Literature DB >> 24041865

Preclinical evaluation of the mTOR-PI3K inhibitor BEZ235 in nasopharyngeal cancer models.

Brigette B Y Ma1, Vivian W Y Lui2, Connie W C Hui3, Cecilia P Y Lau3, Chi H Wong3, Edwin P Hui3, Margaret H L Ng4, Suk H Cheng4, Sai W Tsao5, Chi-Man Tsang5, Crystal S F Cheung3, Kakiu Ho3, Anthony T C Chan3.   

Abstract

The dual PI3K-mTOR inhibitor BEZ235 was evaluated in preclinical models of nasopharyngeal carcinoma (NPC). The IC50 value of BEZ235 for growth was in the nanomolar range in vitro, induce G1 cycle arrest and apoptosis, and inhibited AKT and mTOR signaling in most NPC cell lines. No synergistic effect was observed when BEZ235 was combined with chemotherapy. BEZ235 increased MAPK activation in vitro but not in vivo. A daily schedule was more effective than a weekly schedule on tumor growth and inhibition of downstream mTOR signaling in vivo. The activity of BEZ235 maybe independent of the PIK3CA amplification and mutation status.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved.

Entities:  

Keywords:  BEZ235; MAPK activation; Nasopharyngeal carcinoma

Mesh:

Substances:

Year:  2013        PMID: 24041865     DOI: 10.1016/j.canlet.2013.09.007

Source DB:  PubMed          Journal:  Cancer Lett        ISSN: 0304-3835            Impact factor:   8.679


  13 in total

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2.  Preclinical evaluation of PI3K inhibitor BYL719 as a single agent and its synergism in combination with cisplatin or MEK inhibitor in nasopharyngeal carcinoma (NPC).

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Journal:  Am J Cancer Res       Date:  2015-03-15       Impact factor: 6.166

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Authors:  Stefan Holzhauser; Ourania N Kostopoulou; Anna Ohmayer; Birthe K A Lange; Torbjörn Ramqvist; Teodora Andonova; Cinzia Bersani; Malin Wickström; Tina Dalianis
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5.  Multicenter phase II study of the AKT inhibitor MK-2206 in recurrent or metastatic nasopharyngeal carcinoma from patients in the mayo phase II consortium and the cancer therapeutics research group (MC1079).

Authors:  B B Y Ma; B C Goh; W T Lim; E P Hui; E H Tan; G de Lima Lopes; K W Lo; L Li; H Loong; N R Foster; C Erlichman; A D King; M K M Kam; S F Leung; K C Chan; A T C Chan
Journal:  Invest New Drugs       Date:  2015-06-19       Impact factor: 3.651

6.  NVP-BEZ235 Attenuated Cell Proliferation and Migration in the Squamous Cell Carcinoma of Oral Cavities and p70S6K Inhibition Mimics its Effect.

Authors:  Cheng-Ming Hsu; Pai-Mei Lin; Hsin-Ching Lin; Yao-Te Tsai; Ming-Shao Tsai; Shau-Hsuan Li; Ching-Yuan Wu; Yao-Hsu Yang; Sheng-Fung Lin; Ming-Yu Yang
Journal:  Int J Mol Sci       Date:  2018-11-10       Impact factor: 5.923

7.  Oncogenic roles of carbonic anhydrase IX in human nasopharyngeal carcinoma.

Authors:  Yi Sang; Li Wang; Jian-Jun Tang; Mei-Fang Zhang; Meng-Xia Zhang; Xia Liu; Ru-Hua Zhang; Tie-Bang Kang; Ming-Yuan Chen
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8.  Inhibition of DNA methyltransferase as a novel therapeutic strategy to overcome acquired resistance to dual PI3K/mTOR inhibitors.

Authors:  Xiao-jun Qian; Yun-tian Li; Yan Yu; Fen Yang; Rong Deng; Jiao Ji; Lin Jiao; Xuan Li; Rui-Yan Wu; Wen-Dan Chen; Gong-Kan Feng; Xiao-Feng Zhu
Journal:  Oncotarget       Date:  2015-03-10

9.  NVP-BEZ235, a dual PI3K-mTOR inhibitor, suppresses the growth of FaDu hypopharyngeal squamous cell carcinoma and has a synergistic effect with Cisplatin.

Authors:  Cheng-Ming Hsu; Pai-Mei Lin; Yao-Te Tsai; Ming-Shao Tsai; Chun-Han Tseng; Sheng-Fung Lin; Ming-Yu Yang
Journal:  Cell Death Discov       Date:  2018-05-10

10.  Targeted Therapy With PI3K and FGFR Inhibitors on Human Papillomavirus Positive and Negative Tonsillar and Base of Tongue Cancer Lines With and Without Corresponding Mutations.

Authors:  Stefan Holzhauser; Nicole Wild; Mark Zupancic; Ramona G Ursu; Cinzia Bersani; Anders Näsman; Ourania N Kostopoulou; Tina Dalianis
Journal:  Front Oncol       Date:  2021-05-11       Impact factor: 6.244

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