Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl alpha-keto aldehydes (glyoxals).
Bioorg Med Chem Lett
; 8(4): 373-8, 1998 Feb 17.
Article
em En
| MEDLINE
| ID: mdl-9871688
ABSTRACT
A series of peptidyl alpha-keto aldehydes (glyoxals) have been synthesised as putative inhibitors of the chymotryptic-like activity of proteasome. The most potent peptides, Cbz-Leu-Leu-Tyr-COCHO and Bz-Leu-Leu-Leu-COCHO, function as slow-binding reversible inhibitors, exhibiting final Ki values of approximately 3.0 nM. These are among the lowest values so far reported for (tri)peptide-based aldehyde-related inhibitors.
Buscar no Google
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cisteína Endopeptidases
/
Quimotripsina
/
Inibidores da Tripsina
/
Glioxal
/
Complexos Multienzimáticos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
1998
Tipo de documento:
Article