Selected flavonoid compounds as promising inhibitors of protein kinase CK2α and CK2α', the catalytic subunits of CK2

Phytochemistry. 2017 Apr:136:39-45. doi: 10.1016/j.phytochem.2016.12.018. Epub 2016 Dec 30.

Abstract

CK2 is a ubiquitous protein kinase involved in many cell functions. During the last years it became an interesting target in cancer research. A series of flavonoid compounds was tested as inhibitors of protein kinase CK2. Several substances were found to be highly active against both catalytic subunits with IC50 values below 1 μM in case of CK2α'. The most promising inhibitor we identified is chrysoeriol with IC50 values of 250 and 34 nM for CK2α and CK2α', respectively.

Keywords: Chrysoeriol; Flavonoids; Inhibitors; Protein kinase CK2.

MeSH terms

  • Amino Acid Sequence
  • Casein Kinase II / antagonists & inhibitors*
  • Casein Kinase II / chemistry
  • Casein Kinase II / isolation & purification
  • Casein Kinase II / pharmacology
  • Catalytic Domain
  • Flavones / chemistry
  • Flavones / isolation & purification*
  • Flavones / pharmacology*
  • Humans
  • Molecular Structure

Substances

  • Flavones
  • CSNK2A1 protein, human
  • Casein Kinase II
  • chrysoeriol