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学科主题: 药学
题名:
Studies on the interactions between lactam analogs and the N-terminal extracellular tail of CC chemnokine receptor 4 by CZE
作者: 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
发表日期: 2007-08-01
DOI: 10.1002/elps.200700258
卷: 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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56051
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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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

Recommended Citation:
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.
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