Distinct molecular mechanisms responsible for bortezomib-induced death of therapy-resistant versus -sensitive B-NHL cells

Blood. 2010 Dec 16;116(25):5605-14. doi: 10.1182/blood-2009-12-259754. Epub 2010 Oct 7.

Abstract

Resistance to currently available therapies is a major impediment to the successful treatment of hematological malignancies. Here, we used a model of therapy-resistant B-cell non Hodgkin lymphoma (B-NHL) developed in our laboratory along with primary B-NHL cells to study basic mechanisms of bortezomib activity. In resistant cells and a subset of primary B-NHLs, bortezomib treatment led to stabilization of Bak and subsequent Bak-dependent activation of apoptosis. In contrast to sensitive cells that die strictly by apoptosis, bortezomib was capable of killing resistant cells through activation of apoptosis or caspase-independent mechanism(s) when caspases were pharmacologically inhibited. Our data demonstrate that bortezomib is capable of killing B-NHL cells via multiple mechanisms, regardless of their basal apoptotic potential, and contributes to growing evidence that proteasome inhibitors can act via modulation of B-cell lymphoma 2 (Bcl-2) family proteins. The capacity of bortezomib to act independently of the intrinsic apoptotic threshold of a given B-NHL cell suggests that bortezomib-based therapies could potentially overcome resistance and result in relevant clinical activity in a relapsed/refractory setting.

Publication types

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

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Blotting, Western
  • Boronic Acids / therapeutic use*
  • Bortezomib
  • Caspases / metabolism
  • Drug Resistance, Neoplasm*
  • Enzyme Activation / drug effects
  • Humans
  • Immunoprecipitation
  • Lymphoma, B-Cell / drug therapy*
  • Lymphoma, B-Cell / metabolism
  • Lymphoma, B-Cell / pathology*
  • Prognosis
  • Proto-Oncogene Proteins c-bcl-2 / metabolism*
  • Pyrazines / therapeutic use*
  • Tumor Cells, Cultured
  • Ubiquitination

Substances

  • Antineoplastic Agents
  • Boronic Acids
  • Proto-Oncogene Proteins c-bcl-2
  • Pyrazines
  • Bortezomib
  • Caspases