Downregulation of MicroRNA-644a Promotes Esophageal Squamous Cell Carcinoma Aggressiveness and Stem Cell-like Phenotype via Dysregulation of PITX2

Clin Cancer Res. 2017 Jan 1;23(1):298-310. doi: 10.1158/1078-0432.CCR-16-0414. Epub 2016 Jul 12.

Abstract

Purpose: We previously reported the oncogenic role of paired-like homeodomain 2 (PITX2) in esophageal squamous cell carcinoma (ESCC). In this study, we aimed to identify the miRNA regulators of PITX2 and the mechanism underlying the pathogenesis of ESCC.

Experimental design: Using miRNA profiling and bioinformatics analyses, we identified miR-644a as a negative mediator of PITX2 in ESCC. A series of in vivo and in vitro assays were performed to confirm the effect of miR-644a on PITX2-mediated ESCC malignancy.

Results: ESCC cells and tissues expressed less miR-644a than normal epithelial controls. In patient samples, lower expression of miR-644a in ESCC tissues was significantly correlated with tumor recurrence and/or metastasis, such that miR-644a, PITX2, and the combination of the two were independent prognostic indicators for ESCC patient's survival (P < 0.05). Gain- and loss-of-function studies demonstrated that miR-644a inhibited ESCC cell growth, migration, and invasion in vitro and suppressed tumor growth and metastasis in vivo In addition, miR-644a dramatically suppressed self-renewal and stem cell-like traits in ESCC cells. Furthermore, the effect of upregulation of miR-644a was similar to that of PITX2 knockdown in ESCC cells. Mechanistic studies revealed that miR-644a attenuates ESCC cells' malignancy and stem cell-associated phenotype, at least partially, by inactivation of the Akt/GSK-3β/β-catenin signaling pathway through PITX2. Furthermore, promoter hypermethylation caused downregulation of miR-644a in ESCC.

Conclusions: Downregulation of miR-644a plays an important role in promoting both aggressiveness and stem-like traits of ESCC cells, suggesting that miR-644a may be useful as a novel prognostic biomarker or therapeutic target for the disease. Clin Cancer Res; 23(1); 298-310. ©2016 AACR.

MeSH terms

  • Animals
  • Biomarkers, Tumor
  • Carcinoma, Squamous Cell / genetics*
  • Carcinoma, Squamous Cell / metabolism
  • Carcinoma, Squamous Cell / mortality
  • Carcinoma, Squamous Cell / pathology*
  • Cell Line, Tumor
  • Cell Movement / genetics
  • Cell Proliferation
  • DNA Methylation
  • Disease Models, Animal
  • Disease Progression
  • Esophageal Neoplasms / genetics*
  • Esophageal Neoplasms / metabolism
  • Esophageal Neoplasms / mortality
  • Esophageal Neoplasms / pathology*
  • Esophageal Squamous Cell Carcinoma
  • Gene Expression Profiling
  • Gene Expression Regulation, Neoplastic*
  • Glycogen Synthase Kinase 3 / genetics
  • Heterografts
  • Homeobox Protein PITX2
  • Homeodomain Proteins / genetics*
  • Humans
  • Immunophenotyping
  • Mice
  • MicroRNAs / genetics*
  • Neoplasm Metastasis
  • Neoplastic Stem Cells / metabolism*
  • Phenotype
  • Prognosis
  • Promoter Regions, Genetic
  • Proto-Oncogene Proteins c-akt / metabolism
  • RNA Interference*
  • Transcription Factors / genetics*
  • Tumor Burden / genetics
  • Wnt Signaling Pathway

Substances

  • Biomarkers, Tumor
  • Homeodomain Proteins
  • MIRN644 microRNA, human
  • MicroRNAs
  • Transcription Factors
  • Proto-Oncogene Proteins c-akt
  • Glycogen Synthase Kinase 3