AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer.

TitleAKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer.
Publication TypeJournal Article
Year of Publication2009
AuthorsVasudevan, 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
JournalCancer Cell
Volume16
Issue1
Pagination21-32
Date Published2009 Jul 7
ISSN1878-3686
KeywordsBreast 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.

DOI10.1016/j.ccr.2009.04.012
Alternate JournalCancer Cell
PubMed ID19573809
PubMed Central IDPMC2752826
Grant ListDP2 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