Metformin inhibits glioma cells stemness and epithelial-mesenchymal transition via regulating YAP activity

Biomed Pharmacother. 2018 Jun:102:263-270. doi: 10.1016/j.biopha.2018.03.031. Epub 2018 Mar 22.

Abstract

This work aims to study the roles and mechanisms of metformin in glioma cells stemness and epithelial-mesenchymal transition. Here, we found that metformin suppressed glioma cells spheroid formation and size, inhibited the expression of glioma stemness-related marker, CD133. Additionally, Metformin attenuated TGF-β-induced epithelial-mesenchymal transition in glioma cells. Mechanistically, metformin inhibited the nuclear abundance of YAP, a key effector of Hippo pathway, subsequently leading to its cytoplasmic retention, and thus reduced YAP transcriptional modulating activity. Importantly, overexpression of a mutant form of YAP (YAP-5SA) attenuated the inhibition of metformin on glioma cells stemness and epithelial-mesenchymal transition. Thus, metformin inhibits glioma cells stemness and epithelial-mesenchymal transition via regulating YAP activity.

Keywords: CSCs; Glioma; Hippo; Metformin; YAP/TAZ.

MeSH terms

  • Adaptor Proteins, Signal Transducing / genetics
  • Adaptor Proteins, Signal Transducing / metabolism*
  • Cell Line, Tumor
  • Cell Shape / drug effects
  • Cell Survival / drug effects
  • Central Nervous System Neoplasms / metabolism
  • Central Nervous System Neoplasms / pathology*
  • Dose-Response Relationship, Drug
  • Epithelial-Mesenchymal Transition / drug effects*
  • Glioma / metabolism
  • Glioma / pathology*
  • Humans
  • Metformin / pharmacology*
  • Neoplastic Stem Cells / drug effects*
  • Neoplastic Stem Cells / metabolism
  • Neoplastic Stem Cells / pathology
  • Phosphoproteins / genetics
  • Phosphoproteins / metabolism*
  • Signal Transduction
  • Transcription Factors
  • YAP-Signaling Proteins

Substances

  • Adaptor Proteins, Signal Transducing
  • Phosphoproteins
  • Transcription Factors
  • YAP-Signaling Proteins
  • YAP1 protein, human
  • Metformin