NF-κB as a potential therapeutic target in myelodysplastic syndromes and acute myeloid leukemia

Expert Opin Ther Targets. 2010 Nov;14(11):1157-76. doi: 10.1517/14728222.2010.522570.

Abstract

Importance of the field: The inactive NF-κB-inhibitor of NF-κB (IκB) complex is activated by stimuli including pro-inflammatory cytokines, mitogens, growth factors and stress-inducing agents. The release of NF-κB facilitates its translocation to the nucleus, where it promotes cell survival by initiating transcription of genes encoding stress-response enzymes, cell-adhesion molecules, pro-inflammatory cytokines and anti-apoptotic proteins. NF-κB and associated regulatory factors (IκB kinase subunits and bcl-3) are implicated in hematological and solid tumour malignancies. NF-κB appears to be involved in cell proliferation control, apoptosis control, angiogenesis promotion and possibly regulation of diffusion of metastases. There are several reports that inhibition of NF-κB as a therapeutic target may have a role in tumour cell death or growth inhibition.

Area covered in this review: We review data about inhibition of NF-κB in acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS). We describe the molecular mechanisms underlying NF-κB deregulation in these haematological malignancies.

What the reader will gain: Constitutive activation of NF-κB in the nucleus has been reported in some varieties of MDS/AML. The in vitro and in vivo results of NF-κB inhibition in myeloid malignancies are highlighted.

Take home message: NF-κB selective inhibitory drugs may be useful, either as single agents or associated with conventional chemotherapy.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / pharmacology
  • Animals
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use*
  • Drug Design*
  • Humans
  • I-kappa B Proteins / metabolism
  • Immunomodulation / drug effects
  • Leukemia, Myeloid, Acute / drug therapy*
  • Leukemia, Myeloid, Acute / metabolism
  • Molecular Targeted Therapy
  • Myelodysplastic Syndromes / drug therapy*
  • Myelodysplastic Syndromes / metabolism
  • NF-kappa B / antagonists & inhibitors*
  • NF-kappa B / metabolism*
  • Neovascularization, Pathologic / drug therapy
  • Protease Inhibitors / pharmacology
  • Protease Inhibitors / therapeutic use
  • Proteasome Endopeptidase Complex / metabolism
  • Proteasome Inhibitors
  • Signal Transduction / drug effects

Substances

  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • I-kappa B Proteins
  • NF-kappa B
  • Protease Inhibitors
  • Proteasome Inhibitors
  • Proteasome Endopeptidase Complex