The pan-HDAC inhibitor vorinostat potentiates the activity of the proteasome inhibitor carfilzomib in human DLBCL cells in vitro and in vivo

Blood. 2010 Jun 3;115(22):4478-87. doi: 10.1182/blood-2009-12-257261. Epub 2010 Mar 16.

Abstract

Interactions between histone deacetylase inhibitors (HDACIs) and the novel proteasome inhibitor carfilzomib (CFZ) were investigated in GC- and activated B-cell-like diffuse large B-cell lymphoma (ABC-DLBCL) cells. Coadministration of subtoxic or minimally toxic concentrations of CFZ) with marginally lethal concentrations of HDACIs (vorinostat, SNDX-275, or SBHA) synergistically increased mitochondrial injury, caspase activation, and apoptosis in both GC- and ABC-DLBCL cells. These events were associated with Jun NH2-terminal kinase (JNK) and p38MAPK activation, abrogation of HDACI-mediated nuclear factor-kappaB activation, AKT inactivation, Ku70 acetylation, and induction of gammaH2A.X. Genetic or pharmacologic JNK inhibition significantly diminished CFZ/vorinostat lethality. CFZ/vorinostat induced pronounced lethality in 3 primary DLBCL specimens but minimally affected normal CD34(+) hematopoietic cells. Bortezomib-resistant GC (SUDHL16) and ABC (OCI-LY10) cells exhibited partial cross-resistance to CFZ. However, CFZ/vorinostat dramatically induced resistant cell apoptosis, accompanied by increased JNK activation and gammaH2A.X expression. Finally, subeffective vorinostat doses markedly increased CFZ-mediated tumor growth suppression and apoptosis in a murine xenograft OCI-LY10 model. These findings indicate that HDACIs increase CFZ activity in GC- and ABC-DLBCL cells sensitive or resistant to bortezomib through a JNK-dependent mechanism in association with DNA damage and inhibition of nuclear factor-kappaB activation. Together, they support further investigation of strategies combining CFZ and HDACIs in DLBCL.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Apoptosis / drug effects
  • Boronic Acids / pharmacology
  • Bortezomib
  • Cell Cycle / drug effects
  • Chymotrypsin / antagonists & inhibitors
  • DNA Damage
  • Drug Resistance, Neoplasm
  • Drug Synergism
  • Histone Deacetylase Inhibitors / administration & dosage*
  • Humans
  • Hydroxamic Acids / administration & dosage*
  • In Vitro Techniques
  • JNK Mitogen-Activated Protein Kinases / metabolism
  • Lymphoma, Large B-Cell, Diffuse / drug therapy*
  • Lymphoma, Large B-Cell, Diffuse / metabolism
  • Lymphoma, Large B-Cell, Diffuse / pathology
  • Mice
  • Mice, Nude
  • Mitochondria / drug effects
  • NF-kappa B / metabolism
  • Oligopeptides / administration & dosage*
  • Protease Inhibitors / administration & dosage*
  • Proteasome Inhibitors
  • Pyrazines / pharmacology
  • Vorinostat
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Boronic Acids
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • NF-kappa B
  • Oligopeptides
  • Protease Inhibitors
  • Proteasome Inhibitors
  • Pyrazines
  • Vorinostat
  • Bortezomib
  • carfilzomib
  • JNK Mitogen-Activated Protein Kinases
  • Chymotrypsin