Overcoming rituximab drug-resistance by the genetically engineered anti-CD20-hIFN-α fusion protein: Direct cytotoxicity and synergy with chemotherapy

Int J Oncol. 2015 Nov;47(5):1735-48. doi: 10.3892/ijo.2015.3170. Epub 2015 Sep 16.

Abstract

Treatment of patients with B-NHL with rituximab and CHOP has resulted in significant clinical responses. However, a subset of patients develops resistance to further treatments. The mechanism of unresponsiveness in vivo is not known. We have reported the development of rituximab-resistant clones derived from B-NHL cell lines as models to investigate the mechanism of resistance. The resistant clones exhibit hyper-activated survival/anti-apoptotic pathways and no longer respond to a combination of rituximab and drugs. Recent studies reported the therapeutic efficacy in mice bearing B-cell lymphoma xenografts following treatment with the anti-CD20-hIFNα fusion protein. We hypothesized that the fusion protein may bypass rituximab resistance and inhibit survival signaling pathways. Treatment of the rituximab-resistant clones with anti-CD20-hIFNα, but not with rituximab, IFNα, or rituximab+IFNα resulted in significant inhibition of cell proliferation and induction of cell death. Treatment with anti-CD20-hIFNα sensitized the cells to apoptosis by CDDP, doxorubicin and Treanda. Treatment with anti-CD20-hIFNα inhibited the NF-κB and p38 MAPK activities and induced the activation of PKC-δ and Stat-1. These effects were corroborated by the use of the inhibitors SB203580 (p38 MAPK) and Rottlerin (PKC-δ). Treatment with SB203580 enhanced the sensitization of the resistant clone by anti-CD20-hIFNα to CDDP apoptosis. In contrast, treatment with Rotterin inhibited significantly the sensitization induced by anti-CD20-hIFNα. Overall, the findings demonstrate that treatment with anti-CD20-hIFNα reverses resistance of B-NHL. These findings suggest the potential application of anti-CD20-hIFNα in combination with drugs in patients unresponsive to rituximab-containing regimens.

Publication types

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

MeSH terms

  • Animals
  • Antigens, CD20 / genetics*
  • Antigens, CD20 / therapeutic use
  • Apoptosis
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Resistance, Neoplasm / genetics
  • Humans
  • Imidazoles / administration & dosage
  • Interferon-alpha / genetics*
  • Interferon-alpha / therapeutic use
  • Lymphoma, B-Cell / drug therapy*
  • Lymphoma, B-Cell / genetics*
  • Lymphoma, B-Cell / pathology
  • Mice
  • Oncogene Proteins, Fusion / genetics*
  • Pyridines / administration & dosage
  • Rituximab / administration & dosage
  • p38 Mitogen-Activated Protein Kinases

Substances

  • Antigens, CD20
  • Imidazoles
  • Interferon-alpha
  • Oncogene Proteins, Fusion
  • Pyridines
  • Rituximab
  • p38 Mitogen-Activated Protein Kinases
  • SB 203580