Detection of genome‐edited and endogenously expressed G protein‐coupled receptors. (9th February 2021)

• Record Type: Journal Article
• Authors: Soave, Mark; Stoddart, Leigh A.; White, Carl W.; Kilpatrick, Laura E.; Goulding, Joëlle; Briddon, Stephen J.; Hill, Stephen J.
• Is Part Of: FEBS journal. Volume 288:Number 8(2021)
• Page Start: 2585
• Page End: 2601
• Publication Date: 2021-02-09
• Subjects: advanced imaging -- CRISPR/Cas9 -- endogenous -- fluorescent ligand -- GPCRs -- nanobodies; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pathology, Molecular -- Periodicals; 572
• DOI: 10.1111/febs.15729
• Languages: English
• ISSNs: 1742-464X

Abstract

Abstract : 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. Abstract : G protein‐coupled receptors (GPCRs) are the largest family of membrane receptors and major targets for FDA‐approved drugs. Quantifying GPCR expression and ligand binding characteristics in different cell types is important for drug discovery. The advent of genome editing and developments in fluorescent ligand design offers exciting possibilities to probe GPCRs in their native environment. This review discusses recent techniques employed in studying endogenously expressed GPCR localisation and ligand binding characteristics.