Ack1 mediated AKT/PKB tyrosine 176 phosphorylation regulates its activation

PLoS One. 2010 Mar 19;5(3):e9646. doi: 10.1371/journal.pone.0009646.

Abstract

The AKT/PKB kinase is a key signaling component of one of the most frequently activated pathways in cancer and is a major target of cancer drug development. Most studies have focused on its activation by Receptor Tyrosine Kinase (RTK) mediated Phosphatidylinositol-3-OH kinase (PI3K) activation or loss of Phosphatase and Tensin homolog (PTEN). We have uncovered that growth factors binding to RTKs lead to activation of a non-receptor tyrosine kinase, Ack1 (also known as ACK or TNK2), which directly phosphorylates AKT at an evolutionarily conserved tyrosine 176 in the kinase domain. Tyr176-phosphorylated AKT localizes to the plasma membrane and promotes Thr308/Ser473-phosphorylation leading to AKT activation. Mice expressing activated Ack1 specifically in the prostate exhibit AKT Tyr176-phosphorylation and develop murine prostatic intraepithelial neoplasia (mPINs). Further, expression levels of Tyr176-phosphorylated-AKT and Tyr284-phosphorylated-Ack1 were positively correlated with the severity of disease progression, and inversely correlated with the survival of breast cancer patients. Thus, RTK/Ack1/AKT pathway provides a novel target for drug discovery.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Breast Neoplasms / pathology*
  • Cell Membrane / metabolism
  • Disease Progression
  • Female
  • Humans
  • Male
  • Mice
  • Mice, Transgenic
  • Phosphorylation
  • Prostatic Intraepithelial Neoplasia / pathology
  • Protein Structure, Tertiary
  • Protein-Tyrosine Kinases / metabolism*
  • Proto-Oncogene Proteins c-akt / metabolism*
  • Tyrosine / chemistry*

Substances

  • Tyrosine
  • Tnk2 protein, mouse
  • Protein-Tyrosine Kinases
  • TNK2 protein, human
  • Proto-Oncogene Proteins c-akt