CK2alpha and CK2alpha' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives.

Article Details

Citation

Copy to clipboard

Janeczko M, Orzeszko A, Kazimierczuk Z, Szyszka R, Baier A

CK2alpha and CK2alpha' 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.

PubMed ID

22115617 [ View in PubMed

]

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. CK2alpha' was up to 6 times more sensitive to the studied compounds than CK2alpha. 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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
DIMETHYL-(4,5,6,7-TETRABROMO-1H-BENZOIMIDAZOL-2-YL)-AMINE	Casein kinase II subunit alpha	Ki (nM)	97	N/A	N/A	Details
DIMETHYL-(4,5,6,7-TETRABROMO-1H-BENZOIMIDAZOL-2-YL)-AMINE	Casein kinase II subunit alpha	Ki (nM)	139	N/A	N/A	Details