BMP4 promotes oxaliplatin resistance by an induction of epithelial-mesenchymal transition via MEK1/ERK/ELK1 signaling in hepatocellular carcinoma

Cancer Lett. 2017 Dec 28:411:117-129. doi: 10.1016/j.canlet.2017.09.041. Epub 2017 Oct 4.

Abstract

Background: Bone morphogenetic protein-4 (BMP4) is a key regulator of epithelial-mesenchymal transition (EMT), which is crucial for cancer cells to acquire chemoresistance. The effects of BMP4 on OXA sensitivity in HCC need to be elucidated.

Methods: Functional analysis of BMP4 on EMT-regulated OXA sensitivity was performed in human HCC specimens, in the HCC cell lines HepG2 and HCCLM3, and in a subcutaneous tumor model receiving OXA treatment. The downstream signaling targets of BMP4 in HCC were profiled and confirmed.

Results: BMP4 expression was significantly increased in HCC tissue, and was correlated with tumor de-differentiation and unfavorable prognosis. BMP4 promoted HCC EMT and was correlated with OXA resistance. Blocking of BMP4 reversed EMT and increased OXA chemosensitivity in vitro and in vivo. ELK1, a transcription factor involved in EMT, was an important mediator of BMP4-induced OXA resistance in HCC. Blocking of MEK/ERK/ELK1 attenuated BMP4-induced EMT and enhanced OXA sensitivity.

Conclusions: BMP4 induces EMT and OXA chemoresistance via MEK/ERK/ELK1 signaling pathway in HCC. BMP4 may be a valuable therapeutic target for HCC patients receiving OXA-based chemotherapy.

Keywords: Bone morphogenetic protein 4; ELK1; Epithelial-mesenchymal transition; Hepatocellular carcinoma; Oxaliplatin.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Bone Morphogenetic Protein 4 / genetics*
  • Carcinoma, Hepatocellular / drug therapy*
  • Carcinoma, Hepatocellular / genetics
  • Carcinoma, Hepatocellular / metabolism*
  • Carcinoma, Hepatocellular / pathology
  • Cell Line, Tumor
  • Cell Proliferation / physiology
  • Drug Resistance, Neoplasm
  • Epithelial-Mesenchymal Transition
  • Female
  • Hep G2 Cells
  • Humans
  • Liver Neoplasms / drug therapy*
  • Liver Neoplasms / genetics
  • Liver Neoplasms / metabolism*
  • Liver Neoplasms / pathology
  • MAP Kinase Kinase 1 / genetics
  • MAP Kinase Kinase 1 / metabolism
  • MAP Kinase Signaling System
  • Male
  • Middle Aged
  • Organoplatinum Compounds / pharmacology*
  • Oxaliplatin
  • Transfection
  • ets-Domain Protein Elk-1 / metabolism

Substances

  • Antineoplastic Agents
  • BMP4 protein, human
  • Bone Morphogenetic Protein 4
  • ELK1 protein, human
  • Organoplatinum Compounds
  • ets-Domain Protein Elk-1
  • Oxaliplatin
  • MAP Kinase Kinase 1
  • MAP2K1 protein, human