Gastrin-releasing peptide receptor

The gastrin-releasing peptide receptor (GRPR), now properly known as BB2 is a G protein-coupled receptor whose endogenous ligand is gastrin releasing peptide. In humans it is highly expressed in the pancreas and is also expressed in the stomach, adrenal cortex and brain.

GRPR
Identifiers
AliasesGRPR, BB2, gastrin releasing peptide receptor, BB2R, BRS2
External IDsOMIM: 305670 MGI: 95836 HomoloGene: 21098 GeneCards: GRPR
Orthologs
SpeciesHumanMouse
Entrez

2925

14829

Ensembl

ENSG00000126010

ENSMUSG00000031364

UniProt

P30550

P21729

RefSeq (mRNA)

NM_005314

NM_008177

RefSeq (protein)

NP_005305
NP_005305.1

NP_032203

Location (UCSC)Chr X: 16.12 – 16.15 MbChr X: 162.3 – 162.33 Mb
PubMed search
Wikidata
View/Edit HumanView/Edit Mouse

Gastrin-releasing peptide (GRP) regulates numerous functions of the gastrointestinal and central nervous systems, including release of gastrointestinal hormones, smooth muscle cell contraction, and epithelial cell proliferation and is a potent mitogen for neoplastic tissues. The effects of GRP are mediated through the gastrin-releasing peptide receptor. This receptor is a glycosylated, 7-transmembrane G-protein coupled receptor that activates the phospholipase C signaling pathway. The receptor is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate. An individual with autism and multiple exostoses was found to have a balanced translocation between chromosome 8 and a chromosome X breakpoint located within the gastrin-releasing peptide receptor gene.

The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.

Activation MOR1D‐GRPR heteromers in the spinal cord mediate the common troublesome opioid-induced itch.

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