Studies of C-terminal naphthoquinone dipeptides as 20S proteasome inhibitors.
J Enzyme Inhib Med Chem
; 31(3): 456-63, 2016.
Article
em En
| MEDLINE
| ID: mdl-25942361
ABSTRACT
The ubiquitin proteasome pathway is crucial in regulating many processes in the cell. Modulation of proteasome activities has emerged as a powerful strategy for potential therapies against much important pathologies. In particular, specific inhibitors may represent a useful tool for the treatment of tumors. Here, we report studies of a new series of peptide-based analogues bearing a naphthoquinone pharmacophoric unit at the C-terminal position. Some derivatives showed inhibition in the µM range of the post-acidic-like and chymotrypsin-like active sites of the proteasome.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Naftoquinonas
/
Complexo de Endopeptidases do Proteassoma
/
Dipeptídeos
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Inibidores de Proteassoma
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Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
J Enzyme Inhib Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2016
Tipo de documento:
Article