Atypical protein kinase C{iota} is required for bronchioalveolar stem cell expansion and lung tumorigenesis

Cancer Res. 2009 Oct 1;69(19):7603-11. doi: 10.1158/0008-5472.CAN-09-2066. Epub 2009 Sep 8.

Abstract

Protein kinase Ciota (PKCiota) is an oncogene required for maintenance of the transformed phenotype of non-small cell lung cancer cells. However, the role of PKCiota in lung tumor development has not been investigated. To address this question, we established a mouse model in which oncogenic Kras(G12D) is activated by Cre-mediated recombination in the lung with or without simultaneous genetic loss of the mouse PKCiota gene, Prkci. Genetic loss of Prkci dramatically inhibits Kras-initiated hyperplasia and subsequent lung tumor formation in vivo. This effect correlates with a defect in the ability of Prkci-deficient bronchioalveolar stem cells to undergo Kras-mediated expansion and morphologic transformation in vitro and in vivo. Furthermore, the small molecule PKCiota inhibitor aurothiomalate inhibits Kras-mediated bronchioalveolar stem cell expansion and lung tumor growth in vivo. Thus, Prkci is required for oncogene-induced expansion and transformation of tumor-initiating lung stem cells. Furthermore, aurothiomalate is an effective antitumor agent that targets the tumor-initiating stem cell niche in vivo. These data have important implications for PKCiota as a therapeutic target and for the clinical use of aurothiomalate for lung cancer treatment.

Publication types

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

MeSH terms

  • Animals
  • Bronchioles / enzymology
  • Bronchioles / pathology*
  • Carcinoma, Non-Small-Cell Lung / enzymology*
  • Carcinoma, Non-Small-Cell Lung / genetics
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Cell Transformation, Neoplastic / drug effects
  • Cell Transformation, Neoplastic / genetics
  • Cell Transformation, Neoplastic / metabolism*
  • Cell Transformation, Neoplastic / pathology
  • Genes, ras / drug effects
  • Gold Sodium Thiomalate / pharmacology
  • Humans
  • Isoenzymes / deficiency
  • Isoenzymes / genetics*
  • Isoenzymes / metabolism
  • Lung Neoplasms / enzymology*
  • Lung Neoplasms / genetics
  • Lung Neoplasms / pathology
  • Male
  • Mice
  • Mice, Transgenic
  • Protein Kinase C / deficiency
  • Protein Kinase C / genetics*
  • Protein Kinase C / metabolism
  • Pulmonary Alveoli / enzymology
  • Pulmonary Alveoli / pathology*
  • Stem Cells / enzymology
  • Stem Cells / pathology*

Substances

  • Isoenzymes
  • Gold Sodium Thiomalate
  • Protein Kinase C
  • protein kinase C lambda