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Target intelligence / Profile preview
Mas-related G protein-coupled receptor X4 (MRGPRX4)
- Target
- MRGPRX4
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor, Class A (rhodopsin-like) GPCR, Delta subfamily GPCR
01
Overview
Mas-related G protein-coupled receptor X4 (MRGPRX4) is a Gq-coupled GPCR primarily expressed in small-diameter sensory neurons and skin keratinocytes. It is activated by bile acids and bilirubin, playing a key role in nonhistaminergic itch associated with cholestatic liver diseases. Recent development of selective agonists offers potential for anti-pruritic therapies. RAMP2 interaction reduces receptor signaling.
- Other names
- GPCRMRGX4SNSR6MAS related GPR family member X4
02
Mechanism of action
Gq-coupled GPCR activation leading to PLCβ stimulation and increased intracellular calcium levels.
03
Biological functions
Signal transductionSensory perception of itchPain transmission (proposed)Inflammation (proposed)Wound healing (proposed)Cellular responses via PLCβ and Ca2+ signaling
04
Disease associations
Cholestatic pruritusItchCancer progression (suggested)Liver diseases
05
Safety considerations
Off-target activation by some drugs can lead to pruritus or urticarial rash.Limited research on selective agonists/antagonists.
06
Interacting drugs
Bile acids
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