Calcium calmodulin dependent kinase kinase 2 - a novel therapeutic target for gastric adenocarcinoma

Cancer Biol Ther. 2015;16(2):336-45. doi: 10.4161/15384047.2014.972264.

Abstract

Gastric cancer is one of the most common gastrointestinal malignancies and is associated with poor prognosis. Exploring alterations in the proteomic landscape of gastric cancer is likely to provide potential biomarkers for early detection and molecules for targeted therapeutic intervention. Using iTRAQ-based quantitative proteomic analysis, we identified 22 proteins that were overexpressed and 17 proteins that were downregulated in gastric tumor tissues as compared to the adjacent normal tissue. Calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) was found to be 7-fold overexpressed in gastric tumor tissues. Immunohistochemical labeling of tumor tissue microarrays for validation of CAMKK2 overexpression revealed that it was indeed overexpressed in 94% (92 of 98) of gastric cancer cases. Silencing of CAMKK2 using siRNA significantly reduced cell proliferation, colony formation and invasion of gastric cancer cells. Our results demonstrate that CAMKK2 signals in gastric cancer through AMPK activation and suggest that CAMKK2 could be a novel therapeutic target in gastric cancer.

Keywords: LC-MS/MS, Liquid chromatography-tandem mass spectrometry; PSM, Peptide spectrum match; SCX, Strong cation exchange chromatography; iTRAQ, Isobaric tags for relative and absolute quantitation; in vitro labeling; invasion; mass spectrometry; proliferation; siRNA, short interfering RNA; targeted therapy.

Publication types

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

MeSH terms

  • AMP-Activated Protein Kinases / metabolism
  • Adenocarcinoma / drug therapy
  • Adenocarcinoma / metabolism*
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Calcium-Calmodulin-Dependent Protein Kinase Kinase / antagonists & inhibitors
  • Calcium-Calmodulin-Dependent Protein Kinase Kinase / genetics
  • Calcium-Calmodulin-Dependent Protein Kinase Kinase / metabolism*
  • Cell Line, Tumor
  • Cell Proliferation
  • Enzyme Activation
  • Gene Expression
  • Gene Silencing
  • Humans
  • Immunohistochemistry
  • Molecular Targeted Therapy
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use
  • Proteome
  • Proteomics
  • Reproducibility of Results
  • Stomach Neoplasms / drug therapy
  • Stomach Neoplasms / metabolism*

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Proteome
  • Calcium-Calmodulin-Dependent Protein Kinase Kinase
  • AMP-Activated Protein Kinases