Inhibition of protein kinase CK2 expression and activity blocks tumor cell growth.
Mol Cell Biochem
; 333(1-2): 159-67, 2010 Jan.
Article
em En
| MEDLINE
| ID: mdl-19629644
ABSTRACT
Protein kinase CK2 (CK2) is a highly conserved and ubiquitous serine/threonine kinase. It is a multifunctional and pleiotropic protein kinase implicated in the regulation of cell proliferation, survival, and differentiation. Deregulation of CK2 is observed in a wide variety of tumors. It has been the focus of intensive research efforts to establish the cause-effect relationship between CK2 and neoplastic growth. Here, we further validate the role of CK2 in cancer cell growth using siRNA approach. We also screened a library of more than 200,000 compounds and identified several molecules, which inhibit CK2 with IC(50) < 1 microM. The binding mode of a representative compound with maize CK2 was determined. In addition, the cellular activity of the compounds was demonstrated by their inhibition of phosphorylation of PTEN Ser370 in HCT116 cells. Treatment of a variety of cancer cell lines with the newly identified CK2 inhibitor significantly blocked cell growth with IC(50)s as low as 300 nM.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Caseína Quinase II
/
Proliferação de Células
/
Inibidores Enzimáticos
Idioma:
En
Revista:
Mol Cell Biochem
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Estados Unidos