Development of novel Asf1-H3/H4 inhibitors.
Bioorg Med Chem Lett
; 25(4): 963-8, 2015 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-25582598
ABSTRACT
The histone chaperone anti-silencing function 1 (Asf1) has emerged as a promising target for therapeutic intervention for multiple cancers (Cell2006, 127, 458). Asf1 is involved in the packaging of the eukaryotic genome into chromatin, which is essential for normal growth, development, and differentiation, as this regulates all nuclear processes that use DNA as a substrate. Starting from a collection of HTS leads, we identified a series of N-acyl hydrazones as novel inhibitors of the Asf-histone H3/H4 interaction. These compounds represent the first example of inhibitors capable of disrupting the Asf1-H3/H4 complex.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Histonas
/
Proteínas de Ciclo Celular
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article