Selective bisubstrate inhibitors with sub-nanomolar affinity for protein kinase Pim-1.
ChemMedChem
; 8(6): 909-13, 2013 Jun.
Article
en En
| MEDLINE
| ID: mdl-23616352
ABSTRACT
Potent and selective The unique nature of the ATP binding pocket structure of Pim family protein kinases (PKs) was used for the development of bisubstrate inhibitors and a fluorescent probe with sub-nanomolar affinity. Conjugates of arginine-rich peptides with two ATP mimetic scaffolds were synthesized and tested as inhibitors of Pim-1. Against a panel of 124 protein kinases, a novel ARC-PIM conjugate selectively inhibited PKs of the Pim family.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores de Proteínas Quinasas
/
Nanoestructuras
/
Proteínas Proto-Oncogénicas c-pim-1
Idioma:
En
Revista:
ChemMedChem
Asunto de la revista:
FARMACOLOGIA
/
QUIMICA
Año:
2013
Tipo del documento:
Article
País de afiliación:
Estonia