Screening of break point cluster region Abelson tyrosine kinase inhibitors by capillary electrophoresis

doi:10.1016/j.chroma.2018.01.019

	Screening of break point cluster region Abelson tyrosine kinase inhibitors by capillary electrophoresis
	Xu, Mei 1; Zheng, Mengmeng 1,2; Liu, Guizhen1,3 ; Zhang, Meng 1,2; Kang, Jingwu1,3
	2018-02-16
发表期刊	JOURNAL OF CHROMATOGRAPHY A (IF:3.8[JCR-2023],3.5[5-Year])
ISSN	0021-9673
卷号	1537 页码:128-134
发表状态	已发表
DOI	10.1016/j.chroma.2018.01.019
摘要	In the present study, a capillary electrophoresis (CE) method was developed for screening of inhibitors against the break point cluster region Abelson tyrosine kinase (BCR-ABL). The screening method was established by using 5-carboxyfluorescein labeled peptide substrate of BCR-ABL (F-ABLS), a known BCR-ABL tyrosine kinase inhibitor dasatinib, as well as a small chemical library consisting of 37 natural products. Thus, the inhibition of BCL-ABL kinase by small inhibitors was assayed by a CE system equipped with the laser induced fluorescence detector. The yield of phosphorylated product could be precisely measured through the separation by CE. The method is competent for enzymatic inhibition assay as well as the measurement of the inhibition kinetics. For screening BCR-ABL tyrosine kinase inhibitors, the hits were readily identified once the peak area of the phosphorylated products was reduced in comparison with the negative control. By taking the advantage of the screening method, luteolin and epicatechin gallate were discovered as the new BCR-ABL inhibitors. (C) 2018 Elsevier B.V. All rights reserved.
关键词	BCR-ABL inhibitor Natural products Capillary electrophoresis
收录类别	SCI ; SCIE ; EI
语种	英语
资助项目	Chinese Academy of Sciences[XDB20020200]
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
WOS类目	Biochemical Research Methods ; Chemistry, Analytical
WOS记录号	WOS:000425201700015
出版者	ELSEVIER SCIENCE BV
WOS关键词	TANDEM MASS-SPECTROMETRY ; BCR-ABL ; MEDIATED MICROANALYSIS ; NATURAL-PRODUCTS ; CANCER-CELLS ; IMATINIB ; EXTRACTS ; DOMAIN ; BMS-354825 ; DASATINIB
原始文献类型	Article
引用统计	正在获取...
文献类型	期刊论文
条目标识符	https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/18267
专题	物质科学与技术学院物质科学与技术学院_特聘教授组_康经武组物质科学与技术学院_博士生
通讯作者	Kang, Jingwu
作者单位	1.Chinese Acad Sci, Shanghai Inst Organ Chem, Ctr Excellence Mol Synth, State Key Lab Bioorgan & Nat Prod Chem, Lingling Rd 345, Shanghai 200032, Peoples R China 2.Univ Chinese Acad Sci, Yuquan Rd 19, Beijing 100049, Peoples R China 3.ShanghaiTech Univ, Haike Rd 100, Shanghai 201210, Peoples R China
通讯作者单位	上海科技大学
推荐引用方式 GB/T 7714	Xu, Mei,Zheng, Mengmeng,Liu, Guizhen,et al. Screening of break point cluster region Abelson tyrosine kinase inhibitors by capillary electrophoresis[J]. JOURNAL OF CHROMATOGRAPHY A,2018,1537:128-134.
APA	Xu, Mei,Zheng, Mengmeng,Liu, Guizhen,Zhang, Meng,&Kang, Jingwu.(2018).Screening of break point cluster region Abelson tyrosine kinase inhibitors by capillary electrophoresis.JOURNAL OF CHROMATOGRAPHY A,1537,128-134.
MLA	Xu, Mei,et al."Screening of break point cluster region Abelson tyrosine kinase inhibitors by capillary electrophoresis".JOURNAL OF CHROMATOGRAPHY A 1537(2018):128-134.