Document Detail

YL326, a novel small-molecule inhibitor of cell-cycle progression, induces G(0)/G(1) phase arrest and apoptosis in human hepatic carcinoma cells.
MedLine Citation:
PMID:  22542944     Owner:  NLM     Status:  Publisher    
We previously reported the potential of a novel small molecule 3-amino-6-(3-methoxyphenyl)thieno[2.3-b]pyridine-2-carboxamide (YL326) as an anticancer agent. In the present study, we investigated the anticancer effects and possible mechanisms of YL326 in vitro. We found that YL326 treatment significantly inhibited human hepatic carcinoma cell proliferation in vitro, and the HepG2 cell line was the most sensitive to its treatment. The inhibition of cell proliferation correlated with G(0)/G(1) phase arrest, which was followed by apoptotic cell death. The YL326-mediated cell-cycle arrest was associated with the downregulation of cyclin-dependent kinase (CDK) 2, CDK4 and CDK6 but not cyclin D1 or cyclin E. The phosphorylation of the retinoblastoma protein (Rb) was also observed. YL326 treatment induced apoptotic cell death via the activation of PARP, caspase-3, caspase-9 and Bax as well as the downregulation of Bcl-2. The expression levels of p53 and p21 were also induced by YL326 treatment. Moreover, YL326 treatment was well tolerated. In conclusion, YL326, a novel cell-cycle inhibitor, notably inhibits HepG2 cell proliferation through the induction of G(0)/G(1) phase arrest and subsequent apoptosis. Its potential as a candidate anticancer agent warrants further investigation.
Yuanyuan Han; Haiyun He; Feng Peng; Jiyan Liu; Xiaoyun Dai; Hongjun Lin; Youzhi Xu; Tian Zhou; Yongqiu Mao; Gang Xie; Shengyong Yang; Luoting Yu; Li Yang; Yinglan Zhao
Related Documents :
22892544 - O6-methylguanine dna lesions induce an intra-s-phase arrest from which cells exit into ...
21119604 - Microrna-192 and -215 are upregulated in human gastric cancer in vivo and suppress alca...
22634474 - Granular cell ameloblastoma showing desmoplasia.
20608784 - Newer combination antifungal therapies for invasive aspergillosis.
19720874 - Tor-mediated autophagy regulates cell death in drosophila neurodegenerative disease.
9550714 - Bundle sheath cells and cell-specific plastid development in arabidopsis leaves.
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-4-21
Journal Detail:
Title:  Biochemical and biophysical research communications     Volume:  -     ISSN:  1090-2104     ISO Abbreviation:  -     Publication Date:  2012 Apr 
Date Detail:
Created Date:  2012-4-30     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0372516     Medline TA:  Biochem Biophys Res Commun     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012. Published by Elsevier Inc.
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Biphasic effect of danazol on human vascular endothelial cell permeability and f-actin cytoskeleton ...
Next Document:  CNTF-mediated preactivation of astrocytes attenuates neuronal damage and epileptiform activity in ex...