NSC126188, a piperazine alkyl derivative, induces apoptosis via upregulation of RhoB in HeLa cells

Cited 9 time in scopus
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Title
NSC126188, a piperazine alkyl derivative, induces apoptosis via upregulation of RhoB in HeLa cells
Author(s)
Bo Kyung Kim; D M Kim; Kyung Sook Chung; Song Kyu Park; S J Choi; A Song; Kiho Lee; Chang Woo Lee; K B Song; G Han; J Simon; H M Kim; Mi Sun Won
Bibliographic Citation
Investigational New Drugs, vol. 29, no. 5, pp. 853-860
Publication Year
2011
Abstract
We describe here a piperazine alkyl derivative, NSC126188, which induced apoptosis of HeLa cells by upregulating RhoB expression. NSC126188 caused multi-septation of fission yeast and hypersensitized a {increment}rho3 mutant, which implicates the involvement of functional human homolog RhoB. The treatment of cells with NSC126188 induced apoptosis and a dramatic increase in RhoB expression. In addition, RhoB knockdown using siRNA rescued cells from apoptosis, indicating a crucial role of RhoB in NSC126188-induced apoptosis. In a reporter assay using luciferase and EGFP under control of the RhoB promoter, NSC126188 increased both luciferase activity and the expression of EGFP, implicating transcriptional activation of RhoB by NSC126188. Furthermore, NSC126188 demonstrated in vivo anti-tumor activity, inhibiting tumor growth by 66.8% in a nude mouse xenograft using PC-3 human prostate cancer cells. These results suggest that NSC126188 is a potential lead compound and that upregulation of RhoB is associated with NSC126188-induced apoptosis.
Keyword
Anti-cancer compoundApoptosisNSC126188Piperazine alkyl derivativeRhoB
ISSN
0167-6997
Publisher
Springer
DOI
http://dx.doi.org/10.1007/s10637-010-9433-3
Type
Article
Appears in Collections:
Division of Biomedical Research > Personalized Genomic Medicine Research Center > 1. Journal Articles
Division of Research on National Challenges > 1. Journal Articles
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
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