Application of FRET- and BRET-based live-cell biosensors in deorphanization and ligand discovery studies on orphan G protein-coupled receptors
Joanna J. Sajkowska, C. Tsang, Paweł Kozielewicz
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.
Topics & Concepts
Förster resonance energy transferG protein-coupled receptorDrug discoveryReceptorComputational biologyChemistryEnergy transferLigand (biochemistry)NanotechnologyCell biologyBiologyBiochemistryFluorescencePhysicsMaterials scienceMolecular physicsQuantum mechanicsReceptor Mechanisms and SignalingAdenosine and Purinergic SignalingNeuroscience and Neuropharmacology Research