STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.
PLoS One
; 8(1): e53908, 2013.
Article
em En
| MEDLINE
| ID: mdl-23349762
ABSTRACT
STK295900, a small synthetic molecule belonging to a class of symmetric bibenzimidazoles, exhibits antiproliferative activity against various human cancer cell lines from different origins. Examining the effect of STK295900 in HeLa cells indicates that it induces G(2) phase arrest without invoking DNA damage. Further analysis shows that STK295900 inhibits DNA relaxation that is mediated by topoisomerase 1 (Top 1) and topoisomerase 2 (Top 2) in vitro. In addition, STK295900 also exhibits protective effect against DNA damage induced by camptothecin. However, STK295900 does not affect etoposide-induced DNA damage. Moreover, STK295900 preferentially exerts cytotoxic effect on cancer cell lines while camptothecin, etoposide, and Hoechst 33342 affected both cancer and normal cells. Therefore, STK295900 has a potential to be developed as an anticancer chemotherapeutic agent.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzimidazóis
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Dano ao DNA
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DNA Topoisomerases Tipo II
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DNA Topoisomerases Tipo I
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Inibidores da Topoisomerase
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Pontos de Checagem da Fase G2 do Ciclo Celular
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Compostos de Anilina
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article