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Title 

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

Authors 

Bo Kyung KimD M KimKyung Sook ChungSong Kyu ParkS J ChoiA SongKiho LeeChang Woo LeeK B SongG HanJ SimonH M KimMi Sun Won

Publisher 

Springer Verlag (Germany)

Issue Date 

2011

Citation 

Investigational New Drugs, vol. 29, no. 5, pp. 853-860

Keywords 

Anti-cancer compoundApoptosisNSC126188Piperazine alkyl derivativeRhoB

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.

ISSN 

0167-6997

Link 

http://dx.doi.org/10.1007/s10637-010-9433-3

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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