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

• Published in: Phytochemistry (Oxford) 2017-04, Vol.136, p.39-45
• Main Authors: Baier, Andrea, Galicka, Anna, Nazaruk, Jolanta, Szyszka, Ryszard
• Format: Article
• Language: English
• Subjects: Amino Acid Sequence; Casein Kinase II - antagonists & inhibitors; Casein Kinase II - chemistry; Casein Kinase II - isolation & purification; Casein Kinase II - pharmacology; Catalytic Domain; Chrysoeriol; Flavones - chemistry; Flavones - isolation & purification; Flavones - pharmacology; Flavonoids; Humans; Inhibitors; Molecular Structure; Protein kinase CK2
• ISSN: 0031-9422; 1873-3700
• DOI: 10.1016/j.phytochem.2016.12.018

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. Several flavonoid compounds were tested as potential protein kinase CK2 inhibitor. We identified several substances decreasing the phosphorylating activity. The most promising inhibitor was chrysoeriol (1). [Display omitted] •Several flavonoid compounds are potent CK2 inhibitors.•In most cases the CK2α′ subunit is more effective inhibited than CK2α.•Chrysoeriol was identified as a new and very promising CK2 inhibitor.