PROX1 promotes hepatocellular carcinoma proliferation and sorafenib resistance by enhancing β-catenin expression and nuclear translocation

Oncogene. 2015 Oct 29;34(44):5524-35. doi: 10.1038/onc.2015.7. Epub 2015 Feb 16.

Abstract

Aberrant activation of the Wnt/β-catenin pathway is frequent in hepatocellular carcinoma (HCC) and contributes to HCC initiation and progression. This abnormal activation may result from somatic mutations in the genes of the Wnt/β-catenin pathway and/or dysregulation of the Wnt/β-catenin pathway. The mechanism for the latter remains poorly understood. Prospero-related homeobox 1 (PROX1) is a downstream target of the Wnt/β-catenin pathway in human colorectal cancer and elevated PROX1 expression promotes malignant progression. However, the Wnt/β-catenin pathway does not regulate PROX1 expression in the liver and HCC cells. Here we report that PROX1 promotes HCC cell proliferation in vitro and tumor growth in HCC xenograft mice. PROX1 and β-catenin levels are positively correlated in tumor tissues as well as in cultured HCC cells. PROX1 can upregulate β-catenin transcription by stimulating the β-catenin promoter and enhance the nuclear translocation of β-catenin in HCC cells, which leads to the activation of the Wnt/β-catenin pathway. Moreover, we show that increase in PROX1 expression renders HCC cells more resistant to sorafenib treatment, which is the standard therapy for advanced HCC. Overall, we have pinpointed PROX1 as a critical factor activating the Wnt/β-catenin pathway in HCC, which promotes HCC proliferation and sorafenib resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carcinoma, Hepatocellular / drug therapy
  • Carcinoma, Hepatocellular / genetics*
  • Carcinoma, Hepatocellular / pathology
  • Cell Line
  • Cell Line, Tumor
  • Cell Nucleus / metabolism
  • Cell Proliferation / drug effects
  • Cell Proliferation / genetics*
  • Drug Resistance, Neoplasm / genetics*
  • HEK293 Cells
  • Homeodomain Proteins / genetics*
  • Humans
  • Liver / metabolism
  • Liver / pathology
  • Liver Neoplasms / drug therapy
  • Liver Neoplasms / genetics*
  • Liver Neoplasms / pathology
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Niacinamide / analogs & derivatives
  • Niacinamide / pharmacology
  • Phenylurea Compounds / pharmacology
  • Promoter Regions, Genetic / drug effects
  • Promoter Regions, Genetic / genetics
  • Sorafenib
  • Transcription, Genetic / drug effects
  • Transcription, Genetic / genetics
  • Tumor Suppressor Proteins / genetics*
  • Up-Regulation / drug effects
  • Up-Regulation / genetics
  • Wnt Proteins / genetics
  • beta Catenin / genetics*
  • beta Catenin / metabolism*

Substances

  • Homeodomain Proteins
  • Phenylurea Compounds
  • Tumor Suppressor Proteins
  • Wnt Proteins
  • beta Catenin
  • prospero-related homeobox 1 protein
  • Niacinamide
  • Sorafenib