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Structure-based discovery of small molecules targeting different surfaces of protein-kinase CK2.

Authors :
Prudent R
Sautel CF
Cochet C
Source :
Biochimica et biophysica acta [Biochim Biophys Acta] 2010 Mar; Vol. 1804 (3), pp. 493-8. Date of Electronic Publication: 2009 Sep 18.
Publication Year :
2010

Abstract

Protein kinase CK2 is an unfavorable pronostic marker in several cancers and has consequently emerged as a relevant therapeutic target. Several classes of ATP-competitive inhibitors have been identified, showing variable effectiveness. The molecular architecture of this multisubunit enzyme could offer alternative strategies to develop small molecule inhibitors targeting different surfaces of the kinase. Polyoxometalates were identified as original CK2 inhibitors targeting key structural elements located outside the active site. In addition, the CK2 subunit interface represents an exosite distinct from the catalytic cavity that can be targeted by peptides or small molecules to achieve functional effects.<br /> (Copyright 2009 Elsevier B.V. All rights reserved.)

Details

Language :
English
ISSN :
0006-3002
Volume :
1804
Issue :
3
Database :
MEDLINE
Journal :
Biochimica et biophysica acta
Publication Type :
Academic Journal
Accession number :
19766740
Full Text :
https://doi.org/10.1016/j.bbapap.2009.09.003