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

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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… Click to show full 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.

Keywords: trityl cysteine; chemotherapeutic strategy; eg5 inhibitor; eg5

Journal Title: Oncology letters
Year Published: 2018

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