Target intelligence / Profile preview

Mas-related G-protein Coupled Receptor X2 (MRGPRX2)

Target: MRGPRX2
Molecular classification: G protein-coupled receptor, GPCR, Receptor

Overview

Mas-related G-protein coupled receptor X2 (MRGPRX2) is a class A G protein-coupled receptor (GPCR) predominantly expressed on mast cells, with additional expression in sensory neurons and keratinocytes. It mediates non-IgE-dependent activation of mast cells, leading to the release of proinflammatory mediators. MRGPRX2 plays a role in pseudoallergic reactions, cutaneous inflammation, pruritus, and host defense. Targeting MRGPRX2 could provide new therapies for mast cell-dependent allergic/inflammatory disorders.

Mechanism of action

Activation of MRGPRX2 leads to mast cell degranulation and release of inflammatory mediators.

Biological functions

Mast cell degranulationSignal transductionImmune responsePain transmissionItch transmissionHost defense

Disease associations

Chronic urticariaAtopic dermatitisDrug-induced pseudoallergyInflammation

Safety considerations

Drug-induced pseudoallergic reactionsPotential for off-target effects due to GPCR promiscuityExacerbation of inflammatory conditions

Interacting drugs

Neuromuscular blocking agents (excluding succinylcholine)

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Biomarkers

MRGPRX2 expression levels in skin mast cells

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