Detection of genome-edited and endogenously expressed G protein-coupled receptors

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.

Automated summary

GPCRs, the largest family of membrane receptors, are major drug targets approved by the FDA. Recent advances in genome editing and fluorescent ligand design have provided new possibilities for studying GPCRs in their native environment. This review discusses the technical advances used to study the localization and ligand binding characteristics of genome-edited and endogenously expressed GPCRs.