Determine equilibrium dissociation constant of drug-membrane receptor affinity using the cell membrane chromatography relative standard method

被引：53

作者：

Ma, Weina ^{[1
]}

Yang, Liu ^{[1
]}

Lv, Yanni ^{[1
]}

Fu, Jia ^{[1
]}

Zhang, Yanmin ^{[1
]}

He, Langchong ^{[1
]}

机构：

[1] Xi An Jiao Tong Univ, Sch Pharm, Xian 710061, Peoples R China

来源：

JOURNAL OF CHROMATOGRAPHY A | 2017年 / 1503卷

基金：

中国国家自然科学基金;

关键词：

Cell membrane chromatography; Equilibrium dissociation constant; Drug-membrane receptor affinity; Relative standard method; IN-VIVO; PROTEIN INTERACTIONS; BINDING; TELMISARTAN; DENSITY; SITES; PET;

D O I：

10.1016/j.chroma.2017.04.053

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The equilibrium dissociation constant (ICD) of drug-membrane receptor affinity is the basic parameter that reflects the strength of interaction. The cell membrane chromatography (CMC) method is an effective technique to study the characteristics of drug-membrane receptor affinity. In this study, the KD value of CMC relative standard method for the determination of drug-membrane receptor affinity was established to analyze the relative ICD values of drugs binding to the membrane receptors (Epidermal growth factor receptor and angiotensin II receptor). The K-D values obtained by the CMC relative standard method had a strong correlation with those obtained by the frontal analysis method. Additionally, the ICp values obtained by CMC relative standard method correlated with pharmacological activity of the drug being evaluated. The CMC relative standard method is a convenient and effective method to evaluate drug membrane receptor affinity. (C) 2017 Elsevier B.V. All rights reserved.

引用

页码：12 / 20

页数：9

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