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CR229, a novel derivative of beta-carbolin-1-one, induces cell cycle arrest and apoptosis in HeLa cells via p53 activation

Title
CR229, a novel derivative of beta-carbolin-1-one, induces cell cycle arrest and apoptosis in HeLa cells via p53 activation
Author
이철훈
Keywords
DEPENDENT KINASE INHIBITOR; 3-ARYL BETA-CARBOLIN-1-ONES; INDUCTION; CHK1; MDM2
Issue Date
2007-09
Publisher
BLACKWELL PUBLISHING
Citation
CANCER SCIENCE, v. 98, No. 9, Page. 1402-1407
Abstract
In the course of screening for novel anticancer compounds, CR229 (6-Bromo-2,3,4,9-tetrahydro-carbolin-1-one), a novel derivative of beta-carbolin-1-one, was generated as a new scaffold candidate. For the first time, the authors demonstrate that CR229 inhibited the growth of HeLa cells by the induction of cell cycle arrest and apoptosis. Analysis of flow cytometry and western blots of HeLa cells treated with 2.5 mu M CR229 revealed an appreciable cell cycle arrest in the G1, G2/M phase and apoptotic induction via the p53-dependent pathway. Furthermore, the release of cytochrome c from mitochondria was detected using confocal microscopy in HeLa cells treated with CR229. Accordingly, these data demonstrate that the anticancer activity of CR229 is associated with: (i) the down-regulation of cyclins and cyclin-dependent kinase; (ii) the induction of p53, p21, and p16; and (iii) the activation of caspase-3.
URI
https://onlinelibrary.wiley.com/doi/full/10.1111/j.1349-7006.2007.00552.xhttp://repository.hanyang.ac.kr/handle/20.500.11754/106915
ISSN
1347-9032
DOI
10.1111/j.1349-7006.2007.00552.x
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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