STK295900, a Dual Inhibitor of Topoisomerase 1 and 2, Induces G(2) Arrest in the Absence of DNA Damage

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 D...

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Detalles Bibliográficos
Autores principales: Kim, Sun-Ok, Sakchaisri, Krisada, N. R., Thimmegowda, Soung, Nak Kyun, Jang, Jae-Hyuk, Kim, Young Sang, Lee, Kyung Sang, Kwon, Yong Tae, Asami, Yukihiro, Ahn, Jong Seog, Erikson, Raymond Leo, Kim, Bo Yeon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2013
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3551932/
https://www.ncbi.nlm.nih.gov/pubmed/23349762
http://dx.doi.org/10.1371/journal.pone.0053908
Descripción
Sumario: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.

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