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10 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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GRPR
gastrin releasing peptide receptor
Chromosome X · Xp22.2
NCBI Gene: 2925Ensembl: ENSG00000126010.6HGNC: HGNC:4609UniProt: P30550
70PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
protein bindingplasma membraneG protein-coupled peptide receptor activitypositive regulation of respiratory gaseous exchangeneoplasmneuroblastomaprostate cancerbreast cancer
✦AI Summary

GRPR (gastrin-releasing peptide receptor) is an X-linked G protein-coupled receptor that signals through phosphatidylinositol-calcium pathways and Akt phosphorylation 1. Functionally, GRPR mediates diverse roles across multiple neural circuits. In sensory processing, GRPR is central to itch sensation; spinal neurons expressing GRPR function as key convergent circuits for transmitting peripheral itch information to the brain, with GRP identified as an itch-specific neuropeptide distinct from pain pathways 2. GRPR regulates multiple homeostatic and behavioral functions including food intake, body temperature, memory and cognition, fear responses, depression and anxiety, circadian rhythms, and sighing behavior through modulation of specific brain nuclei including the amygdala, hypothalamus, preBötzinger complex, and suprachiasmatic nucleus 1. Clinically, GRPR has emerged as a cancer target: in melanoma and other E-cadherin-deficient cancers, GRPR participates in an oestrogen-sensitizing pathway that promotes tumor aggressiveness specifically in premenopausal women, and GRPR inhibition reduces metastasis in preclinical models 3. This G protein-coupled receptor thus represents a potential therapeutic target for sex-hormone-dependent cancers and conditions involving itch dysregulation.

Sources cited
1
GRPR distribution in brain regions, G-protein coupling mechanism, and roles in multiple functions including memory, fear, circadian rhythms, food intake, body temperature, and sighing
PMID: 37702025
2
GRP as itch-specific neuropeptide and GRPR on spinal neurons as key component of itch sensation circuit
PMID: 34663954
3
GRPR involvement in oestrogen-sensitizing pathway promoting melanoma aggressiveness in women and therapeutic potential of GRPR inhibition
PMID: 40500450
⚠Limited data available — This gene has 3 indexed publications. Summary and analysis may be incomplete.
Disease Associationsⓘ20
neoplasmOpen Targets
0.11Weak
neuroblastomaOpen Targets
0.10Weak
prostate cancerOpen Targets
0.09Suggestive
breast cancerOpen Targets
0.09Suggestive
pachyonychia congenitaOpen Targets
0.09Suggestive
lung cancerOpen Targets
0.08Suggestive
cancerOpen Targets
0.08Suggestive
lung adenocarcinomaOpen Targets
0.07Suggestive
posterior cortical atrophyOpen Targets
0.07Suggestive
small cell lung carcinomaOpen Targets
0.06Suggestive
Alzheimer diseaseOpen Targets
0.05Suggestive
autism spectrum disorderOpen Targets
0.05Suggestive
head and neck squamous cell carcinomaOpen Targets
0.04Suggestive
autismOpen Targets
0.04Suggestive
AnxietyOpen Targets
0.04Suggestive
glioblastoma multiformeOpen Targets
0.04Suggestive
attention deficit hyperactivity disorderOpen Targets
0.04Suggestive
hereditary attention deficit-hyperactivity disorderOpen Targets
0.04Suggestive
oral squamous cell carcinomaOpen Targets
0.04Suggestive
gliomaOpen Targets
0.04Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
FOLH1Protein interaction100%NMBProtein interaction100%TAC1Protein interaction98%GNAQProtein interaction97%PLCB3Protein interaction95%KNG1Protein interaction95%
Tissue Expression6 tissues
Brain
100%
Heart
87%
Bone Marrow
65%
Lung
52%
Ovary
13%
Liver
9%
Gene Interaction Network
Click a node to explore
GRPRFOLH1NMBTAC1GNAQPLCB3KNG1
PROTEIN STRUCTURE
Preparing viewer…
PDB7W41 · 2.95 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.59Moderately Constrained
pLIⓘ
0.90Intermediate
Observed/Expected LoF0.26 [0.13–0.59]
RankingsWhere GRPR stands among ~20K protein-coding genes
  • #6,720of 20,598
    Most Researched70
  • #3,986of 17,882
    Most Constrained (LOEUF)0.59 · top quartile
Genes detectedGRPR
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
PMID: 21563332
1.00
2
PMID: 21563331
0.90
3
PMID: 23166958
0.80
4
PMID: 20641919
0.70
5
Targeting GRPR for sex hormone-dependent cancer after loss of E-cadherin.
PMID: 40500450
Nature · 2025
0.60