Dithiolo-thione 계열 유도체 SWU-20009의 Akt 활성 저해 효과

• 영문명: Inhibitory Effects of Dithiolo-thione Derivative SWU-20009 on Akt Activity
• 발행기관: 대한약학회
• 저자명: 고종희(Jong Hee Ko) 연승우(Seung Woo Yeon) 이홍섭(Hong Sub Lee) 김태용(Tae Yong Kim) 노동윤(Dong Youn Noh) 신경순(Kyong Soon Shin) 홍순광(Soon Kwang Hong) 강상순(Sang Sun Kang)
• 간행물 정보: 『약학회지』제48권 제2호 (2004년), 105~110쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2004.04.30

영문 초록

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 cancers 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-20709 and SWU-20025 on Akt activities. Among these compounds, only SWU-20009 (2-Thioxo - [1,3]dithiolo[4,5- β][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.

키워드

Akt PKB, kinase inhibitor cancer