Mutant p53 targeting by the low molecular weight compound STIMA-1.
Mol Oncol
; 2(1): 70-80, 2008 Jun.
Article
em En
| MEDLINE
| ID: mdl-19383329
ABSTRACT
Reactivation of mutant p53 in human tumor cells should induce cell death by apoptosis and thus eliminate the tumor. Several small molecules that reactivate mutant p53 have been identified. Here we show that STIMA-1, a low molecular weight compound with some structural similarities to the previously identified molecule CP-31398, can stimulate mutant p53 DNA binding in vitro and induce expression of p53 target proteins and trigger apoptosis in mutant p53-expressing human tumor cells. Human diploid fibroblasts are significantly more resistant to STIMA-1 than mutant or wild type p53-carrying tumor cells. STIMA-1 may provide new insights into possible mechanisms of mutant p53 reactivation and thus facilitate the development of novel anticancer drugs that target mutant p53-carrying tumors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos de Vinila
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Proteína Supressora de Tumor p53
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Sistemas de Liberação de Medicamentos
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Quinazolinonas
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Neoplasias
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Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article