NSC126188, a piperazine alkyl derivative, induces apoptosis via upregulation of RhoB in HeLa cells
- Authors
- SONG KYU PARK; Kiho Lee
- Issue Date
- 10월-2011
- Publisher
- SPRINGER
- Citation
- INVESTIGATIONAL NEW DRUGS, v.29, no.5, pp.853 - 860
- Indexed
- SCIE
SCOPUS
- Journal Title
- INVESTIGATIONAL NEW DRUGS
- Volume
- 29
- Number
- 5
- Start Page
- 853
- End Page
- 860
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/84586
- ISSN
- 0167-6997
- 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 a dagger 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.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - College of Pharmacy > Department of Pharmaceutical Science > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.