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Inhibitory Effects of Dithiolo-thione Derivative SWU-20009 on Akt Activity  

고종희 (일동제약주식회사 중앙연구소)
연승우 (일동제약주식회사 중앙연구소)
이홍섭 (일동제약주식회사 중앙연구소)
김태용 (일동제약주식회사 중앙연구소)
노동윤 (서울여자대학교 화학과)
신경순 (서울여자대학교 화학과)
홍순광 (명지대학교 생물학과)
강상순 (충북대학교 과학교육과)
Publication Information
YAKHAK HOEJI / v.48, no.2, 2004 , pp. 105-110 More about this Journal
Abstract
Akt (or Protein Kinase B; PKB) is a serine/threonine kinase and is activated by phosphoinositide 3-kinase (PI3K) pathway. Recent evidence indicates that the abnormal activities or expression of Akt is closely associated with cancer, diabetes and neuro-degenerative diseases. These findings mean that Akt is likely to be a new therapeutic target for the treatment of disease. Here, we screened the effects of dithiolo-dithione derivatives such as SWU-20004, SWU-20009 and SWU-20025 on Akt activities. Among these compounds, only SWU-20009 (2-Thioxo-[1,3]dithiolo[4,5- $\beta$][1,4]dithiine-5,6-dicarboxylic acid dimethyl ester) inhibited the growth of KATOIII cell at micromolar range of concentration. Further investigation also revealed that SWU-20009 inhibited cellular Akt activity and induced apoptotic cell death.
Keywords
Akt; PKB; kinase; inhibitor; cancer;
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