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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:
Immobilised Histidine Tagged beta(2)-Adrenoceptor Oriented by a Diazonium Salt Reaction and Its Application in Exploring Drug-Protein Interaction Using Ephedrine and Pseudoephedrine as Probes
作者: Li, Qian1; Bian, Liujiao1; Zhao, Xinfeng1; Gao, Xiaokang1; Zheng, Jianbin2; Li, Zijian3,4; Zhang, Youyi3,4; Jiang, Ru5; Zheng, Xiaohui1
刊名: PLOS ONE
发表日期: 2014-04-18
DOI: 10.1371/journal.pone.0094955
卷: 9, 期:4
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Multidisciplinary Sciences
研究领域[WOS]: Science & Technology - Other Topics
关键词[WOS]: BETA-ADRENERGIC-RECEPTOR ; HUMAN SERUM-ALBUMIN ; PERFORMANCE AFFINITY-CHROMATOGRAPHY ; COUPLED RECEPTORS ; BINDING ; IDENTIFICATION ; TARGETS
英文摘要:

A new oriented method using a diazonium salt reaction was developed for linking beta(2)-adrenoceptor (beta(2)-AR) on the surface of macroporous silica gel. Stationary phase containing the immobilised receptor was used to investigate the interaction between beta(2)-AR and ephedrine plus pseudoephedrine by zonal elution. The isotherms of the two drugs best fit the Langmuir model. Only one type of binding site was found for ephedrine and pseudoephedrine targeting beta(2)-AR. At 37 degrees C, the association constants during the binding were (5.94+/-0.05) x10(3)/M for ephedrine and (3.80+/-0.02) x10(3)/M for pseudoephedrine, with the binding sites of (8.92+/-0.06) x10(-4) M. Thermodynamic studies showed that the binding of the two compounds to beta(2)-AR was a spontaneous reaction with exothermal processes. The Delta G(theta), Delta H-theta and Delta S-theta for the interaction between ephedrine and beta(2)-AR were -(22.33+/-0.04) kJ/mol, -(6.51+/-0.69) kJ/mol and 50.94+/-0.31 J/mol.K, respectively. For the binding of pseudoephedrine to the receptor, these values were -(21.17+/-0.02) kJ/mol, -(7.48+/-0.56) kJ/mol and 44.13+/-0.01 J/mol.K. Electrostatic interaction proved to be the driving force during the binding of the two drugs to beta(2)-AR. The proposed immobilised method will have great potential for attaching protein to solid substrates and realizing the interactions between proteins and drugs.

语种: 英语
所属项目编号: 21075097 ; 21005060 ; 2013KCT-24 ; 2013YQ170525 ; 2013YQ17052509
项目资助者: National Nature Science Foundation of China ; Innovative Research Team of Shaanxi Province ; Ministry of Science and Technology of the People&prime ; s Republic of China
WOS记录号: WOS:000335226500046
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59331
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, Coll Life Sci, Xian 710069, Shaanxi, Peoples R China
2.NW Univ Xian, Inst Analyt Sci, Xian 710069, Shaanxi, Peoples R China
3.Peking Univ, Inst Vasc Med, Hosp 3, Beijing 100871, Peoples R China
4.Minist Educ, Key Lab Mol Cardiovasc Sci, Beijing, Peoples R China
5.Fourth Mil Med Univ, Sch Pharm, Xian 710032, Shaanxi, Peoples R China

Recommended Citation:
Li, Qian,Bian, Liujiao,Zhao, Xinfeng,et al. Immobilised Histidine Tagged beta(2)-Adrenoceptor Oriented by a Diazonium Salt Reaction and Its Application in Exploring Drug-Protein Interaction Using Ephedrine and Pseudoephedrine as Probes[J]. PLOS ONE,2014,9(4).
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