Mouse Hippocampal Primary Culture under Tau Cytotoxicity
Chih‐Hsin Lin, Yu-Shao Hsieh, Ying‐Chieh Sun, Wun‐Han Huang, Shu‐Ling Chen, Zheng-Kui Weng, Te‐Hsien Lin, Yih‐Ru Wu, Kuo‐Hsuan Chang, Hei‐Jen Huang, Guan‐Chiun Lee, Hsiu Mei Hsieh‐Li, Guey‐Jen Lee‐Chen
Abstract
. In addition, VB-030 and VB-037 further improved neuronal survival and/or neurite length and branch in mouse hippocampal primary culture under Tau cytotoxicity. Overall, through inhibiting GSK-3β kinase activity and/or p-P38 (Thr180/Tyr182), both compounds may serve as promising candidates to reduce Tau aggregation/cytotoxicity for AD treatment.
Topics & Concepts
CytotoxicityMolecular biologyHippocampal formationSH-SY5YChemistryCell cultureMedicineBiologyBiochemistryGeneticsIn vitroInternal medicineNeuroblastomaNuclear Receptors and SignalingComputational Drug Discovery Methods14-3-3 protein interactions