STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G2 arrest in the absence of DNA damage

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Title
STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G2 arrest in the absence of DNA damage
Author(s)
Sun Ok Kim; K Sakchaisri; N R Thimmegowda; Nak Kyun SoungJae-Hyuk Jang; Y S Kim; K S Lee; Y T Kwon; Y Asami; Jong Seog Ahn; R Erikson; Bo Yeon Kim
Bibliographic Citation
PLoS One, vol. 8, no. 1, pp. e53908-e53908
Publication Year
2013
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 G2 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.
ISSN
1932-6203
Publisher
Public Library of Science
DOI
http://dx.doi.org/10.1371/journal.pone.0053908
Type
Article
Appears in Collections:
Ochang Branch Institute > Anticancer Agent Research Center > 1. Journal Articles
Ochang Branch Institute > Natural Medicine Research Center > 1. Journal Articles
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