A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCV NS3 protease.
Bioorg Med Chem Lett
; 12(4): 701-4, 2002 Feb 25.
Article
en En
| MEDLINE
| ID: mdl-11844705
ABSTRACT
The difluoromethyl group was designed by computational chemistry methods as a mimetic of the canonical P1 cysteine thiol for inhibitors of the hepatitis C virus NS3 protease. This modification led to the development of competitive, non-covalent inhibitor 4 (K(i) 30 nM) and reversible covalent inhibitors (6, K(i) 0.5 nM; and 8 K*(i) 10 pM).
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Oligopéptidos
/
Modelos Moleculares
/
Proteínas no Estructurales Virales
/
Hepacivirus
/
Cisteína
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2002
Tipo del documento:
Article
País de afiliación:
Italia