Sensitivity of tumor cells to proteasome inhibitors is associated with expression levels and composition of proteasome subunits

Cancer. 2008 Feb 1;112(3):659-70. doi: 10.1002/cncr.23224.

Abstract

Background: Sensitivity of tumor cells to induction of apoptosis by proteasome inhibitors varies greatly. This study was undertaken to investigate the sensitivity of neoplastic B cells and solid tumor cells to proteasome inhibition with respect to constitutive expression levels of proteasome subunits.

Methods: Twelve neoplastic B-cell lines and 12 solid tumor cell lines were assessed for their expression levels of proteasome subunits by using quantitative reverse transcriptase-polymerase chain reaction analysis and were assessed for their sensitivity to the proteasome inhibitors PS-341 and lactacystin by using a flow cytometry assay that detected activated caspases.

Results: The neoplastic B-cell lines were categorized into 3 groups representing refractory cell lines, cell lines with moderate sensitivity, and cell lines with high sensitivity. Correlating expression levels of proteasome subunits with sensitivity to proteasome inhibition indicated that refractory B cells exhibited lower expression levels of the standard subunit beta2 and of the immunoproteasome subunit LMP2 compared with sensitive B cell lines. Compared with neoplastic B cells solid tumor cells were less sensitive. They expressed the immunoproteasome subunits LMP2, LMP7 and MECL-1 and the standard subunit beta2 clearly below the median of the expression level of the sensitive B cell lines. IFN-gamma pretreatment enhanced sensitivity to PS-341 in 50% of the tumor cell lines, potentially related to the induction of immunoproteasomes.

Conclusions: The results of this study indicated that sensitivity to proteasome inhibition is correlated with expression levels of proteasome subunits, which determine the enzymatic activity of the proteasome. Combining PS-341 with IFN-gamma may enhance its clinical efficacy.

MeSH terms

  • Acetylcysteine / analogs & derivatives
  • Acetylcysteine / pharmacology
  • Apoptosis / drug effects
  • B-Lymphocytes / drug effects
  • B-Lymphocytes / metabolism
  • B-Lymphocytes / pathology
  • Boronic Acids / pharmacology
  • Bortezomib
  • Cell Line, Tumor
  • Cysteine Endopeptidases / metabolism
  • Drug Screening Assays, Antitumor
  • Humans
  • Interferon-gamma / pharmacology
  • Lymphoma / metabolism*
  • Lymphoma / pathology
  • Multienzyme Complexes / metabolism
  • Multiple Myeloma / metabolism*
  • Multiple Myeloma / pathology
  • Protease Inhibitors / pharmacology*
  • Proteasome Endopeptidase Complex / metabolism*
  • Protein Subunits / metabolism*
  • Pyrazines / pharmacology

Substances

  • Boronic Acids
  • Multienzyme Complexes
  • Protease Inhibitors
  • Protein Subunits
  • Pyrazines
  • lactacystin
  • LMP-2 protein
  • Bortezomib
  • Interferon-gamma
  • Cysteine Endopeptidases
  • LMP7 protein
  • PSMB10 protein, human
  • Proteasome Endopeptidase Complex
  • Acetylcysteine