Dual Inactivation of Akt and ERK by TIC10 Signals Foxo3a Nuclear Translocation, TRAIL Gene Induction, and Potent Antitumor Effects

• DOI: 10.1126/scitranslmed.3004828
• Publication Date: 2013-02-06T21:31:09Z
• Authors: Joshua E. Allen; Gabriel Krigsfeld; Patrick A. Mayes; Luv Patel; David T. Dicker; Akshal S. Patel; Nathan G. Dolloff; Evangelos Messaris; Kimberly A. Scata; Wenge Wang; Jun-Ying Zhou; Gen Sheng Wu; Wafik S. El-Deiry
• Keywords: Cell Nucleus; 0303 health sciences; Cell Death; Forkhead Box Protein O3; Imidazoles; Antineoplastic Agents; Apoptosis; Forkhead Transcription Factors; Bystander Effect; Heterocyclic Compounds, 4 or More Rings; Models, Biological; 3. Good health; Enzyme Activation; Gene Expression Regulation, Neoplastic; Mice; Protein Transport; 03 medical and health sciences; Cell Line, Tumor; Animals; Humans; Extracellular Signal-Regulated MAP Kinases; Glioblastoma; Proto-Oncogene Proteins c-akt

TIC10 is a small molecule that activates Foxo3a through dual inactivation of Akt and ERK, up-regulates the expression TRAIL gene, an endogenous tumor suppressor, effectively improves therapeutic properties utility as anticancer therapy.