A new assay based on fluorescence resonance energy transfer to determine the binding affinity of BCl-xL inhibitors

被引：3

作者：

Feng, Yu ^{[1
]}

Shen, Xu ^{[1
,3
]}

Chen, Kaixian ^{[2
]}

Jiang, Hualiang ^{[2
,3
]}

Liu, Dongxiang ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, Dept Mol Pharmacol, Shanghai 201203, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Drug Design & Discovery, Shanghai 201203, Peoples R China

[3] E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

来源：

BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY | 2008年 / 72卷 / 07期

关键词：

fluorescence resonance energy transfer; Bcl-x(L); inhibitor; binding assay; apoptosis;

D O I：

10.1271/bbb.70735

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We developed a new assay of BCl-x(L) inhibitors based on fluorescence resonance energy transfer that occurs between an AEDANS-labeled Bak-BH3 peptide and three tryptophans in the BH1 and BH2 domains of Bcl-x(L). The method can tolerate up to 5% DMSO, and it was validated with several BCl-x(L) inhibitors. It can be adapted to screen for compounds targeting other Bcl-2 family proteins.

引用

页码：1936 / 1939

页数：4

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