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Structure-based discovery of small molecules targeting different surfaces of protein-kinase CK2.
- 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.)
- Subjects :
- Animals
Biomarkers, Tumor chemistry
Biomarkers, Tumor metabolism
Casein Kinase II chemistry
Casein Kinase II metabolism
Catalytic Domain
Humans
Neoplasms drug therapy
Protein Synthesis Inhibitors therapeutic use
Tungsten Compounds therapeutic use
Biomarkers, Tumor antagonists & inhibitors
Casein Kinase II antagonists & inhibitors
Neoplasms enzymology
Protein Synthesis Inhibitors chemistry
Tungsten Compounds chemistry
Subjects
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