Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.
J Med Chem
; 55(12): 5982-6, 2012 Jun 28.
Article
em En
| MEDLINE
| ID: mdl-22686657
ABSTRACT
A series of dipeptide nitriles with different P3 substituents was designed to explore the S3 binding pocket of cathepsin S. Racemic 7-16 and the enantiopure derivative (R)-22 proved to be potent inhibitors of human cathepsin S and exhibited notable selectivity over human cathepsins L, K, and B. Inhibition of cathepsin F, the functional synergist of cathepsin S, was not observed. The azadipeptide analogue of 22, compound 26, was highly potent but nonselective.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Catepsinas
/
Catepsina F
/
Proteólise
/
Nitrilas
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article