Protein kinase C inhibitor sotrastaurin selectively inhibits the growth of CD79 mutant diffuse large B-cell lymphomas

Cancer Res. 2011 Apr 1;71(7):2643-53. doi: 10.1158/0008-5472.CAN-10-2525. Epub 2011 Feb 15.

Abstract

The activated B-cell-like (ABC) subtype of diffuse large B-cell lymphoma (DLBCL) correlates with poor prognosis. The ABC subtype of DLBCL is associated with constitutive activation of the NF-κB pathway, and oncogenic lesions have been identified in its regulators, including CARD11/CARMA1 (caspase recruitment domain-containing protein 11), A20/TNFAIP3, and CD79A/B. In this study, we offer evidence of therapeutic potential for the selective PKC (protein kinase C) inhibitor sotrastaurin (STN) in preclinical models of DLBCL. A significant fraction of ABC DLBCL cell lines exhibited strong sensitivity to STN, and we found that the molecular nature of NF-κB pathway lesions predicted responsiveness. CD79A/B mutations correlated with STN sensitivity, whereas CARD11 mutations rendered ABC DLBCL cell lines insensitive. Growth inhibitory effects of PKC inhibition correlated with NF-κB pathway inhibition and were mediated by induction of G₁-phase cell-cycle arrest and/or cell death. We found that STN produced significant antitumor effects in a mouse xenograft model of CD79A/B-mutated DLBCL. Collectively, our findings offer a strong rationale for the clinical evaluation of STN in ABC DLBCL patients who harbor CD79 mutations also illustrating the necessity to stratify DLBCL patients according to their genetic abnormalities.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CARD Signaling Adaptor Proteins / genetics
  • CARD Signaling Adaptor Proteins / metabolism
  • CD79 Antigens / genetics*
  • Cell Growth Processes / drug effects
  • Cell Line, Tumor
  • G1 Phase / drug effects
  • Guanylate Cyclase / genetics
  • Guanylate Cyclase / metabolism
  • Humans
  • Lymphoma, Large B-Cell, Diffuse / drug therapy*
  • Lymphoma, Large B-Cell, Diffuse / enzymology
  • Mice
  • Mutation
  • NF-kappa B / metabolism
  • Protein Kinase C / antagonists & inhibitors
  • Protein Kinase Inhibitors / pharmacology*
  • Proto-Oncogene Proteins c-bcr / metabolism
  • Pyrroles / pharmacology*
  • Quinazolines / pharmacology*
  • Signal Transduction / drug effects

Substances

  • CARD Signaling Adaptor Proteins
  • CD79 Antigens
  • CD79A protein, human
  • CD79B protein, human
  • NF-kappa B
  • Protein Kinase Inhibitors
  • Pyrroles
  • Quinazolines
  • sotrastaurin
  • BCR protein, human
  • Proto-Oncogene Proteins c-bcr
  • Protein Kinase C
  • CARD11 protein, human
  • Guanylate Cyclase