STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.

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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Main Authors: Sun-Ok Kim, Krisada Sakchaisri, N R Thimmegowda, Nak Kyun Soung, Jae-Hyuk Jang, Young Sang Kim, Kyung Sang Lee, Yong Tae Kwon, Yukihiro Asami, Jong Seog Ahn, Raymond Leo Erikson, Bo Yeon Kim
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2013-01-01
Series:PLoS ONE
Online Access:http://europepmc.org/articles/PMC3551932?pdf=render
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spelling doaj-63f6f3a1e25b4d7c94e5ff019b4c02742020-11-24T22:25:46ZengPublic Library of Science (PLoS)PLoS ONE1932-62032013-01-0181e5390810.1371/journal.pone.0053908STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.Sun-Ok KimKrisada SakchaisriN R ThimmegowdaNak Kyun SoungJae-Hyuk JangYoung Sang KimKyung Sang LeeYong Tae KwonYukihiro AsamiJong Seog AhnRaymond Leo EriksonBo Yeon KimSTK295900, 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.http://europepmc.org/articles/PMC3551932?pdf=render
collection DOAJ
language English
format Article
sources DOAJ
author Sun-Ok Kim
Krisada Sakchaisri
N R Thimmegowda
Nak Kyun Soung
Jae-Hyuk Jang
Young Sang Kim
Kyung Sang Lee
Yong Tae Kwon
Yukihiro Asami
Jong Seog Ahn
Raymond Leo Erikson
Bo Yeon Kim
spellingShingle Sun-Ok Kim
Krisada Sakchaisri
N R Thimmegowda
Nak Kyun Soung
Jae-Hyuk Jang
Young Sang Kim
Kyung Sang Lee
Yong Tae Kwon
Yukihiro Asami
Jong Seog Ahn
Raymond Leo Erikson
Bo Yeon Kim
STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.
PLoS ONE
author_facet Sun-Ok Kim
Krisada Sakchaisri
N R Thimmegowda
Nak Kyun Soung
Jae-Hyuk Jang
Young Sang Kim
Kyung Sang Lee
Yong Tae Kwon
Yukihiro Asami
Jong Seog Ahn
Raymond Leo Erikson
Bo Yeon Kim
author_sort Sun-Ok Kim
title STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.
title_short STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.
title_full STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.
title_fullStr STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.
title_full_unstemmed STK295900, a dual inhibitor of topoisomerase 1 and 2, induces G(2) arrest in the absence of DNA damage.
title_sort stk295900, a dual inhibitor of topoisomerase 1 and 2, induces g(2) arrest in the absence of dna damage.
publisher Public Library of Science (PLoS)
series PLoS ONE
issn 1932-6203
publishDate 2013-01-01
description 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.
url http://europepmc.org/articles/PMC3551932?pdf=render
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