Protein kinase CK2 inhibition down modulates the NF-κB and STAT3 survival pathways, enhances the cellular proteotoxic stress and synergistically boosts the cytotoxic effect of bortezomib on multiple myeloma and mantle cell lymphoma cells

PLoS One. 2013 Sep 27;8(9):e75280. doi: 10.1371/journal.pone.0075280. eCollection 2013.

Abstract

CK2 is a pivotal pro-survival protein kinase in multiple myeloma that may likely impinge on bortezomib-regulated cellular pathways. In the present study, we investigated CK2 expression in multiple myeloma and mantle cell lymphoma, two bortezomib-responsive B cell tumors, as well as its involvement in bortezomib-induced cytotoxicity and signaling cascades potentially mediating bortezomib resistance. In both tumors, CK2 expression correlated with that of its activated targets NF-κB and STAT3 transcription factors. Bortezomib-induced proliferation arrest and apoptosis were significantly amplified by the simultaneous inhibition of CK2 with two inhibitors (CX-4945 and K27) in multiple myeloma and mantle cell lymphoma cell lines, in a model of multiple myeloma bone marrow microenvironment and in cells isolated from patients. CK2 inhibition empowered bortezomib-triggered mitochondrial-dependent cell death. Phosphorylation of NF-κB p65 on Ser529 (a CK2 target site) and rise of the levels of the endoplasmic reticulum stress kinase/endoribonuclease Ire1α were markedly reduced upon CK2 inhibition, as were STAT3 phospho Ser727 levels. On the contrary, CK2 inhibition increased phospho Ser51 eIF2α levels and enhanced the bortezomib-dependent accumulation of poly-ubiquitylated proteins and of the proteotoxic stress-associated chaperone Hsp70. Our data suggest that CK2 over expression in multiple myeloma and mantle cell lymphoma cells might sustain survival signaling cascades and can antagonize bortezomib-induced apoptosis at different levels. CK2 inhibitors could be useful in bortezomib-based combination therapies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Analysis of Variance
  • Apoptosis / drug effects
  • Base Sequence
  • Blotting, Western
  • Boronic Acids / metabolism
  • Boronic Acids / pharmacology*
  • Bortezomib
  • Casein Kinase II / antagonists & inhibitors*
  • Casein Kinase II / genetics
  • Cell Line, Tumor
  • DNA Primers / genetics
  • Humans
  • Immunohistochemistry
  • Leukocytes, Mononuclear
  • Lymphoma, Mantle-Cell / drug therapy*
  • Molecular Sequence Data
  • Multiple Myeloma / drug therapy*
  • NF-kappa B / metabolism*
  • Naphthyridines / pharmacology
  • Phenazines
  • Pyrazines / metabolism
  • Pyrazines / pharmacology*
  • RNA Interference
  • Real-Time Polymerase Chain Reaction
  • STAT3 Transcription Factor / metabolism*
  • Signal Transduction / drug effects*
  • Signal Transduction / physiology

Substances

  • Boronic Acids
  • DNA Primers
  • NF-kappa B
  • Naphthyridines
  • Phenazines
  • Pyrazines
  • STAT3 Transcription Factor
  • Bortezomib
  • Adenosine Triphosphate
  • silmitasertib
  • Casein Kinase II

Grants and funding

This study was supported by a grant from the Ministero dell'Istruzione, dell' Università e della Ricerca Scientifica (MIUR; www.miur.it) n° RBFR086EW9 (FIRB "Futuro in Ricerca") and from a University of Padova (www.unipd.it) grant n° CPDA114940/11 "Progetti di Ricerca di Ateneo" to Francesco Piazza and from the Associazione Italiana per la Ricerca sul Cancro (A.I.R.C., Milan; www.airc.it) to Gianpietro Semenzato. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.