MRGPRX2, active

Background Information:

The Mas‑related G protein–coupled receptor X2 (MRGPRX2) is a class A GPCR that plays a key role in mast cell–mediated immune responses, especially in non‑IgE hypersensitivity and inflammation. It is activated by a broad range of cationic ligands, including host defense peptides, neuropeptides such as substance P, and numerous small‑molecule drugs. Upon ligand binding, MRGPRX2 couples mainly to Gq and Gi proteins, triggering phospholipase C activation, intracellular calcium mobilization, and rapid mast‑cell degranulation. This leads to the release of histamine, proteases, and other pro‑inflammatory mediators that drive vasodilation, immune‑cell recruitment, and neurogenic inflammation. Through these pathways, MRGPRX2 links neuronal signals to mast‑cell activation and contributes to innate immune defense. The receptor is highly expressed in skin and connective‑tissue mast cells, positioning it as a major mediator of immediate hypersensitivity reactions.
Because of its central role in mast‑cell activation, MRGPRX2 has become an important therapeutic target in immunology and inflammatory disease research. Modulating MRGPRX2 activity offers opportunities for developing new treatments for chronic urticaria, pseudo‑allergic drug reactions, and other mast‑cell–driven disorders. Its involvement in non‑IgE–mediated hypersensitivity and increasing clinical relevance continue to drive significant interest in drug‑discovery programs aimed at reducing aberrant inflammatory and allergic responses.
Our recombinant full‑length MRGPRX2 is produced in a eukaryotic expression system to preserve native folding and essential post‑translational modifications. The purified wild‑type receptor remains structurally and functionally intact, providing a high‑quality reagent for biochemical, structural, and pharmacological studies, including ligand screening, antibody discovery, and mechanistic investigations.

Target Class:

GPCR

Sub Family:

Class A

Protein Name:

MRGPRX2

Protein Aliases:

MRGX2

UniProt Number:

Q96LB1

Gene Name:

MRGPRX2

Gene ID:

117194

Gene Aliases:

MGRG3; MRGX2

Target Species:

Human