Title | AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer. |
Publication Type | Journal Article |
Year of Publication | 2009 |
Authors | Vasudevan, KM, Barbie, DA, Davies, MA, Rabinovsky, R, McNear, CJ, Kim, JJ, Hennessy, BT, Tseng, H, Pochanard, P, Kim, SY, Dunn, IF, Schinzel, AC, Sandy, P, Hoersch, S, Sheng, Q, Gupta, PB, Boehm, JS, Reiling, JH, Silver, S, Lu, Y, Stemke-Hale, K, Dutta, B, Joy, C, Sahin, AA, Gonzalez-Angulo, AM, Lluch, A, Rameh, LE, Jacks, T, Root, DE, Lander, ES, Mills, GB, Hahn, WC, Sellers, WR, Garraway, LA |
Journal | Cancer Cell |
Volume | 16 |
Issue | 1 |
Pagination | 21-32 |
Date Published | 2009 Jul 7 |
ISSN | 1878-3686 |
Keywords | Breast Neoplasms, Cell Line, Tumor, Cell Survival, Enzyme Activation, Female, Gene Expression Profiling, Humans, Mutation, Neoplasms, Phosphatidylinositol 3-Kinases, Protein-Serine-Threonine Kinases, Proto-Oncogene Proteins c-akt, PTEN Phosphohydrolase, Signal Transduction |
Abstract | Dysregulation of the phosphatidylinositol 3-kinase (PI3K) signaling pathway occurs frequently in human cancer. PTEN tumor suppressor or PIK3CA oncogene mutations both direct PI3K-dependent tumorigenesis largely through activation of the AKT/PKB kinase. However, here we show through phosphoprotein profiling and functional genomic studies that many PIK3CA mutant cancer cell lines and human breast tumors exhibit only minimal AKT activation and a diminished reliance on AKT for anchorage-independent growth. Instead, these cells retain robust PDK1 activation and membrane localization and exhibit dependency on the PDK1 substrate SGK3. SGK3 undergoes PI3K- and PDK1-dependent activation in PIK3CA mutant cancer cells. Thus, PI3K may promote cancer through both AKT-dependent and AKT-independent mechanisms. Knowledge of differential PI3K/PDK1 signaling could inform rational therapeutics in cancers harboring PIK3CA mutations. |
DOI | 10.1016/j.ccr.2009.04.012 |
Alternate Journal | Cancer Cell |
PubMed ID | 19573809 |
PubMed Central ID | PMC2752826 |
Grant List | DP2 OD002750 / OD / NIH HHS / United States DP2 OD002750-01 / OD / NIH HHS / United States P01CA050661 / CA / NCI NIH HHS / United States P30 CA016672 / CA / NCI NIH HHS / United States P30CA14051 / CA / NCI NIH HHS / United States P50CA093459 / CA / NCI NIH HHS / United States P50CA112967 / CA / NCI NIH HHS / United States R01 CA085912 / CA / NCI NIH HHS / United States R01 CA085912-09 / CA / NCI NIH HHS / United States R01CA085912 / CA / NCI NIH HHS / United States R33CA128625 / CA / NCI NIH HHS / United States T32CA09172-33 / CA / NCI NIH HHS / United States |