The BH3 mimetic S1 induces autophagy through ER stress and disruption of Bcl-2/Beclin 1 interaction in human glioma U251 cells

Cancer Lett. 2012 Oct 28;323(2):180-7. doi: 10.1016/j.canlet.2012.04.009. Epub 2012 May 8.

Abstract

Previous results showed that a novel BH3 mimetic S1 could induce cell death in a wide range of cancer types in vitro through Bax/Bak-dependent apoptosis. We demonstrated that in addition to mitochondrial pathway apoptosis, endoplasmic reticulum (ER) stress-associated apoptosis was also induced by S1. Moreover, S1 can induce autophagy in U251 cells, which may occur through ER stress and disruption of the association of Bcl-2 and Beclin 1. Inhibition of autophagy by the autophagic inhibitors 3-methyladenine (3-MA) or chloroquine (CQ) increased S1-induced apoptosis. In conclusion, autophagy plays an important role in S1-induced U251 cell death.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis Regulatory Proteins / metabolism*
  • Autophagy / drug effects*
  • Beclin-1
  • Brain Neoplasms / immunology
  • Brain Neoplasms / metabolism
  • Brain Neoplasms / pathology*
  • Cell Line, Tumor
  • Endoplasmic Reticulum / drug effects*
  • Endoplasmic Reticulum / metabolism
  • Glioma / immunology
  • Glioma / metabolism
  • Glioma / pathology*
  • Humans
  • In Situ Nick-End Labeling
  • Membrane Proteins / metabolism*
  • Microscopy, Confocal
  • Microscopy, Fluorescence
  • Molecular Mimicry*
  • Peptide Fragments / pharmacology*
  • Proto-Oncogene Proteins / pharmacology*
  • Proto-Oncogene Proteins c-bcl-2 / metabolism*

Substances

  • Apoptosis Regulatory Proteins
  • BECN1 protein, human
  • Bax protein (53-86)
  • Beclin-1
  • Membrane Proteins
  • Peptide Fragments
  • Proto-Oncogene Proteins
  • Proto-Oncogene Proteins c-bcl-2