G protein-coupled receptors (GPCRs) with no known endogenous ligand are termed orphans. Deorphanization of a GPCR involves identifying the ligand, which can be a painstaking exercise. In this Comment, we discuss the challenges in the process, its role in drug discovery and alternative approaches to characterizing orphan GPCRs.
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Acknowledgements
Wellcome Trust (205862/Z/16/Z to F.M.) and TENOVUS (G20.09 to F.M.)
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Smith, N.J., Murray, F. Shifting our perspective on orphan G protein-coupled receptors. Nat Struct Mol Biol 31, 582–583 (2024). https://doi.org/10.1038/s41594-024-01270-1
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DOI: https://doi.org/10.1038/s41594-024-01270-1
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