Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins.
Bioorg Med Chem
; 20(5): 1779-93, 2012 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-22304848
ABSTRACT
The tenovins are small molecule inhibitors of the NAD(+)-dependent family of protein deacetylases known as the sirtuins. There remains considerable interest in inhibitors of this enzyme family due to possible applications in both cancer and neurodegenerative disease therapy. Through the synthesis of novel tenovin analogues, further insights into the structural requirements for activity against the sirtuins in vitro are provided. In addition, the activity of one of the analogues in cells led to an improved understanding of the function of SirT1 in cells.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sirtuínas
/
Inibidores de Histona Desacetilases
Limite:
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article