Mas-related G protein-coupled receptor X2 (MRGPRX2) (MRGPRX2)

Mas-related G protein-coupled receptor X2 (MRGPRX2) is a Class A G protein-coupled receptor primarily expressed on human skin mast cells and sensory neurons (Source: UniProt Q96LB1). Unlike the classical IgE-mediated pathway, MRGPRX2 is activated by a diverse array of cationic substances, including neuropeptides like Substance P, antimicrobial peptides, and various FDA-approved drugs such as fluoroquinolones and neuromuscular blockers (Source: PubMed PMID: 31108173). This activation leads to rapid mast cell degranulation and the release of pro-inflammatory mediators, which are central to the development of pseudo-allergic reactions, chronic spontaneous urticaria, and atopic dermatitis (Source: PubMed PMID: 34153480). MRGPRX2 also plays a role in neurogenic inflammation and itch by facilitating communication between the immune and nervous systems. Due to its involvement in these pathways, MRGPRX2 is a high-priority therapeutic target for treating chronic inflammatory skin diseases and drug-induced hypersensitivity. Current drug development efforts focus on small-molecule antagonists, such as EP262, which aim to block this non-IgE-mediated activation and provide a novel approach for patients who do not respond to standard antihistamine treatments (Source: Escient Pharmaceuticals).

Other names

MRGX2Mas-related gene X2 proteinG-protein coupled receptor MRGX2

Antagonism of the MRGPRX2 receptor to inhibit non-IgE-mediated mast cell degranulation and the release of pro-inflammatory mediators (Source: PubMed PMID: 34153480).