Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Bioorg Med Chem Lett
; 22(8): 2968-72, 2012 Apr 15.
Article
en En
| MEDLINE
| ID: mdl-22437115
ABSTRACT
A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Quinolinas
/
Compuestos Heterocíclicos de 4 o más Anillos
/
Isoxazoles
/
Proteínas del Tejido Nervioso
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
Idioma:
En
Año:
2012
Tipo del documento:
Article