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

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Sajkowska JJ, Tsang CH, Kozielewicz P

SLAS Discov 29 (6) 100174 [2024-09-00; online 2024-07-29]

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.

PubMed 39084335

DOI 10.1016/j.slasd.2024.100174

Crossref 10.1016/j.slasd.2024.100174

pii: S2472-5552(24)00036-4