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Papers of the Week
Inhibition of Mast Cell Degranulation by Novel Small Molecule MRGPRX2 Antagonists.
Authors
Wollam J, Solomon M, Villescaz C, Lanier M, Evans S, Bacon C, Freeman D, Vasquez A, Vest A, Napora J, Charlot B, Cavarlez C, Kim A, Dvorak L, Selfridge B, Huang L, Nevarez A, Dedman H, Brooks J, Frischbutter S, Metz M, Serhan N, Gaudenzio N, Timony G, Martinborough E, Boehm MF, Viswanath VAbstract
Mas-related G-protein coupled receptor X2 (MRGPRX2) is a promiscuous receptor on mast cells that mediates IgE-independent degranulation and has been implicated in multiple mast cell-mediated disorders, including chronic urticaria, atopic dermatitis, and pain disorders. Although it is a promising therapeutic target, few potent, selective, small molecule antagonists have been identified, and functional effects of human MRGPRX2 inhibition have not been evaluated in vivo.