Literature DB >> 23603977

NVP-BEZ235, a novel dual PI3K/mTOR inhibitor, enhances the radiosensitivity of human glioma stem cells in vitro.

Wen-juan Wang1, Lin-mei Long, Neng Yang, Qing-qing Zhang, Wen-jun Ji, Jiang-hu Zhao, Zheng-hong Qin, Zhong Wang, Gang Chen, Zhong-qin Liang.   

Abstract

AIM: NVP-BEZ235 is a novel dual PI3K/mTOR inhibitor and shows dramatic effects on gliomas. The aim of this study was to investigate the effects of NVP-BEZ235 on the radiosensitivity and autophagy of glioma stem cells (GSCs) in vitro.
METHODS: Human GSCs (SU-2) were tested. The cell viability and survival from ionizing radiation (IR) were evaluated using MTT and clonogenic survival assay, respectively. Immunofluorescence assays were used to identify the formation of autophagosomes. The apoptotic cells were quantified with annexin V-FITC/PI staining and flow cytometry, and observed using Hoechst 33258 staining and fluorescence microscope. Western blot analysis was used to analyze the expression levels of proteins. Cell cycle status was determined by measuring DNA content after staining with PI. DNA repair in the cells was assessed using a comet assay.
RESULTS: Treatment of SU-2 cells with NVP-BEZ235 (10-320 nmol/L) alone suppressed the cell growth in a concentration-dependent manner. A low concentration of NVP-BEZ235 (10 nmol/L) significantly increased the radiation sensitivity of SU-2 cells, which could be blocked by co-treatment with 3-MA (50 μmol/L). In NVP-BEZ235-treated SU-2 cells, more punctate patterns of microtubule-associated protein LC3 immunoreactivity was observed, and the level of membrane-bound LC3-II was significantly increased. A combination of IR with NVP-BEZ235 significantly increased the apoptosis of SU-2 cells, as shown in the increased levels of BID, Bax, and active caspase-3, and decreased level of Bcl-2. Furthermore, the combination of IR with NVP-BEZ235 led to G1 cell cycle arrest. Moreover, NVP-BEZ235 significantly attenuated the repair of IR-induced DNA damage as reflected by the tail length of the comet.
CONCLUSION: NVP-BEZ235 increases the radiosensitivity of GSCs in vitro by activating autophagy that is associated with synergistic increase of apoptosis and cell-cycle arrest and decrease of DNA repair capacity.

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Year:  2013        PMID: 23603977      PMCID: PMC4002877          DOI: 10.1038/aps.2013.22

Source DB:  PubMed          Journal:  Acta Pharmacol Sin        ISSN: 1671-4083            Impact factor:   6.150


  51 in total

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  35 in total

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Review 3.  Role of autophagy in regulating the radiosensitivity of tumor cells.

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Review 4.  Brain tumor stem cells: Molecular characteristics and their impact on therapy.

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Review 5.  Apoptotic and autophagic pathways with relevant small-molecule compounds, in cancer stem cells.

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Review 6.  Radiotherapy as a tool to elicit clinically actionable signalling pathways in cancer.

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7.  Identification of expression quantitative trait loci of MTOR associated with the progression of glioma.

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Review 8.  ATM, ATR, CHK1, CHK2 and WEE1 inhibitors in cancer and cancer stem cells.

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9.  Essential role of autophagy in fucoxanthin-induced cytotoxicity to human epithelial cervical cancer HeLa cells.

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10.  NVP-BEZ235 or JAKi Treatment leads to decreased survival of examined GBM and BBC cells.

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