CK2α and CK2α' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives

Eur J Med Chem. 2012 Jan;47(1):345-50. doi: 10.1016/j.ejmech.2011.11.002. Epub 2011 Nov 13.

Abstract

The goal of this study was to test the inhibitory activity of a series of tetrahalogenobenzimidazoles, including a number of novel derivatives, on individual catalytic subunits of human CK2. 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazoles and their newly obtained N(1)- and 2-S-carboxyalkyl derivatives showed potent inhibitory activity against both these subunits. CK2α' was up to 6 times more sensitive to the studied compounds than CK2α. The investigated iododerivatives showed, in most cases, stronger inhibitory properties than the respective brominated congeners, but the differences showed considerable dependence on the protein substrate used.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzimidazoles / pharmacology*
  • Casein Kinase II / antagonists & inhibitors*
  • Casein Kinase II / chemistry
  • Casein Kinase II / metabolism
  • Catalytic Domain
  • Humans
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Subunits / antagonists & inhibitors*
  • Protein Subunits / chemistry
  • Protein Subunits / metabolism

Substances

  • 4,5,6,7-tetrabromobenzimidazole
  • 4,5,6,7-tetraiodo-1H-benzimidazole
  • Benzimidazoles
  • Protein Kinase Inhibitors
  • Protein Subunits
  • Casein Kinase II