Article
Inspecting the structure-activity relationship of protein kinase CK2 inhibitors derived from tetrabromo-benzimidazole.
Chemistry & biology - 1 Nov 2005
Battistutta Roberto, Mazzorana Marco, Sarno Stefania, Kazimierczuk Zygmunt, Zanotti Giuseppe, Pinna Lorenzo A
Abstract excerpt
CK2 is a very pleiotropic protein kinase whose high constitutive activity is suspected to cooperate to neoplasia. Here, the crystal structure of the complexes between CK2 and three selective tetrabromo-benzimidazole derivatives inhibiting CK2 with Ki values between 40 and 400 nM are presented. The ligands bind to the CK2 active site in a different way with respect to the parent compound TBB. They enter more...
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