Distinctive requirement of PKCε in the control of Rho GTPases in epithelial and mesenchymally transformed lung cancer cells

Oncogene. 2019 Jul;38(27):5396-5412. doi: 10.1038/s41388-019-0796-4. Epub 2019 Mar 28.

Abstract

Diacylglycerol (DAG)/phorbol ester-regulated protein kinase C (PKC) isozymes have been widely linked to tumor promotion and the development of a metastatic phenotype. PKCε, an oncogenic member of the PKC family, is abnormally overexpressed in lung cancer and other cancer types. This kinase plays significant roles in proliferation, survival, and migration; however, its role in epithelial-to-mesenchymal transition (EMT) has been scarcely studied. Silencing experiments in non-small lung cancer (NSCLC) cells revealed that PKCε or other DAG-regulated PKCs (PKCα and PKCδ) were dispensable for the acquisition of a mesenchymal phenotype induced by transforming growth factor beta (TGF-β). Unexpectedly, we found a nearly complete down-regulation of PKCε expression in TGF-β-mesenchymally transformed NSCLC cells. PMA and AJH-836 (a DAG-mimetic that preferentially activates PKCε) promote ruffle formation in NSCLC cells via Rac1, however they fail to induce these morphological changes in TGF-β-mesenchymally transformed cells despite their elevated Rac1 activity. Several Rac guanine nucleotide exchange-factors (Rac-GEFs) were also up-regulated in TGF-β-treated NSCLC cells, including Trio and Tiam2, which were required for cell motility. Lastly, we found that silencing or inhibiting PKCε enhances RhoA activity and stress fiber formation, a phenotype also observed in TGF-β-transformed cells. Our studies established a distinctive involvement of PKCε in epithelial and mesenchymal NSCLC cells, and identified a complex interplay between PKCε and small GTPases that contributes to regulation of NSCLC cell morphology and motile activity.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Carcinoma, Non-Small-Cell Lung / enzymology*
  • Carcinoma, Non-Small-Cell Lung / pathology*
  • Cell Line, Tumor
  • Diglycerides / metabolism
  • Down-Regulation / drug effects
  • Enzyme Activation
  • Epithelial-Mesenchymal Transition / drug effects*
  • Humans
  • Lung Neoplasms / enzymology*
  • Lung Neoplasms / pathology*
  • Protein Kinase C-epsilon / metabolism*
  • Transforming Growth Factor beta / pharmacology
  • Up-Regulation / drug effects
  • rho GTP-Binding Proteins / metabolism*

Substances

  • Diglycerides
  • Transforming Growth Factor beta
  • Protein Kinase C-epsilon
  • rho GTP-Binding Proteins