Electrochemical screening of the indole/quinolone derivatives as potential protein kinase CK2 inhibitors
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...
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| Veröffentlicht in: | Analytical biochemistry 2012-02, Vol.421 (2), p.617-621 |
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| container_end_page | 621 |
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| container_issue | 2 |
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| container_title | Analytical biochemistry |
| container_volume | 421 |
| creator | Martić, Sanela Tackenburg, Stefanie Bilokin, Yaroslav Golub, Andriy Bdzhola, Volodymyr Yarmoluk, Sergiy Kraatz, Heinz-Bernhard |
| description | 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±10mV. 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. |
| doi_str_mv | 10.1016/j.ab.2011.11.017 |
| format | Article |
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Fc-phosphorylation of immobilized peptide RRRDDDSDDD on Au surfaces resulted in a current density at approximately 460±10mV. An electrochemical redox signal was significantly decreased in the presence of inhibitors. 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Fc-phosphorylation of immobilized peptide RRRDDDSDDD on Au surfaces resulted in a current density at approximately 460±10mV. 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.</description><subject>Biosensing Techniques</subject><subject>Biosensor</subject><subject>Casein Kinase II - antagonists & inhibitors</subject><subject>drugs</subject><subject>Electrochemical Techniques</subject><subject>Electrochemistry</subject><subject>Ferrocene</subject><subject>gold</subject><subject>Indoles - isolation & purification</subject><subject>Indoles - pharmacology</subject><subject>Inhibitor</subject><subject>inhibitory concentration 50</subject><subject>monitoring</subject><subject>non-specific serine/threonine protein kinase</subject><subject>Oxidation-Reduction</subject><subject>phosphorylation</subject><subject>Protein Kinase Inhibitors - isolation & purification</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Protein kinases</subject><subject>Quinolones - isolation & purification</subject><subject>Quinolones - pharmacology</subject><subject>screening</subject><issn>0003-2697</issn><issn>1096-0309</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kUFPGzEQRq2qFaSUe0_gG6cNYzvrXfdWRdBWReqBcra83lkyYWMHexOJf4-jQG-VRrIP7_tsvWHsq4C5AKGv13PXzSUIMS8DovnAZgKMrkCB-chmAKAqqU1zyj7nvIYCLmp9wk6lFE1rwMzY6mZEP6XoV7gh70aefUIMFB55HPi0Qk6hjyNeP-8oxDEG5D0m2ruJ9pi5y3wbJwwTleg2lSsF_kTBZeTL37KEV9TRFFP-wj4Nbsx4_naesYfbm7_Ln9Xdnx-_lt_vKq8aNVWoayklaulbpRuoW6-w74STAqR2rlkoKaFDaTS42izqznQDLqAvcFu3pldn7OrYW37zvMM82Q1lj-PoAsZdtkaC0hqUKSQcSZ9izgkHu020cenFCrAHvXZtXWcPem2ZordELt7Kd90G-3-Bd58FuDwCg4vWPSbK9uG-NOiyCtEK0Rbi25HAImFPmGz2hMFjT6lswvaR_v_-K5e0k1M</recordid><startdate>20120215</startdate><enddate>20120215</enddate><creator>Martić, Sanela</creator><creator>Tackenburg, Stefanie</creator><creator>Bilokin, Yaroslav</creator><creator>Golub, Andriy</creator><creator>Bdzhola, Volodymyr</creator><creator>Yarmoluk, Sergiy</creator><creator>Kraatz, Heinz-Bernhard</creator><general>Elsevier Inc</general><scope>FBQ</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20120215</creationdate><title>Electrochemical screening of the indole/quinolone derivatives as potential protein kinase CK2 inhibitors</title><author>Martić, Sanela ; 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| fulltext | fulltext |
| identifier | ISSN: 0003-2697 |
| ispartof | Analytical biochemistry, 2012-02, Vol.421 (2), p.617-621 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Biosensing Techniques Biosensor Casein Kinase II - antagonists & inhibitors drugs Electrochemical Techniques Electrochemistry Ferrocene gold Indoles - isolation & purification Indoles - pharmacology Inhibitor inhibitory concentration 50 monitoring non-specific serine/threonine protein kinase Oxidation-Reduction phosphorylation Protein Kinase Inhibitors - isolation & purification Protein Kinase Inhibitors - pharmacology Protein kinases Quinolones - isolation & purification Quinolones - pharmacology screening |
| title | Electrochemical screening of the indole/quinolone derivatives as potential protein kinase CK2 inhibitors |
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