Design, validation and efficacy of bisubstrate inhibitors specifically affecting ecto-CK2 kinase activity.

@article{Cozza2015DesignVA,
  title={Design, validation and efficacy of bisubstrate inhibitors specifically affecting ecto-CK2 kinase activity.},
  author={Giorgio Cozza and Sofia Zanin and Stefania Sarno and Elena Costa and Cristina Girardi and Giovanni Ribaudo and Mauro Salvi and Giuseppe Zagotto and Maria Ruzzene and Lorenzo A Pinna},
  journal={The Biochemical journal},
  year={2015},
  volume={471 3},
  pages={415-30}
}
By derivatizing the purely competitive CK2 inhibitor N1-(4,5,6,7-tetrabromo-1H-benzimidazol-2-yl)-propane-1,3-diamine (K137) at its 3-amino position with a peptidic fragment composed of three or four glutamic or aspartic acid residues, a new family of bisubstrate inhibitors has been generated whose ability to simultaneously interact with both the ATP and the phosphoacceptor substrate-binding sites has been probed by running mixed competition kinetics and by mutational mapping of the kinase… CONTINUE READING
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