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Target intelligence / Profile preview
Mas-related G protein-coupled receptor member X2 (MRGPRX2)
- Target
- MRGPRX2
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
MRGPRX2 is a G protein-coupled receptor (GPCR) primarily expressed in human mast cells, especially those found in the skin and connective tissues. It is activated by various exogenous and endogenous cationic substances, leading to rapid degranulation of mast cells independent of IgE/FcεRI cross-linking. It is implicated in drug-induced hypersensitivity reactions, neurogenic inflammation, and pain/itch sensation.
02
Mechanism of action
Activation of mast cells leading to degranulation and release of inflammatory mediators.
03
Biological functions
Signal transductionImmune responseHost defenseMast cell degranulationSensory perception
04
Disease associations
Drug-induced hypersensitivityInflammationNeurogenic inflammationPainItchUrticaria
05
Safety considerations
Potential for off-target effects due to broad expression and promiscuous ligand binding.Modulation of immune responses.Exacerbation of inflammatory conditions if not targeted appropriately.Pseudoallergic reactions
06
Interacting drugs
Substance P
12 more in the full profile.
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