G蛋白偶联受体配体结合分析技术

发布时间：2018-04-25 07:22

本文选题：G蛋白偶联受体 + 受体-配体结合分析　；参考：《药物分析杂志》2015年01期

【摘要】：G蛋白偶联受体(G-protein-coupled receptors,GPCRs)是迄今发现的最大的多药物靶点的受体超家族,其激动剂或拮抗剂常被用于治疗各种疾病,在药物研发中扮演重要角色。测定配体与受体亲和力的结合实验是药物评价、研发和作用机理研究中不可缺少的部分。用于研究GPCRs与其配体结合的分析技术,可以按照标记方式的异同分为三类:同位素标记法、非同位素标记法和非标记法。非同位素标记法多采用荧光配体标记,利用竞争法或荧光共振能量转移直接获知结合情况;非标记法中利用各种生物传感器,通过检测配体结合受体后胞内分子运动引起的电信号或光信号的变化来表征结合情况。此外,质谱也已被用于受体-配体平衡解离常数的测定,显示了其在非标记结合分析及受体功能研究中的潜力。本文归纳了目前用于GPCRs结合分析的主要技术,对其原理及优缺点进行了综述,并对受体-配体结合分析中新方法的应用进行了展望。
[Abstract]:The G protein coupling receptor (G-protein-coupled receptors, GPCRs) is the largest multi drug target receptor superfamily found so far. Its agonists or antagonists are often used in the treatment of various diseases and play an important role in drug development. Determination of ligand affinity with receptor is a study of drug evaluation, research and mechanism research. An indispensable part. The analytical techniques used to study the binding of GPCRs to its ligands can be divided into three categories according to the similarities and differences of the labeling methods: isotopic labeling, non isotope labeling and non labeling. Non isotopic markers are mostly labeled with fluorescent ligands and are directly known by competitive method or fluorescence resonance energy transfer. A variety of biosensors are used to characterize the combination of the electrical signals or light signals induced by the ligand binding to the receptor. Furthermore, the mass spectrometry has also been used to determine the equilibrium dissociation constant of the receptor ligand, showing its potential in the non labelled binding analysis and the study of the receptor function. The main techniques used for GPCRs binding analysis are summarized, and their principles and advantages and disadvantages are reviewed. The application of new methods in the receptor ligand binding analysis is prospected.

【作者单位】：华南理工大学生物科学与工程学院创新医药中心;华南理工大学生物科学与工程学院广东省发酵与酶工程重点实验室;
【基金】：广州市科技计划项目科学研究专项(2014J4100022) 中央高校基本科研业务费专项资金(2013ZM0048) 广东省发酵与酶工程重点实验室开放基金(j2kj-K411001III)
【分类号】：R96

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