IR@PKUHSC  > 北京大学临床肿瘤学院  > 肿瘤放疗科
学科主题药学
Capillary electrophoresis for screening of 20S proteasome inhibitors
Chen, Wenjing1; Mou, Ke2; Xu, Bo3; Ling, Xiaomei1; Cui, Jingrong3; Xu, Ping2
关键词20s Proteasome Enzyme Inhibitor Mg132 Mg115 Peptidyl Vinyl Ester Capillary Electrophoresis
刊名ANALYTICAL BIOCHEMISTRY
2009-11-01
DOI10.1016/j.ab.2009.07.020
394期:1页:62-67
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Analytical
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]MULTICATALYTIC PROTEINASE COMPLEX ; CHYMOTRYPSIN-LIKE ACTIVITY ; FLUORESCENCE DETECTION ; S PROTEASOME ; BORONIC ACID ; DEGRADATION ; ASSAY ; METABOLISM ; SUBSTRATE ; ALDEHYDES
英文摘要

A method for studying 20S proteasome inhibitors by capillary electrophoresis (CE) has been developed. Proteasome plays a fundamental role in degrading key regulatory proteins. The 20S proteasome can degrade intrinsically disordered proteins in an ATP-independent manner without additional "helper" molecules. The discovery of new proteasome inhibitors with little or no toxicity is highly desirable in anticancer therapy. In this study, the inhibitory effects of MG132 and MG115 on the 20S proteasome were evaluated by CE for the first time. The optimized CE conditions were as follows: fused-silica capillary of 30 cm effective length and 75 mu m internal diameter, pressure injection of 0.5 psi for 5 s, 50 mM Hepes buffer (pH 7.6) with 2% dimethyl sulfoxide, constant voltage of 20 kV, and detection wavelength at 340 nm. Also, the new method was used to study the inhibitory effects of 30 novel peptidyl vinyl ester derivatives of MG132. The 50% inhibition concentrations (IC(50) values) of MG132 and MG115 were 40.0 and 84.7 nM, respectively. Two new compounds, XP32 and XP35, showed considerable inhibitory effects on the 20S proteasome. When the concentrations of them were fixed at 172 nM, their inhibition rates were 36.2% and 29.1%, respectively. The results showed that the CE method was powerful, sensitive, and fast and required little sample. It could be employed as one of the reliable drug screening methods for 20S proteasome inhibitors. (C) 2009 Elsevier Inc. All rights reserved.

语种英语
WOS记录号WOS:000272883900009
项目编号30772650 ; 20772008
资助机构National Natural Science Foundation of China
引用统计
被引频次:14[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52541
专题北京大学临床肿瘤学院_肿瘤放疗科
北京大学药学院_化学生物学系
北京大学药学院_分子与细胞药理学系
作者单位1.Peking Univ, Dept Pharmaceut Anal, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Peking Univ, Dept Med Chem, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
3.Peking Univ, Natl Res Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Chen, Wenjing,Mou, Ke,Xu, Bo,et al. Capillary electrophoresis for screening of 20S proteasome inhibitors[J]. ANALYTICAL BIOCHEMISTRY,2009,394(1):62-67.
APA Chen, Wenjing,Mou, Ke,Xu, Bo,Ling, Xiaomei,Cui, Jingrong,&Xu, Ping.(2009).Capillary electrophoresis for screening of 20S proteasome inhibitors.ANALYTICAL BIOCHEMISTRY,394(1),62-67.
MLA Chen, Wenjing,et al."Capillary electrophoresis for screening of 20S proteasome inhibitors".ANALYTICAL BIOCHEMISTRY 394.1(2009):62-67.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Chen, Wenjing]的文章
[Mou, Ke]的文章
[Xu, Bo]的文章
百度学术
百度学术中相似的文章
[Chen, Wenjing]的文章
[Mou, Ke]的文章
[Xu, Bo]的文章
必应学术
必应学术中相似的文章
[Chen, Wenjing]的文章
[Mou, Ke]的文章
[Xu, Bo]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。