Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

By S. Maira, F. Stauffer, Joseph Brueggen, P. Furet, C. Schnell, C. Fritsch, S. Brachmann, P. Chène, A. de Pover, Kevin Schoemaker and 7 more. Molecular Cancer Therapeutics, 2008

1,165 citations recorded by the source corpus.

Subfields: Molecular Biology

View Paper: https://www.semanticscholar.org/paper/1b2551a052b2ec093f84925ddfbffa85699c7c8a

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In Molecular Biology

1. Stephen J. Elledge
2. X. Chen
3. Ji Luo
4. N. Solimini
5. Jean J. Zhao
6. R. DePinho
7. T. Roberts
8. J. Bartek

Citations in the corpus

• Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction (2009, positive): “…and tumor vasculature Folkman, 2007 BEZ235 (small molecule) PI3K OA Causes cell-cycle arrest in tumor cells and inhibits tumor angiogenesis Maira et al., 2008 GRN163L (modified oligo) hTERT OA Mimics telomere sequence and inhibits the hTERT active site Dikmen et al., 2005; Harley, 2008…”
• BRafV600E cooperates with Pten silencing to elicit metastatic melanoma (2009, background): “Given the prevalence of BRAF and PTEN alterations in melanoma, testing such agents in a validated preclinical mouse model may inform the clinical development of various new and more selective BRAF, MEK, PI3′-kinase, AKT and mTor inhibitor”
• Targeting the phosphoinositide 3-kinase (PI3K) pathway in cancer (2009, background): “BEZ235 is an imidazoquinazoline derivative that inhibits multiple class I PI3K isoforms and mTOR kinase activity by binding to the ATP-binding pocke”
• Identification of human triple-negative breast cancer subtypes and preclinical models for selection of targeted therapies. (2011, methodology): “While PIK3CA mutations predicted NVP-BEZ235 sensitivity, PTEN deficiencies (mutation or loss of protein expression) did not correlate with sensitivity.”