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学科主题: 药学
题名:
Screening of thiourea derivatives and carbonyl-2-aminothiazole derivatives for potential CCR4 antagonists using capillary zone electrophoresis
作者: 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
发表日期: 2011
DOI: 10.1016/j.jchromb.2010.11.014
卷: 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
所属项目编号: 2006AA02A305 ; 2009ZX09103-724 ; 30872292 ; 90813025 ; 81072612 ; 7102107 ; K20090207 ; 2009ZX09301-010
项目资助者: 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
WOS记录号: WOS:000286539900011
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/53696
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, 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

Recommended Citation:
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.
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