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题名: Microdialysis sampling method for evaluation of binding kinetics of small molecules to macromolecules
作者: Wang, Hailin1;  Wang, Zhixin1;  Liu, Meiling1;  Zou, Hanfa2
通讯作者: 邹汉法
刊名: ANALYTICAL CHEMISTRY
发表日期: 2008-04-15
DOI: 10.1021/ac702066x
卷: 80, 期:8, 页:2993-2999
收录类别: SCI
文章类型: Article
部门归属: 18
项目归属: 1809
产权排名: 2;4
WOS标题词: Science & Technology ;  Physical Sciences
类目[WOS]: Chemistry, Analytical
研究领域[WOS]: Chemistry
英文摘要: Here we present an application of microdialysis sampling for evaluation of the binding kinetics of small molecules to macromolecules. It is label-free, and no immobilization of any interaction partner is required. The method was established by the coupling of a binding reaction with a membrane transport in a miniature and dynamic microdialysis sampling system. A theoretical model was established to describe the quantitative relationship between the binding kinetics of small ligands to macromolecules and the enhanced mass transport of small ligands and was applied to estimate the binding kinetics. To demonstrate the proof-of-principle, we examined the binding kinetics of an abundant plasma protein human serum albumin (HSA) and a representative drug ketoprofen as an example. The primary binding constant of ketoprofen to HSA was estimated as 1.63 ( +/- 0.12) x 106 M-1. The estimated association and dissociation rate constants (k(1) and k(-1)) were about 3.71 x 10(5) M-1 s(-1) and 0.227 s(-1), respectively. The results suggest a fast binding of ketoprofen to HSA and a fast dissociation of the formed complex, which are consistent with the reversible binding property of drug and HSA (k(-1) in the order of s(-1)). This is the first report on binding-kinetics measurement using microdialysis sampling.
关键词[WOS]: SURFACE-PLASMON RESONANCE ;  HUMAN SERUM-ALBUMIN ;  NONEQUILIBRIUM CAPILLARY-ELECTROPHORESIS ;  PERFORMANCE LIQUID-CHROMATOGRAPHY ;  EQUILIBRIUM MIXTURES ;  INTRACEREBRAL MICRODIALYSIS ;  NONCOMPETITIVE INHIBITORS ;  QUANTITATIVE-ANALYSIS ;  PROTEIN INTERACTIONS ;  STATIONARY-PHASE
语种: 英语
原文出处: 查看原文
WOS记录号: WOS:000254969100045
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/100005
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Chinese Acad Sci, Ecoenvironm Sci Res Ctr, State Key Lab Environm Chem & Ecotoxicol, Beijing 100085, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Natl Chromat Res & Anal Ctr, Dalian 116023, Peoples R China

Recommended Citation:
Wang, Hailin,Wang, Zhixin,Liu, Meiling,et al. Microdialysis sampling method for evaluation of binding kinetics of small molecules to macromolecules[J]. ANALYTICAL CHEMISTRY,2008,80(8):2993-2999.
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