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Revealing binding interaction between seven drugs and immobilized beta(2)-adrenoceptor by high-performance affinity chromatography using frontal analysis
Zhao Xin-feng1; Huang Jing-jing1; Li Qian1; Wei Lu-sha1; Zheng Jian-bin2; Zheng Xiao-hui1; Li Zi-jian3,4; Zhang You-yi3,4
关键词Affinity Chromatography Dissociation Constant Frontal Analysis 2-adrenoceptor
刊名JOURNAL OF MOLECULAR RECOGNITION
2013-05-01
DOI10.1002/jmr.2271
26期:5页:252-257
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Biophysics
研究领域[WOS]Biochemistry & Molecular Biology ; Biophysics
关键词[WOS]PROTEIN-COUPLED RECEPTOR ; ACETYLCHOLINE-RECEPTORS ; STATIONARY PHASES ; P-GLYCOPROTEIN ; SELECTIVITY ; ANTAGONISTS ; ASSAY
英文摘要

The development of new approaches to study the affinity between ligands and G-protein-coupled receptors proves to be of growing interest for pharmacologists, chemists, and biologists. The aim of this work was to determine the binding of seven drugs to 2-adrenoceptors by frontal analysis using immobilized receptor stationary phase. The dissociation constants (Kd) were determined to be (3.16 +/- 0.09)x104M for salbutamol, (4.29 +/- 0.12)x104M for terbutaline, (6.19 +/- 0.16)x104M for methoxyphenamine, (2.11 +/- 0.07)x104M for tulobuterol, (1.82 +/- 0.11)x104M for fenoterol, (9.75 +/- 0.24)x106M formoterol, and (9.84 +/- 0.26)x105M for clenbuterol. These results showed a good correlation with the data determined by radioligand binding assay. Further investigations revealed that the dissociation constant mainly attributed to the number of hydrogen bonds in the structures of ligands. This study indicates that affinity chromatography using immobilized receptor stationary phase can be used for the direct determination of drug-receptor binding interactions and has the potential to become a reliable alternative for quantitative studies of ligandreceptor interactions. Copyright (c) 2013 John Wiley & Sons, Ltd.

语种英语
WOS记录号WOS:000316812000005
引用统计
被引频次:12[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/400002259/50695
专题北京大学第三临床医学院_心血管内科
作者单位1.Minist Educ, Key Lab Mol Cardiovasc Sci, Beijing 100083, Peoples R China
2.Northwest Univ, Coll Life Sci, Xian 710069, Peoples R China
3.Northwest Univ, Inst Analyt Sci, Xian 710069, Peoples R China
4.Peking Univ, Inst Vasc Med, Third Hosp, Beijing 100083, Peoples R China
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Zhao Xin-feng,Huang Jing-jing,Li Qian,et al. Revealing binding interaction between seven drugs and immobilized beta(2)-adrenoceptor by high-performance affinity chromatography using frontal analysis[J]. JOURNAL OF MOLECULAR RECOGNITION,2013,26(5):252-257.
APA Zhao Xin-feng.,Huang Jing-jing.,Li Qian.,Wei Lu-sha.,Zheng Jian-bin.,...&Zhang You-yi.(2013).Revealing binding interaction between seven drugs and immobilized beta(2)-adrenoceptor by high-performance affinity chromatography using frontal analysis.JOURNAL OF MOLECULAR RECOGNITION,26(5),252-257.
MLA Zhao Xin-feng,et al."Revealing binding interaction between seven drugs and immobilized beta(2)-adrenoceptor by high-performance affinity chromatography using frontal analysis".JOURNAL OF MOLECULAR RECOGNITION 26.5(2013):252-257.
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