An IκB kinase 2 inhibitor IMD-0354 suppresses the survival of adult T-cell leukemia cells

Cancer Sci. 2012 Jan;103(1):100-6. doi: 10.1111/j.1349-7006.2011.02110.x. Epub 2011 Nov 27.

Abstract

Adult T-cell leukemia (ATL) is a fatal T-cell malignancy associated with human T-cell leukemia virus type I infection. The aberrant expression of nuclear factor-κB (NF-κB) is considered to contribute to the malignant phenotype and chemo-resistance of ATL cells. Because of the poor prognosis of ATL, the development of new therapeutic strategies is direly needed. In the present study, we show that an IκB kinase 2 (IKK2) inhibitor, IMD-0354, efficiently inhibits the survival of CD4(+) CD25(+) primary ATL cells and prevents the growth of or induces apoptosis of patient-derived ATL cell lines. Assays of transcription with integrated forms of reporter genes revealed that IMD-0354 suppresses NF-κB-dependent transcriptional activity. Moreover, the daily administration of IMD-0354 prevents the growth of tumors in mice inoculated with ATL cells. Our results suggest that targeting IKK2 with a small molecule inhibitor, such as IMD-0354, is an attractive strategy for the treatment of ATL.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Animals
  • Apoptosis / drug effects*
  • Benzamides / pharmacology*
  • Blotting, Western
  • Case-Control Studies
  • Caspases / metabolism
  • Cell Cycle / drug effects
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Enzyme Inhibitors / pharmacology*
  • Flow Cytometry
  • Humans
  • I-kappa B Kinase / antagonists & inhibitors*
  • I-kappa B Kinase / metabolism
  • Leukemia-Lymphoma, Adult T-Cell / drug therapy*
  • Leukemia-Lymphoma, Adult T-Cell / metabolism
  • Leukemia-Lymphoma, Adult T-Cell / pathology*
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • Luciferases / metabolism
  • Mice
  • Mice, Inbred NOD
  • Mice, SCID
  • NF-kappa B / genetics
  • NF-kappa B / metabolism*

Substances

  • Benzamides
  • Enzyme Inhibitors
  • NF-kappa B
  • N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide
  • Luciferases
  • I-kappa B Kinase
  • Caspases