Mas-related G-protein coupled receptor member B2 (Mrgprb2) (Mrgprb2)

Mas-related G-protein coupled receptor member B2 (Mrgprb2) is a G protein-coupled receptor (GPCR) primarily expressed on the surface of connective tissue mast cells in mice, serving as the functional ortholog to the human MRGPRX2 receptor (NCBI, PMC4491428). It is a key mediator of IgE-independent mast cell activation, responding to a broad spectrum of cationic substances known as basic secretagogues, including neuropeptides like Substance P, host defense peptides such as LL-37, and various FDA-approved drugs like neuromuscular blocking agents and fluoroquinolones (PubMed: 25517090, PMC8543168). Upon activation, Mrgprb2 triggers a rapid signaling cascade involving Gi protein activation and calcium mobilization, leading to the release of inflammatory mediators such as histamine, tryptase, and cytokines (PMC8543168, PMC11516444). This pathway is critically involved in the pathogenesis of pseudo-allergic drug reactions, neurogenic inflammation, and chronic inflammatory skin diseases like rosacea and atopic dermatitis (PMC6613044, PMC11516444). Consequently, Mrgprb2 and its human counterpart are significant therapeutic targets for the development of antagonists aimed at mitigating non-IgE-mediated allergic and inflammatory conditions (Frontiers in Immunology, 2024).

Other names

Mas-related G protein-coupled receptor g14MrgB2Mas-related GPR member B2

Agonists bind to the receptor on mast cells, activating Gi protein-mediated signaling and calcium mobilization, which leads to rapid degranulation and release of inflammatory mediators like histamine and tryptase. Antagonists and inverse agonists block this activation to prevent pseudo-allergic and inflammatory responses (PMC8543168, PMC11516444).