A liquid chromatography/mass spectrometry-based method for the selection of ATP competitive kinase inhibitors.
J Biomol Screen
; 10(5): 447-55, 2005 Aug.
Article
em En
| MEDLINE
| ID: mdl-16093554
ABSTRACT
The currently approved kinase inhibitors for therapeutic uses and a number of kinase inhibitors that are undergoing clinical trials are directed toward the adenosine triphosphate (ATP) binding site of protein kinases. The 5'-fluorosulfonylbenzoyl 5'-adenosine (FSBA) is an ATP-affinity reagent that covalently modifies a conserved lysine present in the nucleotide-binding site of most kinases. The authors have developed a liquid chromatography/mass spectrometry-based method to monitor binding of ATP competitive protein kinase inhibitors using FSBA as a nonselective activity-based probe for protein kinases. Their method provides a general, rapid, and reproducible means to screen and validate selective ATP competitive inhibitors of protein kinases.
Buscar no Google
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Espectrometria de Massas
/
Cromatografia Líquida
/
Avaliação Pré-Clínica de Medicamentos
/
Inibidores Enzimáticos
Tipo de estudo:
Prognostic_studies
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article