Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog.
Bioorg Med Chem Lett
; 26(7): 1660-3, 2016 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-26923693
ABSTRACT
The G-quadruplexes located in the P1 promoter of B-cell lymphoma-2 (Bcl-2) gene are implicated to regulate Bcl-2 expression. Here, we designed a new pyridostatin analog named PDF, which exhibited high specificity and stabilizing effect toward G-quadruplexes. The luciferase assay demonstrated that PDF could significantly suppress Bcl-2 transcriptional activation in human laryngeal squamous carcinoma cells (Hep-2) cells. Besides, PDF also induced cell apoptosis in vitro assays. These results provide an excellent G-quadruplex specific ligand as an efficient Bcl-2 inhibitor. These results also implicate that PDF may be a potential anticancer drug to head neck cancer.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Picolínicos
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Regulação para Baixo
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Proteínas Proto-Oncogênicas c-bcl-2
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Quadruplex G
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Aminoquinolinas
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Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article