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IR@PKUHSC  > 北京大学第三临床医学院  > 心血管内科  > 期刊论文
学科主题: 临床医学
题名:
Construction of adrenergic receptor subtype affinity chromatographic models for detection of ligand-receptor interactions
作者: Wang, Xueyan2,3; Meng, Xue2,3; Pei, Weijing2,4; Li, Zijian1; Zhang, Youyi1; Zheng, Jianbin3; Zheng, Xiaohui2,3
刊名: ANALYTICAL METHODS
发表日期: 2012-10-01
DOI: 10.1039/c2ay25601k
卷: 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
所属项目编号: CXB 201005260069A ; 20106101110001 ; ZYB200907070034A ; 2008BAI51B01
项目资助者: 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
WOS记录号: WOS:000309238300053
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56226
Appears in Collections:北京大学第三临床医学院_心血管内科_期刊论文

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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

Recommended Citation:
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.
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