Selected flavonoid compounds as promising inhibitors of protein kinase CK2α and CK2α′, the catalytic subunits of CK2. (April 2017)

• Record Type: Journal Article
• Authors: Baier, Andrea; Galicka, Anna; Nazaruk, Jolanta; Szyszka, Ryszard
• Is Part Of: Phytochemistry. Volume 136(2017)
• Page Start: 39
• Page End: 45
• Publication Date: 2017-04
• Subjects: Protein kinase CK2 -- Flavonoids -- Inhibitors -- Chrysoeriol; Botanical chemistry -- Periodicals; Biochemistry -- Periodicals; Botany -- Periodicals; Chimie végétale -- Périodiques; 572.2
• DOI: 10.1016/j.phytochem.2016.12.018
• Languages: English
• ISSNs: 0031-9422

Abstract

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. Graphical abstract: 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 ). Highlights: 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.