GPCR药物研发中的钙离子动员检测

Ca2+ mobilization assays in GPCR drug discovery.

作者信息

Woszczek Grzegorz, Fuerst Elisabeth

机构信息

Division of Asthma, Allergy and Lung Biology, King's College London, 5th Floor, Tower Wing, Guy's Hospital, London, SE1 9RT, UK,

出版信息

Methods Mol Biol. 2015;1272:79-89. doi: 10.1007/978-1-4939-2336-6_6.

DOI:10.1007/978-1-4939-2336-6_6

PMID:25563178

Abstract

Intracellular calcium mobilization can be measured using several methods varying in indicator dyes and devices used. In this chapter, we describe the fluorescence-based method (FLIPR Calcium 4 Assay) developed by Molecular Devices for a FlexStation and routinely used in our laboratory for detecting intracellular calcium changes. The assay is designed to study calcium mobilization induced by majority of GPCRs and calcium channels and allows for simultaneous concentration-dependent analysis of several receptor agonists and antagonists, useful in receptor characterization and drug discovery projects.

摘要

细胞内钙动员可以通过几种方法来测量，这些方法在所用的指示染料和设备上有所不同。在本章中，我们描述了由分子设备公司为FlexStation开发的基于荧光的方法（FLIPR钙4检测法），该方法在我们实验室中常规用于检测细胞内钙变化。该检测法旨在研究大多数G蛋白偶联受体（GPCR）和钙通道诱导的钙动员，并允许对几种受体激动剂和拮抗剂进行同时的浓度依赖性分析，这在受体表征和药物发现项目中很有用。