title: CK2α and CK2α' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives.
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.
authors: Department of Molecular Biology, Institute of Biotechnology, The John Paul II Catholic University of Lublin, Al. Krasnicka 102, 20-718 Lublin, Poland.
authors: Monika
authors: M
authors: Janeczko
authors: Andrzej
authors: A
authors: Orzeszko
authors: Zygmunt
authors: Z
authors: Kazimierczuk
authors: Ryszard
authors: R
authors: Szyszka
authors: Andrea
authors: A
authors: Baier
mesh_terms: D001562:Benzimidazoles / Q000494:pharmacology*; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D020134:Catalytic Domain; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D021122:Protein Subunits / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
chemical_list: C475924:4,5,6,7-tetrabromobenzimidazole; C572361:4,5,6,7-tetraiodo-1H-benzimidazole; D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D021122:Protein Subunits; D047390:Casein Kinase II