Application of FRET- and BRET-based live-cell biosensors in deorphanization and ligand discovery studies on orphan G protein-coupled receptors

Autor: Joanna J. Sajkowska, Choi Har Tsang, Paweł Kozielewicz
Jazyk: angličtina
Rok vydání: 2024
Předmět:
Zdroj: SLAS Discovery, Vol 29, Iss 6, Pp 100174- (2024)
Druh dokumentu: article
ISSN: 2472-5552
DOI: 10.1016/j.slasd.2024.100174
Popis: Bioluminescence- and fluorescence-based resonance energy transfer assays have gained considerable attention in pharmacological research as high-throughput scalable tools applicable to drug discovery. To this end, G protein-coupled receptors represent the biggest target class for marketed drugs, and among them, orphan G protein-coupled receptors have the biggest untapped therapeutic potential. In this review, the cases where biophysical methods, BRET and FRET, were employed for deorphanization and ligand discovery studies on orphan G protein-coupled receptors are listed and discussed.
Databáze: Directory of Open Access Journals