ArticleJournal of the American Chemical Society2026
GPR3 Ligands Discovered through Combined Virtual and Conformational Biosensor-Based Screening.
Article in Journal of the American Chemical Society, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed.
- Structure-based screening and a conformational biosensor identify a GPR183 inverse agonist and an activation switch.Nature communications · 2026Article
- Cold exposure induces the constitutively active thermogenic receptor, GPR3, via ERRα and ERRγ.Molecular metabolism · 2026Article
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Authors and funding
15 authors.
Funding
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Abstract
GPR3 belongs to the protein superfamily of G protein-coupled receptors (GPCRs) and plays a central role in both benign and malignant physiological processes, such as energy expenditure in adipocytes and Alzheimer's disease pathology, respectively. Despite the therapeutic potential of both receptor agonists and inverse agonists, GPR3 so far has lacked drug-like ligands and innovative screening technologies, hindering effective drug discovery efforts targeting this receptor. To overcome the limitations of conventional ligand screening techniques based on cAMP accumulation or β-arrestin recruitment, we developed a conformational GPR3 biosensor to monitor receptor activity in living cells with high-throughput screening (HTS)-compatible sensitivity and robustness. Combined with virtual compound screening against homology models of GPR3 and classical medicinal chemistry, this biosensor enabled us to identify new ligands, one of which (compound
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