title: Electrochemical screening of the indole/quinolone derivatives as potential protein kinase CK2 inhibitors.
abstract: An electrochemical method based on the bioorganometallic Fc-ATP cosubstrate for kinase-catalyzed phosphorylation reactions was used for monitoring casein kinase 2 (CK2) phosphorylations in the absence and presence of five indole/quinolone-based potential inhibitors. Fc-phosphorylation of immobilized peptide RRRDDDSDDD on Au surfaces resulted in a current density at approximately 460 ± 10 mV. An electrochemical redox signal was significantly decreased in the presence of inhibitors. In addition, the electrochemical signal was concentration dependent with respect to the potential inhibitors 1 to 5, which proved to be viable CK2 drug targets with estimated IC₅₀ values in the nanomolar range.
authors.affiliation: Department of Physical and Environmental Sciences, University of Toronto at Scarborough, Toronto, Ontario M1C 1A4, Canada.
authors.forename: Sanela
authors.initials: S
authors.lastname: Martić
authors.forename: Stefanie
authors.initials: S
authors.lastname: Tackenburg
authors.forename: Yaroslav
authors.initials: Y
authors.lastname: Bilokin
authors.forename: Andriy
authors.initials: A
authors.lastname: Golub
authors.forename: Volodymyr
authors.initials: V
authors.lastname: Bdzhola
authors.forename: Sergiy
authors.initials: S
authors.lastname: Yarmoluk
authors.forename: Heinz-Bernhard
authors.initials: HB
authors.lastname: Kraatz
mesh_terms: D015374:Biosensing Techniques; D047390:Casein Kinase II / Q000037:antagonists & inhibitors*; D055664:Electrochemical Techniques; D007211:Indoles / Q000302:isolation & purification / Q000494:pharmacology*; D010084:Oxidation-Reduction; D047428:Protein Kinase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D015363:Quinolones / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D007211:Indoles; D047428:Protein Kinase Inhibitors; D015363:Quinolones; D047390:Casein Kinase II