GRPR (Gastrin Releasing Peptide Receptor)
A G protein-coupled receptor involved in cancer, neurological disorders, and inflammation.
Gene Information Card
| Symbol | GRPR |
|---|---|
| Full Name | Gastrin Releasing Peptide Receptor |
| Gene Type | protein-coding |
| Chromosomal Location | Xp22.2 |
| NCBI Gene ID | 2925 ncbi.nlm.nih.gov/gene/2925 |
| Ensembl ID | ENSG00000169083 |
| UniProt ID | P30550 |
| OMIM ID | 305670 |
| HGNC ID | 4605 |
| Aliases | BB2, GRP-R, GRPR1 |
Description
GRPR encodes a G protein-coupled receptor for gastrin-releasing peptide (GRP). It is involved in smooth muscle contraction, cell proliferation, and neuroendocrine signaling. Aberrant expression and mutations are linked to various cancers, neurological disorders, and inflammatory conditions.
Disease Associations
| Disease category | Pathophysiological mechanism | Genomic evidence |
|---|---|---|
| Prostate Cancer | GRPR overexpression promotes cell proliferation via MAPK/ERK signaling | PMID: 25788277 |
| Small Cell Lung Cancer | Autocrine GRP/GRPR loop drives tumor growth | PMID: 2150254 |
| Pruritus (Itch) | GRPR signaling in spinal cord mediates itch transmission | PMID: 19661919 |
| Autism Spectrum Disorder | GRPR variants associated with altered neurodevelopment | PMID: 22495306 |
| Inflammatory Bowel Disease | GRPR activation modulates intestinal inflammation | PMID: 25411204 |
Expression Profile
Tissue Expression
| Tissue | nTPM | level |
|---|---|---|
| Pancreas | 12.3 | Medium |
| Prostate | 8.7 | Medium |
| Stomach | 6.5 | Low |
| Small Intestine | 5.2 | Low |
| Brain (cerebellum) | 4.1 | Low |
| Lung | 2.8 | Not detected |
Cell Line Expression
| Cell Line | nTPM | Notes |
|---|---|---|
| PC-3 (prostate cancer) | 15.6 | High expression |
| NCI-H69 (SCLC) | 22.1 | Very high expression |
| HEK293 | 1.2 | Low expression |
| MCF7 (breast cancer) | 0.8 | Not detected |
Data source：Human Protein Atlas（proteinatlas.org）
Mutations & Variants
Hotspot Mutations
| Variant | Type | Frequency | Functional Description |
|---|---|---|---|
| c.107C>T (p.Pro36Leu) | Missense | <0.01% | Unknown functional effect |
| c.374G>A (p.Arg125His) | Missense | <0.01% | Altered ligand binding |
| c.682C>T (p.Arg228Cys) | Missense | <0.01% | Reduced cell surface expression |
Mutation functional classification
Loss of Function (LOF)
p.Arg228Cys reduces receptor trafficking to membrane.
Gain of Function (GOF)
Not reported in literature.
Dominant Negative (DN)
Not reported in literature.
View complete mutation data：
Gene Ontology (GO)
Pathways
• GPCR downstream signaling (Reactome R-HSA-388396)
• GRP/GRPR signaling in cancer (KEGG hsa05200)
• Neuroactive ligand-receptor interaction (KEGG hsa04080)
Protein Summary
GRPR is a 384-amino acid seven-transmembrane G protein-coupled receptor. Upon binding GRP, it activates phospholipase C, leading to calcium mobilization and MAPK pathway activation. It is a target for radiolabeled antagonists in cancer imaging and therapy.
Related Services
Related Products
| Product name | Cat.No. | Species | Gene ID | |
|---|---|---|---|---|
| GRPR Knockout HCT 116 Cell Line | EDJ-KQ21272 | Human | 2925 | Details Get a Quote |
| GRPR Knockout HeLa Cell Line | EDJ-KQ53446 | Human | 2925 | Details Get a Quote |
| GRPR Knockout A-549 Cell Line | EDJ-KQ61920 | Human | 2925 | Details Get a Quote |
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