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Updated: May 21, 2025

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

用于成像A类G蛋白结合受体的光工具

Renáta Szabó¹, Ágnes Hornyánszky¹, Dóra Judit Kiss²

¹Medicinal Chemistry Research Group, HUN-REN Research Centre for Natural Sciences, H-1117 Budapest, Hungary; Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, H-1111 Budapest, Hungary; National Laboratory for Drug Research and Development, H-1117 Budapest, Hungary.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

|March 20, 2025

概括

新的光探针正在加强对G蛋白结合受体 (GPCRs) 的研究,包括尚未探索的孤儿受体. 这些工具有助于药物发现和理解受体功能.

科学领域:

生物化学和药理学生物化学和药理学
分子生物学分子生物学
药物发现药物发现药物发现

背景情况:

G蛋白结合受体 (GPCRs) 在生物过程中至关重要,是主要的药物标.
许多GPCR,特别是孤儿受体,需要进一步研究.
光配体是描述GPCR的功能和组织的重要工具.

研究的目的:

对A类GPCRs (2018-2024) 的光探针开发的最新进展进行审查.
分析新探针在GPCR子类中的分布,并确定新向的受体.
突出结构生物学进步对光探针设计的影响.

主要方法:

2018年至2024年期间发表的A类GPCR光探针开发的系统审查.
分析了120多个新开发的探针,针对60个GPCRs.
整合数据与最近的结构生物学发现 (cryo-EM,AlphaFold).

主要成果:

对12种新的受体亚型和6种孤儿GPCR (例如GPR6,GPR52,GPR84) 开发新型光探针.
在多种GPCR家族 (aminergic,peptidergic,lipid等) 的探针选择性方面取得显著进展. ) 的情况.
由于结构生物学的进步促进了探针设计,对GPCRs的理解得到了增强.

结论:

光探针对于GPCR研究和药物发现越来越重要.
最近的创新使得GPCR的向范围更广,包括以前未被描述的受体.
这些工具支持先进的应用,如体内成像,诊断和光导向手术,加速药物开发.

关键词:

一个A类的A类.药物发现药物发现光探测器的光探测器与G蛋白结合受体的受体是G蛋白结合受体.图像成像技术可以提供图像.

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

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Reporter Genes

Reporter Genes

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Immunofluorescence Microscopy

Immunofluorescence Microscopy

A fluorescence microscope uses fluorescent chromophores called fluorochromes, which can absorb energy from a light source and then emit this energy as visible light. Fluorochromes include naturally fluorescent substances (such as chlorophylls) and fluorescent stains that are added to the specimen to create contrast. Dyes such as Texas red and FITC are examples of fluorochromes. Other examples include the nucleic acid dyes 4’,6’-diamidino-2-phenylindole (DAPI), and acridine orange.