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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 ed...

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Detalles Bibliográficos
Autores principales: Soave, Mark, Stoddart, Leigh A., White, Carl W., Kilpatrick, Laura E., Goulding, Joëlle, Briddon, Stephen J., Hill, Stephen J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8647918/
https://www.ncbi.nlm.nih.gov/pubmed/33506623
http://dx.doi.org/10.1111/febs.15729
Descripción
Sumario: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.