The orphan MAS-related G protein-coupled receptor member X2 (MRGPRX2) is expressed primarily in human dorsal root ganglia and mast cells, and has been suggested to modulate pain and itch. Using a high-throughput screen of 5,695 unique compounds, Lansu et al. discovered that many exogenous and endogenous opioids are agonists of MRGPRX2. Subsequent in silico structure-based modelling and docking identified the potent and highly selective MRGPRX2 probe ZINC-3573. The MRGPRX2-activating opioids and ZINC-3573 induced intracellular Ca2+ release and degranulation in a human mast cell line.
References
Lansu, K. et al. In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat. Chem. Bio. http://dx.doi.org/10.1038/nchembio.2334 (2017)
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Sarah, C. Novel probe for MRGPRX2. Nat Rev Drug Discov 16, 314 (2017). https://doi.org/10.1038/nrd.2017.77
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DOI: https://doi.org/10.1038/nrd.2017.77
