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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 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. © 2013 Kim et al.

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Details

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: 22 Jun 2021 15:55
URI: http://d-scholarship.pitt.edu/id/eprint/17732

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