Structure-based discovery of small molecules targeting different surfaces of protein-kinase CK2.
Biochim Biophys Acta
; 1804(3): 493-8, 2010 Mar.
Article
em En
| MEDLINE
| ID: mdl-19766740
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Inibidores da Síntese de Proteínas
/
Biomarcadores Tumorais
/
Compostos de Tungstênio
/
Caseína Quinase II
/
Neoplasias
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article