Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, The Midlands, UK.
FEBS J. 2021 Apr;288(8):2585-2601. doi: 10.1111/febs.15729. Epub 2021 Feb 9.
G protein-coupled receptors (GPCRs) are the largest family of membrane receptors and major targets for FDA-approved drugs. The ability to quantify GPCR expression and ligand binding characteristics in different cell types and tissues is therefore important for drug discovery. The advent of genome editing along with developments in fluorescent ligand design offers exciting new possibilities to probe GPCRs in their native environment. This review provides an overview of the recent technical advances employed to study the localisation and ligand binding characteristics of genome-edited and endogenously expressed GPCRs.
G 蛋白偶联受体(GPCRs)是最大的膜受体家族,也是美国食品和药物管理局(FDA)批准药物的主要靶点。因此,定量检测不同细胞类型和组织中 GPCR 的表达和配体结合特性对于药物发现非常重要。基因组编辑技术的出现以及荧光配体设计的发展为在天然环境中研究 GPCR 提供了令人兴奋的新可能性。本文综述了近年来用于研究基因组编辑和内源性表达的 GPCR 定位和配体结合特性的技术进展。