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Studies on the interactions between lactam analogs and the N-terminal extracellular tail of CC chemnokine receptor 4 by CZE
Sun, Zhe; Ling, Xiaomei; Sun, Wei; Xiao, Junhai; Yin, Caihua; Wang, Ying
关键词Ccr4 Antagonist Cze Diastereomer Interactions Lactam Analogs
刊名ELECTROPHORESIS
2007-08-01
DOI10.1002/elps.200700258
28期:17页:3064-3069
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Chemistry, Analytical
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]CAPILLARY-ELECTROPHORESIS ; ATOPIC-DERMATITIS ; CHEMOKINE ; BINDING ; IDENTIFICATION ; ANTAGONISTS ; LIGAND
英文摘要

CC chemokine receptor 4 (CCR4) is a kind of G-protein-coupled receptors with a characteristic seven-transmembrane structure and selectively expressed on Th2-type CD4+ T-cells, which play a pivotal role in allergic inflammation. In this study, the interactions between 2-(2-(2,4-dichloro-phenyl)-4-{[(2-methyl-3-chloro-phenyl)-1-ylmethyl]-carbamoyl}-methyl)-5-oxo-pyrrole-1-yl)-N-(3-piperidinyl-propyl)-acetamide (compound A), a known CCR4 antagonist, and ML40 were studied by CZE for the first time. Both qualitative and quantitative characterizations of the drug-peptide binding were determined. The binding constant of the interaction between the trans-diastereomer of compound A and ML40, calculated from the Scatchard plot by regression, was (1.06 +/- 0.11) X 10(5)/M. Also, it was cone firmed that the trans-diastereomer was more potent affinity with CCR4 than its cis-counterpart. The experimental results show that this reported method by CZE for the determination of the compound A and ML40 interactions is powerful, sensitive, and fast, requires less amounts of reagents, and further, it can be employed as one of the reliable screening methods to a series of lactam analogs in the drug discovery for allergic inflammation diseases.

语种英语
WOS记录号WOS:000249743500014
引用统计
被引频次:7[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/400002259/56051
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut Anal, Beijing, Peoples R China
2.Beijing Inst Pharmacol & Toxicol, Beijing, Peoples R China
3.Peking Univ, Ctr Human Dis Genom, Beijing 100871, Peoples R China
4.Peking Univ, Sch Basic Med Sci, Hlth Sci Ctr, Dept Med Immunol, Beijing 100871, Peoples R China
推荐引用方式
GB/T 7714
Sun, Zhe,Ling, Xiaomei,Sun, Wei,et al. Studies on the interactions between lactam analogs and the N-terminal extracellular tail of CC chemnokine receptor 4 by CZE[J]. ELECTROPHORESIS,2007,28(17):3064-3069.
APA Sun, Zhe,Ling, Xiaomei,Sun, Wei,Xiao, Junhai,Yin, Caihua,&Wang, Ying.(2007).Studies on the interactions between lactam analogs and the N-terminal extracellular tail of CC chemnokine receptor 4 by CZE.ELECTROPHORESIS,28(17),3064-3069.
MLA Sun, Zhe,et al."Studies on the interactions between lactam analogs and the N-terminal extracellular tail of CC chemnokine receptor 4 by CZE".ELECTROPHORESIS 28.17(2007):3064-3069.
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