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Multisite-directed inhibitors of protein kinase CK2: new challenges

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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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Correspondence to Ana Ramos or Beatriz de Pascual-Teresa.

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Świder, R., Masłyk, M., Martín-Santamaría, S. et al. Multisite-directed inhibitors of protein kinase CK2: new challenges. Mol Cell Biochem 356, 117–119 (2011). https://doi.org/10.1007/s11010-011-0962-7

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  • DOI: https://doi.org/10.1007/s11010-011-0962-7

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