Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
J Med Chem
; 58(8): 3611-25, 2015 Apr 23.
Article
en En
| MEDLINE
| ID: mdl-25849762
ABSTRACT
A weak screening hit with suboptimal physicochemical properties was optimized against PFKFB3 kinase using critical structure-guided insights. The resulting compounds demonstrated high selectivity over related PFKFB isoforms and modulation of the target in a cellular context. A selected example demonstrated exposure in animals following oral dosing. Examples from this series may serve as useful probes to understand the emerging biology of this metabolic target.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Diseño de Fármacos
/
Fosfofructoquinasa-2
/
Inhibidores de Proteínas Quinasas
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2015
Tipo del documento:
Article