Jun 21, 2022 · The present application describes a series of novel compounds as MrgX2 (Mas-related Gene X2) antagonists for the treatment of skin disorders, IBD, arthritis, asthma, and migraine. Further, the application discloses compounds, their preparation, use, and pharmaceutical composition, and treatment.

Recent work has emphasized the role of the Mas-related G protein-coupled receptor (MRGPR) family, specically, Mrgprb2, in mast cell activation. Mrgprb2 is fi the mouse receptor for several cationic molecules, collectively called basic secretagogues, and the ortholog of the human receptor MRGPRX2.

We showed GSK3212448 to be a potent MrgX2 agonist particularly at rat MrgX2. We screened sets of drug‐like molecules and peptides to confirm the highly promiscuous nature of MrgX2. Approximately 20% of drug‐like molecules activated MrgX2 (pEC 50 ranging from 4.5 to 6), with the principle determinant being basicity.

Mas-related G-protein coupled receptor member X2 is a protein that in humans is encoded by the MRGPRX2 gene. [5][6] It is most abundant on cutaneous mast cells, sensory neurons, and keratinocytes. [7]

In this review, we discuss the roles in innate immunity through functional studies on MRGPRX2-mediated IgE-independent MC activation and also the therapeutic potential of MRGPRX2 inhibitors on allergic and inflammatory diseases.

Dec 30, 2011 · This study identified MrgX2 as a novel G protein-coupled receptor for the antibacterial peptide LL-37 and demonstrated that unlike most G protein-coupled receptors it is resistant to agonist-induced receptor phosphorylation, desensitization, and internalization.

Sep 1, 2022 · Mas-related G-protein coupled receptor X2 (MRGPRX2) is expressed particularly on mast cells and its activation leads to the mast cell degranulation with release of inflammatory mediators. At first glance, it appears that biopharmaceuticals dodged the latest U.S. tariff bullet; med-tech, not so much.

Activation of MrgX2, an orphan G protein-coupled receptor expressed on mast cells, leads to degranulation and histamine release.

Dec 2, 2019 · Human MrgX2 binds promiscuously to structurally diverse peptides and small molecules that tend to have basic properties (basic secretagogues), resulting in acute histamine-like adverse drug reactions of injected therapeutic agents.

Apr 14, 2022 · The present application describes a series of novel compounds as MrgX2 (Mas-related Gene X2) antagonists for the treatment of skin disorders, IBD, arthritis, asthma, and migraine. Further, the application discloses compounds, their preparation, use, and pharmaceutical composition, and treatment.