S-trityl-L-cysteine, a novel Eg5 inhibitor, is a potent chemotherapeutic strategy in neuroblastoma

S-三苯甲基-L-半胱氨酸是一种新型 Eg5 抑制剂,是神经母细胞瘤的有效化疗策略

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作者:Wei Wu, Shao Jingbo, Weijue Xu, Jiangbin Liu, Yiming Huang, Qingfeng Sheng, Zhibao Lv

Abstract

Eg5 is a member of the kinesin-5 family. It is involved in the formation of the bipolar spindle and serves a crucial role in mitosis; meaning that mitotic activation may serve as a chemotherapeutic strategy. However, the anticancer activity of Eg5 inhibitors in neuroblastoma remains uncharacterized. In the present study, the expression of Eg5 was examined in clinical tissue samples and neuroblastoma cell lines, SK-N-SH, SH-SY5Y and SK-N-BE2. Additionally, the antitumor activity of the Eg5 inhibitor, S-trityl-L-cysteine (STLC), was confirmed in vitro. STLC could mediate cell apoptosis, as well as cell cycle arrest, in a dose-dependent manner, which may contribute toward its antitumor activity. STLC-mediated apoptosis and cell cycle arrest were triggered by activation of the mitogen-activated protein kinase and nuclear factor kB signaling pathways. These results suggested that STLC may have potential in the in vivo treatment of neuroblastoma.

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