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Screening of thiourea derivatives and carbonyl-2-aminothiazole derivatives for potential CCR4 antagonists using capillary zone electrophoresis
Zhang, Shuyu1; Qi, Hui2; Yakufu, Pazilaiti1; Zhao, Fang2; Ling, Xiaomei1; Xiao, Junhai3; Wang, Ying2
关键词Capillary Zone Electrophoresis Ccr4 Antagonists/interactions Thiourea Derivatives C-arbonyl-2-aminothiazole Derivatives
刊名JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
2011
DOI10.1016/j.jchromb.2010.11.014
879期:1页:75-82
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]MACROPHAGE-DERIVED CHEMOKINE ; FUNCTIONAL LIGAND ; BINDING ; RECEPTOR ; PEPTIDES ; IDENTIFICATION ; PATHOGENESIS ; CONSTANTS ; FACTOR-1 ; ASTHMA
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. CCR4 has been identified as a potentially important drug target for the treatment of T cell-mediated allergic inflammatory diseases. In this study, a novel series of CCR4 antagonists were screened by investigating the interactions between the compounds and the human CCR4 N-terminal peptide ML40 using capillary zone electrophoresis (CZE) for the first time. Both qualitative and quantitative characterizations of the compound-peptide binding were determined. The results showed that, compared with positive control, ten of the compounds were interacted with ML40, which were A3C223, A3C231, A4C238, A3C241, A4C241, A4C239, ZXF0337, ZXF0432, ZXF0519 and ZXF0637A, and their binding constants were calculated from the Scatchard plot by regression. The binding constants of the compounds to ML40 were calculated and the binding constant of ZXF0432 was the largest among them [(7.6334 +/- 0.1907) x 10(4) M-1]. Here, a sensitive and selective high-performance analytical method based on CZE was developed for screening of thiourea derivatives and C-arbonyl-2-aminothiazole derivatives for potential CCR4 antagonists for the first time. The methodology presented should be generally applicable to study compounds-ML40 interactions as a powerful, sensitive and fast screening method for CCR4 antagonist discovery. (C) 2010 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000286539900011
项目编号2006AA02A305 ; 2009ZX09103-724 ; 30872292 ; 90813025 ; 81072612 ; 7102107 ; K20090207 ; 2009ZX09301-010
资助机构National High-Tech Research and Development Program of China ; National Key New Drug Creation Program of China ; National Natural Science Foundation of China ; Natural Science Foundation of Beijing ; Open Foundation of State Key Laboratory of Natural and Biomimetic Drugs of China ; National New Drug Research and Development Project of China
引用统计
被引频次:2[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/400002259/53696
专题北京大学第三临床医学院_皮肤科
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, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Ctr Human Dis Genom, Sch Basic Med Sci, Dept Med Immunol, Beijing 100191, Peoples R China
3.Beijing Inst Pharmacol & Toxicol, Beijing 100850, Peoples R China
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GB/T 7714
Zhang, Shuyu,Qi, Hui,Yakufu, Pazilaiti,et al. Screening of thiourea derivatives and carbonyl-2-aminothiazole derivatives for potential CCR4 antagonists using capillary zone electrophoresis[J]. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,2011,879(1):75-82.
APA Zhang, Shuyu.,Qi, Hui.,Yakufu, Pazilaiti.,Zhao, Fang.,Ling, Xiaomei.,...&Wang, Ying.(2011).Screening of thiourea derivatives and carbonyl-2-aminothiazole derivatives for potential CCR4 antagonists using capillary zone electrophoresis.JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,879(1),75-82.
MLA Zhang, Shuyu,et al."Screening of thiourea derivatives and carbonyl-2-aminothiazole derivatives for potential CCR4 antagonists using capillary zone electrophoresis".JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES 879.1(2011):75-82.
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