Probing the pharmacology of G protein-coupled receptors with fluorescent ligands.
Probing the pharmacology of G protein-coupled receptors with fluorescent ligands.
复制标题
用荧光配体探讨 G 蛋白偶联受体的药理学。
DOI：
10.1016/j.neuropharm.2015.04.033
复制
发表时间：
2015
影响因子：
4.7
通讯作者：
Stoddart LA
中科院分区：
文献类型：
--
作者：
Stoddart LA
G蛋白偶联受体控制着广泛的生理过程，是许多临床用药的靶标。了解受体与激动剂和拮抗剂结合的方式、它们在膜上的组织以及激动剂结合后的调节是开发新药的关键。获得这种知识的一种方式是使用荧光配体，这种配体已经被用来研究内源性表达系统中受体的表达和功能。具有合适成像性能的荧光配体可以与共聚焦显微镜结合使用，以研究受体激活后的调节。或者，通过使用单分子显微镜，他们可以探测膜内受体的空间组织。本文是《神经药理学中的荧光工具》特刊的一部分，重点介绍了荧光配体的应用技术和已发现的G蛋白偶联受体药理学的新方面。
G protein-coupled receptors control a wide range of physiological processes and are the target for many clinically used drugs. Understanding the way in which receptors bind agonists and antagonists, their organisation in the membrane and their regulation after agonist binding are important properties which are key to developing new drugs. One way to achieve this knowledge is through the use of fluorescent ligands, which have been used to study the expression and function of receptors in endogenously expressing systems. Fluorescent ligands with appropriate imaging properties can be used in conjunction with confocal microscopy to investigate the regulation of receptors after activation. Alternatively, through the use of single molecule microscopy, they can probe the spatial organisation of receptors within the membrane. This review focuses on the techniques in which fluorescent ligands have been used and the novel aspects of G protein-coupled receptor pharmacology which have been uncovered.This article is part of the Special Issue entitled ‘Fluorescent Tools in Neuropharmacology’.