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. 2011 Oct;356(1-2):117-9.
doi: 10.1007/s11010-011-0962-7. Epub 2011 Jul 13.

Multisite-directed inhibitors of protein kinase CK2: new challenges

Robert Świder  1 , Maciej Masłyk, Sonsoles Martín-Santamaría, Ana Ramos, Beatriz de Pascual-Teresa
Affiliations

Multisite-directed inhibitors of protein kinase CK2: new challenges

Robert Świder et al. Mol Cell Biochem. 2011 Oct.

Abstract

New 4,5,6,7-tetrabromo benzotriazole derivatives have been synthesized, and their activities against CK2 have been tested. A click chemistry approach based on the copper-catalyzed azide-alkyne cycloaddition has been utilized to connect benzotriazoles, which efficiently interact with the ATP-binding site, to other subunits designed to simultaneously bind to the active and the substrate-binding sites of the enzyme. Docking studies allowed us to identify key interactions between CK2 and the designed ligands, which will be useful to optimize this series of multisite-directed inhibitors.

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