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学科主题临床医学
Construction of adrenergic receptor subtype affinity chromatographic models for detection of ligand-receptor interactions
Wang, Xueyan2,3; Meng, Xue2,3; Pei, Weijing2,4; Li, Zijian1; Zhang, Youyi1; Zheng, Jianbin3; Zheng, Xiaohui2,3
刊名ANALYTICAL METHODS
2012-10-01
DOI10.1039/c2ay25601k
4期:10页:3420-3424
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Analytical ; Food Science & Technology ; Spectroscopy
研究领域[WOS]Chemistry ; Food Science & Technology ; Spectroscopy
关键词[WOS]HUMAN SERUM-ALBUMIN ; CHIRAL SEPARATION MECHANISMS ; CONFORMATIONAL MOBILITY ; (S)-WARFARIN BINDING ; STATIONARY-PHASE ; HPLC COLUMNS ; CELLS ; BETA(2)-ADRENOCEPTOR ; ALPHA-3-BETA-4 ; (R)-WARFARIN
英文摘要

Adrenergic receptors (ARs) are members of the super family of G protein-coupled receptors (GPCRs). A large number of small molecular drugs performed their actions on ARs. In this study, two subtypes of ARs affinity chromatographic models have been constructed for investigating the interactions between small molecular compounds and the alpha- and beta-AR subtypes. The alpha-ARs were obtained from HEK 293 cells stably transfected human alpha-ARs on the membrane and the beta-ARs were obtained from lung tissues of rabbits. ARs were purified and immobilized on the surface of macro-pore silica gel by covalent bonds. Then the gel was packed into a stainless steel column (4.6 x 50 mm). Binding abilities between small molecules and immobilized ARs were determined by on-line chromatographic technologies. Preliminary on-line binding studies employing frontal chromatographic techniques were conducted with the known alpha-AR agonist (norepinephrine, NE) and beta-AR antagonist (propranolo). Calculated association constants (K-a) and binding sites (m(Ltot)) values for NE on immobilized alpha-AR were 0.9 x 10(4) L mol(-1) and 5.5 x 10(-7) mol L-1, and on immobilized beta-AR were 0.2 x 10(4) L mol(-1) and 3.3 x 10(-7) mol L-1, respectively. K-a and m(Ltot) values for propranolol on immobilized alpha-AR were 1.1 x 10(3) L mol(-1) and 1.0 x 10(-7) mol L-1, and on immobilized beta-AR were 2.5 x 10(4) L mol(-1) and 5.0 x 10(-7) mol L-1, respectively. Above association values were obviously different, but the changes of their laws were comparatively unanimous: there was stronger binding between small molecular compounds and their immobilized target ARs. The conclusions indicated that the immobilized ARs stationary phases can be used to assess the binding affinities of compounds and screen possible active compounds qualitatively. In addition, this study represented an example of using immobilized subtype ARs in a chromatographic system.

语种英语
WOS记录号WOS:000309238300053
项目编号CXB 201005260069A ; 20106101110001 ; ZYB200907070034A ; 2008BAI51B01
资助机构Research Fund for Shenzhen biological, internet, new energy industry development ; Research Fund for Doctoral Program of university and college ; Shenzhen-Hong Kong Innovation Circle ; National Key Technology RD Program
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/400002259/56226
专题北京大学第三临床医学院_心血管内科
作者单位1.NW Univ Xian, Xian 710069, Peoples R China
2.Peking Univ, Inst Cardiovasc Sci, Hosp 3, Beijing, Peoples R China
3.Tsinghua Univ, Key Lab New Drugs Res TCM Shenzhen, Res Inst, Shenzhen 518057, Peoples R China
4.Shenzhen Tradit Chinese Med & Nat Prod Res Ctr, Shenzhen, Peoples R China
推荐引用方式
GB/T 7714
Wang, Xueyan,Meng, Xue,Pei, Weijing,et al. Construction of adrenergic receptor subtype affinity chromatographic models for detection of ligand-receptor interactions[J]. ANALYTICAL METHODS,2012,4(10):3420-3424.
APA Wang, Xueyan.,Meng, Xue.,Pei, Weijing.,Li, Zijian.,Zhang, Youyi.,...&Zheng, Xiaohui.(2012).Construction of adrenergic receptor subtype affinity chromatographic models for detection of ligand-receptor interactions.ANALYTICAL METHODS,4(10),3420-3424.
MLA Wang, Xueyan,et al."Construction of adrenergic receptor subtype affinity chromatographic models for detection of ligand-receptor interactions".ANALYTICAL METHODS 4.10(2012):3420-3424.
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