Tethering identifies fragment that yields potent inhibitors of human caspase-1.
Bioorg Med Chem Lett
; 16(3): 559-62, 2006 Feb.
Article
en En
| MEDLINE
| ID: mdl-16274992
ABSTRACT
Disulfide Tethering was applied to the active site of human caspase-1, resulting in the discovery of a novel, tricyclic molecular fragment that selectively binds in S4. This fragment was developed into a class of potent inhibitors of human caspase-1. Several key analogues determined the optimal distance of the tricycle from the catalytic residues, the relative importance of various features of the tricycle, and the importance of the linker.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores Enzimáticos
/
Inhibidores de Caspasas
/
Compuestos Heterocíclicos con 3 Anillos
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2006
Tipo del documento:
Article
País de afiliación:
Estados Unidos