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STK295900, a Dual Inhibitor of Topoisomerase 1 and 2, Induces G <inf>2</inf> Arrest in the Absence of DNA Damage

Kim, SO and Sakchaisri, K and Thimmegowda, NR and Soung, NK and Jang, JH and Kim, YS and Lee, KS and Kwon, YT and Asami, Y and Ahn, JS and Erikson, RL and Kim, BY (2013) STK295900, a Dual Inhibitor of Topoisomerase 1 and 2, Induces G <inf>2</inf> Arrest in the Absence of DNA Damage. PLoS ONE, 8 (1).

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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. © 2013 Kim et al.


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Item Type: Article
Status: Published
Creators/Authors:
CreatorsEmailPitt UsernameORCID
Kim, SO
Sakchaisri, K
Thimmegowda, NR
Soung, NK
Jang, JH
Kim, YS
Lee, KS
Kwon, YTyok5@pitt.eduYOK5
Asami, Y
Ahn, JS
Erikson, RL
Kim, BY
Date: 29 January 2013
Date Type: Publication
Journal or Publication Title: PLoS ONE
Volume: 8
Number: 1
DOI or Unique Handle: 10.1371/journal.pone.0053908
Schools and Programs: School of Pharmacy > Pharmaceutical Sciences
Refereed: Yes
Other ID: NLM PMC3551932
PubMed Central ID: PMC3551932
PubMed ID: 23349762
Date Deposited: 14 Mar 2013 14:37
Last Modified: 05 Mar 2019 03:55
URI: http://d-scholarship.pitt.edu/id/eprint/17732

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