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Mechanisms of anti-leukemic activity of the Bcl-2 homology domain-3 mimetic S1.

Biomed. Pharmacother.. 2013; 
LiuYubo,LiZhiqiang,SongTing,XueZuguang,ZhangZhi
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摘要

Most of leukemia exhibits inherent overexpressed Bcl-2-like proteins. Small molecule S1 is a BH3 mimetic discovered by our previous studies. The aim of this study is to dissect the details of apoptosis signaling induced by S1 in acute myeloid leukaemia (AML) cells and to provide a molecular basis for the use of S1 in AML treatment. The anti-leukemic activity of S1 was evaluated in three cultured AML cell lines and eight patient samples. S1 induced apoptosis via an intrinsic apoptosis pathway by the disruption of protein-protein interactions of Bcl-2 family members and triggered the activation of Bax and Bak in AML cells. For the first time, we report that S1 can release pro-apoptotic protein from Bcl-XL and s... More

关键词

AML,BH3 mimetic,Bak-depen