A copper chelate induces apoptosis and overcomes multidrug resistance in T-cell acute lymphoblastic leukemia through redox imbalance and inhibition of EGFR/PI3K/Akt expression

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• 作者：Kaushik Banerjee^a ; Satyajit Das^a ; Avijit Sarkar^b ; Mitali Chatterjee^b ; Jaydip Biswas^a ; Soumitra Kumar Choudhuri^a ; ^{soumitra01@yahoo.com}
• 关键词：PEG ; polyethylene glycol ; EGFR1 ; epidermal growth factor receptor 1 ; PI3K ; phosphatidylinositol 3-kinase ; CNS ; central nervous system ; PBMC ; peripheral blood mononuclear cell ; Ac-DEVD-cho ; N-Ac-Asp-Glu-Val-Asp-aldehyde ; z-VAD-fmk ; N-benzyloxycarbonyl-Val-Ala-Asp(O-Me) fluoromethyl ketone
• 刊名：Biomedicine & Pharmacotherapy
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：84
• 期：Complete
• 页码：71-92
• 全文大小：8168 K
• 卷排序：84

文摘

Cu-5-SMAG but not its ligand 5-SMAG targets leukemic cells while sparing the normal cells. Through redox imbalance and induction of apoptosis Cu-5-SMAG overcomes MDR in T-ALL. Cu-5-SMAG downregulates EGFR1, Akt activation and PI3K expression in CEM/ADR5000 cells. Cu-5-SMAG significantly increases the life-span of EAC/Dox and EAC/S bearing mice without inducing any significant side effects. Mere introduction of Cu doesn’t made a molecule effective as Cu-OBPHA fails to exert similar effect like Cu-5-SMAG.