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学科主题: 临床医学
题名:
Binding interactions between prazosin and alpha(1A)-adrenoceptor: investigation on the thermodynamic behaviors and the binding mechanism by high performance affinity chromatography
作者: Wang, Jing1; Li, Qian1; Yang, Lingjian1; Zhang, Yajun1; Yu, Jie1; Zhao, Xinfeng1; Zheng, Jianbin2; Zhang, Youyi3,4; Zheng, Xiaohui1
刊名: ANALYTICAL METHODS
发表日期: 2015
DOI: 10.1039/c4ay03046j
卷: 7, 期:8, 页:3340-3346
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 ; PROTEIN-COUPLED RECEPTORS ; FRONTAL ANALYSIS ; IMMOBILIZED BETA(2)-ADRENOCEPTOR ; LIQUID-CHROMATOGRAPHY ; STATIONARY-PHASE ; CONSTANTS ; RESONANCE ; DRUGS
英文摘要:

Although the association constant and the number of binding sites of prazosin to alpha(1A)-adrenoceptor were determined by high performance affinity chromatography (HPAC) in our previous work, the thermodynamic behaviors and the binding mechanism of the drug to immobilized alpha(1A)-adrenoceptor remained unclear. This work intended to address the issue by HPAC and molecular docking. The investigations involved the determination of association constants by frontal analysis at different temperatures, the calculation of enthalpy, entropy and free energy changes, the examination of mobile phase composition on the binding parameters and the site-directed molecular docking. The changes of enthalpy, entropy and free energy during the interaction were -20.79 kJ mol(-1), -59.28 J mol(-1) K-1 and -2.4 kJ mol(-1), respectively. The binding of prazosin to alpha(1A)-adrenoceptor was an endothermic process with an increase in entropy. This reaction was mainly driven by hydrogen bonds. The ionic strength of the mobile phase provided a positive response to the values of association constants, while the power of hydrogen and the concentration of isopropyl in the mobile phase showed a negative trend. Ser(203) and Ser(192) in the fifth transmembrane segment of the receptor were the positions for the formation of hydrogen bonds. It is possible to utilize the immobilized receptor to determine the mechanism of drug-receptor interactions.

语种: 英语
所属项目编号: 21475103 ; 2013KCT-24 ; 2013YQ170525 ; 2013YQ17052509
项目资助者: National Nature Science Foundation of China ; program for Innovative Research Team of Shaanxi Province ; Ministry of Science and Technology of the People&prime ; s Republic of China
WOS记录号: WOS:000352897500005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/66311
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, Minist Educ, Key Lab Resource Biol & Biotechnol Western China, Xian 710069, Peoples R China
2.NW Univ Xian, Inst Analyt Sci, Xian 710069, Peoples R China
3.Peking Univ, Hosp 3, Inst Vasc Med, Beijing 100083, Peoples R China
4.Minist Educ, Key Lab Mol Cardiovasc Sci, Beijing 100083, Peoples R China

Recommended Citation:
Wang, Jing,Li, Qian,Yang, Lingjian,et al. Binding interactions between prazosin and alpha(1A)-adrenoceptor: investigation on the thermodynamic behaviors and the binding mechanism by high performance affinity chromatography[J]. ANALYTICAL METHODS,2015,7(8):3340-3346.
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