The gastrin-releasing peptide receptor (GRPR), now properly known as BB2 [5] is a G protein-coupled receptor whose endogenous ligand is gastrin releasing peptide.[6] In humans it is highly expressed in the pancreas and is also expressed in the stomach, adrenal cortex and brain.[7]
AliasesGRPR, BB2, gastrin releasing peptide receptor, BB2R, BRS2 Quick facts GRPR, Identifiers ...
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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 an X chromosome breakpoint located within the gastrin-releasing peptide receptor gene.[8][9]
The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.[10]
Activation MOR1D‐GRPR heteromers in the spinal cord mediate the common troublesome opioid-induced itch.
