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Review
. 2024 Sep;29(6):100174.
doi: 10.1016/j.slasd.2024.100174. Epub 2024 Jul 29.

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

Joanna J Sajkowska  1 , Choi Har Tsang  2 , Paweł Kozielewicz  3
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Free article
Review

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

Joanna J Sajkowska et al. SLAS Discov. 2024 Sep.
Free article

Abstract

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.

Keywords: BRET; Deorphanization; FRET; Ligand discovery; Live-cell assays; Orphan G protein-coupled receptors.

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Conflict of interest statement

Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Paweł Kozielewicz reports financial support was provided by Swedish Research Council. Paweł Kozielewicz reports financial support was provided by Jeanssons Foundations. Paweł Kozielewicz reports financial support was provided by Karolinska Institute.

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