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GeneE
10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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MRGPRX2
MAS related GPR family member X2
Chromosome 11 · 11p15.1
NCBI Gene: 117194Ensembl: ENSG00000183695.3HGNC: HGNC:17983UniProt: Q96LB1
71PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
chemokine-mediated signaling pathwayadenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayphospholipase C-activating G protein-coupled receptor signaling pathwaycell migrationPancreatic pseudocystanaphylaxisendometriosismajor depressive disorder
✦AI Summary

MRGPRX2 is a mast cell-specific G protein-coupled receptor that mediates IgE-independent mast cell degranulation and itch-related hypersensitivity reactions 1. The receptor recognizes basic secretagogues—cationic amphiphilic drugs and endogenous peptides—including substance P, LL-37, opioids, and compounds with cyclized tetrahydroisoquinoline structures 123. MRGPRX2 couples to both Gq and Gi proteins: Gq coupling activates phospholipase C-beta to release second messengers (DAG and IP3), while Gi coupling inhibits adenylate cyclase 23. Ligand binding triggers mast cell degranulation and histamine release, initiating pseudo-allergic reactions and neurogenic inflammation 1. Substance P activation initiates neuropeptide-mediated signaling that promotes pain and inflammation through mast cell activation and immune cell recruitment 4. MRGPRX2 dysfunction contributes to chr11 urticaria, atopic dermatitis, itch disorders, and post-stroke brain inflammation 564. Small molecule MRGPRX2 antagonists potently inhibit agonist-induced degranulation in vitro and in vivo, supporting therapeutic potential for mast cell-mediated diseases 5. Additionally, MRGPRX2 participates in rosacea pathophysiology through LL37-associated signaling cascades 7.

Sources cited
1
Demonstrates MRGPRX2/Mrgprb2 is the mast cell receptor for basic secretagogues; mediates histamine release, inflammation, and pseudo-allergic reactions to drugs and peptides
PMID: 25517090
2
Provides structural and functional evidence that MRGPRX2 couples to both Gi and Gq proteins; describes agonist-stabilized structures with cortistatin-14 and synthetic agonists
PMID: 34789874
3
Reports cryo-EM structures of MRGPRX2-Gi1 complex with polycationic compounds and inflammatory peptides; identifies structural features for sensing cationic allergens
PMID: 34789875
4
Demonstrates that novel small molecule MRGPRX2 antagonists potently inhibit agonist-induced mast cell degranulation in vitro and in vivo; supports therapeutic utility for mast cell-mediated diseases
PMID: 38971540
5
Identifies MrgprX2 as a main marker of nonhistaminergic pruriceptors; indicates role in itch pathophysiology
PMID: 37201903
6
Shows that MRGPRX2 is expressed in human meningeal mast cells and activated by substance P after stroke; regulates post-stroke brain inflammation via meningeal-brain axis
PMID: 40712576
7
Demonstrates MRGPRX2-TRPV4 signaling participates in LL37-associated pathways in rosacea pathophysiology involving mast cell activation and cytokine release
PMID: 39351216
Disease Associationsⓘ20
Pancreatic pseudocystOpen Targets
0.31Weak
anaphylaxisOpen Targets
0.08Suggestive
endometriosisOpen Targets
0.07Suggestive
major depressive disorderOpen Targets
0.06Suggestive
mycosis fungoidesOpen Targets
0.06Suggestive
inflammatory bowel diseaseOpen Targets
0.05Suggestive
strokeOpen Targets
0.05Suggestive
Alzheimer diseaseOpen Targets
0.04Suggestive
irritable bowel syndromeOpen Targets
0.04Suggestive
Recurrent infection due to specific granule deficiencyOpen Targets
0.04Suggestive
neutrophil immunodeficiency syndromeOpen Targets
0.04Suggestive
immunodeficiency 86Open Targets
0.04Suggestive
hepatorenocardiac degenerative fibrosisOpen Targets
0.04Suggestive
rosaceaOpen Targets
0.04Suggestive
renal cysts and diabetes syndromeOpen Targets
0.04Suggestive
Mayer-Rokitansky-Kuster-Hauser syndromeOpen Targets
0.03Suggestive
Mayer-Rokitansky-Küster-Hauser syndromeOpen Targets
0.03Suggestive
Mayer-Rokitansky-Kuster-Hauser syndrome type 1Open Targets
0.03Suggestive
psoriasisOpen Targets
0.03Suggestive
renal hypodysplasia/aplasia 3Open Targets
0.03Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
CORTProtein interaction100%CAMPProtein interaction98%ADMProtein interaction93%GNASProtein interaction90%GNB1Protein interaction90%CENPS-CORTProtein interaction90%
Tissue Expression6 tissues
Lung
100%
Brain
0%
Liver
0%
Heart
0%
Ovary
0%
Bone Marrow
0%
Gene Interaction Network
Click a node to explore
MRGPRX2CORTCAMPADMGNASGNB1CENPS-CORT
PROTEIN STRUCTURE
Preparing viewer…
PDB7S8L · 2.45 Å · EM
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.89LoF Tolerant
pLIⓘ
0.29Tolerant
Observed/Expected LoF0.00 [0.00–1.89]
RankingsWhere MRGPRX2 stands among ~20K protein-coding genes
  • #6,646of 20,598
    Most Researched71
  • #17,191of 17,882
    Most Constrained (LOEUF)1.89
Genes detectedMRGPRX2
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Signaling pathways and targeted therapy for rosacea.
PMID: 39351216
Front Immunol · 2024
1.00
2
Identification of a mast-cell-specific receptor crucial for pseudo-allergic drug reactions.
PMID: 25517090
Nature · 2015
0.90
3
Inhibition of mast cell degranulation by novel small molecule MRGPRX2 antagonists.
PMID: 38971540
J Allergy Clin Immunol · 2024
0.80
4
Basic mechanisms of itch.
PMID: 37201903
J Allergy Clin Immunol · 2023
0.70
5
Structure, function and pharmacology of human itch GPCRs.
PMID: 34789874
Nature · 2021
0.60