Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide.
Bioorg Med Chem Lett
; 11(20): 2779-82, 2001 Oct 22.
Article
en En
| MEDLINE
| ID: mdl-11591522
ABSTRACT
A series of compounds was designed and prepared as inhibitors of interleukin-1beta converting enzyme (ICE), also known as caspase-1. These inhibitors, which employ a diphenyl ether sulfonamide, were designed to improve potency by forming favorable interactions between the diphenyl ether rings and the prime side hydrophobic region. An X-ray crystal structure of a representative member of the diphenyl ether sulfonamide series bound to the active site of caspase-1 was obtained.
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Banco de datos:
MEDLINE
Asunto principal:
Sulfonamidas
/
Inhibidores Enzimáticos
/
Éteres
/
Inhibidores de Caspasas
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2001
Tipo del documento:
Article
País de afiliación:
Estados Unidos