Gli promotes epithelial-mesenchymal transition in human lung adenocarcinomas

Oncotarget. 2016 Dec 6;7(49):80415-80425. doi: 10.18632/oncotarget.11246.

Abstract

Adenocarcinoma is the most common type of lung cancer. Epithelial-mesenchymal transition (EMT) is required for tumor invasion/metastasis and the components that control this process are potential therapeutic targets. This study we examined the role of Gli in lung adenocarcinoma and whether its activation regulates metastasis through EMT in lung adenocarcinoma. We found that tumors with high Gli expression had significantly lower E-Cadherin expression in two independent cohorts of patients with lung adenocarcinoma that we studied. In vitro up-regulation of SHh resulted in increased cell migration while small molecule inhibitors of Smo or Gli significantly reduced cell mobility both in a wound healing assay and in a 3D cell invasion assay. Inhibition of Gli in vivo decreased tumor growth and induced an increase in E-Cadherin expression. Our results indicate that Gli may be critical for lung adenocarcinoma metastasis and that a novel Gli inhibitor shows promise as a therapeutic agent by preventing cell migration and invasion in vitro and significantly reducing tumor growth and increasing E-Cadherin expression in vivo.

Keywords: adenocarcinoma; epithelial-mesenchymal transition; gli; lung cancer; sonic hedgehog.

MeSH terms

  • A549 Cells
  • Adenocarcinoma / drug therapy
  • Adenocarcinoma / genetics
  • Adenocarcinoma / metabolism*
  • Adenocarcinoma / secondary
  • Adenocarcinoma of Lung
  • Animals
  • Antigens, CD
  • Antineoplastic Agents / pharmacology
  • Cadherins / genetics
  • Cadherins / metabolism
  • Cell Movement
  • Epithelial-Mesenchymal Transition* / drug effects
  • Female
  • Gene Expression Regulation, Neoplastic
  • Hedgehog Proteins / genetics
  • Hedgehog Proteins / metabolism
  • Humans
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / genetics
  • Lung Neoplasms / metabolism*
  • Lung Neoplasms / pathology
  • Male
  • Mice, Nude
  • Middle Aged
  • Neoplasm Invasiveness
  • Signal Transduction
  • Smoothened Receptor / antagonists & inhibitors
  • Smoothened Receptor / metabolism
  • Time Factors
  • Tumor Burden
  • Xenograft Model Antitumor Assays
  • Zinc Finger Protein GLI1 / antagonists & inhibitors
  • Zinc Finger Protein GLI1 / genetics
  • Zinc Finger Protein GLI1 / metabolism*

Substances

  • Antigens, CD
  • Antineoplastic Agents
  • CDH1 protein, human
  • Cadherins
  • GLI1 protein, human
  • Hedgehog Proteins
  • SHH protein, human
  • SMO protein, human
  • Smoothened Receptor
  • Zinc Finger Protein GLI1