BH3 response profiles from neuroblastoma mitochondria predict activity of small molecule Bcl-2 family antagonists

Cell Death Differ. 2010 May;17(5):872-82. doi: 10.1038/cdd.2009.171. Epub 2009 Nov 6.

Abstract

Bcl-2 family proteins regulate mitochondrial apoptosis downstream of diverse stressors. Cancer cells frequently deregulate Bcl-2 proteins leading to chemoresistance. We have optimized a platform for solid tumors in which Bcl-2 family resistance patterns are inferred. Functional mitochondria were isolated from neuroblastoma (NB) cell lines, exposed to distinct BH3-domain peptides, and assayed for cytochrome c release. Such BH3 profiles revealed three patterns of cytochrome c response. A subset had a dominant NoxaBH3 response implying Mcl1 dependence. These cells were more sensitive to small molecules that antagonize Mcl1 (AT-101) than those that antagonize Bcl-2, Bcl-xL and Bcl-w (ABT-737). A second subset had a dominant BikBH3 response, implying a Bcl-xL/-w dependence, and was exquisitely sensitive to ABT-737 (IC(50) <200 nM). Finally, most NB cell lines derived at relapse were relatively resistant to pro-death BH3 peptides and Bcl-2 antagonists. Our findings define heterogeneity for apoptosis resistance in NB, help triage emerging Bcl-2 antagonists for clinical use, and provide a platform for studies to characterize post-therapy resistance mechanisms for NB and other solid tumors.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Biphenyl Compounds / pharmacology
  • Cell Line
  • Cell Line, Tumor
  • Cytochromes c / metabolism
  • Gossypol / analogs & derivatives
  • Gossypol / pharmacology
  • Humans
  • Immunoblotting
  • Immunoprecipitation
  • Mitochondria / metabolism*
  • Neuroblastoma / metabolism*
  • Nitrophenols / pharmacology
  • Peptide Fragments / pharmacology*
  • Piperazines / pharmacology
  • Proto-Oncogene Proteins / pharmacology*
  • Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors*
  • Sulfonamides / pharmacology

Substances

  • ABT-737
  • Bax protein (53-86)
  • Biphenyl Compounds
  • Nitrophenols
  • Peptide Fragments
  • Piperazines
  • Proto-Oncogene Proteins
  • Proto-Oncogene Proteins c-bcl-2
  • Sulfonamides
  • Cytochromes c
  • Gossypol
  • gossypol acetic acid