Department of Pharmacy, Ruijin Hospital Affiliated to School of Medicine, Shanghai Jiaotong University, Shanghai, 200025, China; School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, China.
School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, China.
J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Dec 15;1161:122436. doi: 10.1016/j.jchromb.2020.122436. Epub 2020 Nov 18.
Bio-affinity chromatography is used in the study of drug-receptor interactions. A stepwise frontal analysis (SFA) method was developed based on frontal analysis (FA). A high expression alpha 1A adrenergic receptor (α AR) cell membrane chromatography (CMC) method was then developed and combined with SFA to investigate the affinity of three model α AR-binding drugs towards α AR. Equilibrium dissociation constant (K) values for drug-receptor interactions were determined by FA and SFA; results showed that these methods were highly consistent. The results demonstrate that the CMC/SFA method is a time-saving and less wasteful method than traditional method for the evaluation of drug-receptor binding characteristics, and could be used to study the interactions between drugs and membrane receptors.
生物亲和色谱法用于研究药物-受体相互作用。本研究基于前沿分析(FA)建立逐步前沿分析(SFA)方法。然后建立高表达的α 1A 肾上腺素能受体(α AR)细胞膜色谱(CMC)方法,并与 SFA 相结合,研究三种模型α AR 结合药物与α AR 的亲和力。通过 FA 和 SFA 测定药物-受体相互作用的平衡解离常数(K)值;结果表明这两种方法高度一致。结果表明,与传统方法相比,CMC/SFA 方法是一种更省时、更节省的评估药物-受体结合特性的方法,可用于研究药物与膜受体之间的相互作用。