Gastrin-releasing peptide receptor

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The gastrin-releasing peptide receptor (GRPR), now properly known as BB2 [1] is a G protein-coupled receptor whose endogenous ligand is gastrin releasing peptide.[2] In humans it is highly expressed in the pancreas and is also expressed in the stomach, adrenal cortex and brain.[3]

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.[4]

The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.[5]

References

  1. "Bombesin Receptors: BB2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
  2. Benya RV, Kusui T, Pradhan TK, Battey JF, Jensen RT (1995). "Expression and characterization of cloned human bombesin receptors". Mol. Pharmacol. 47 (1): 10–20. PMID 7838118.
  3. Corjay MH, Dobrzanski DJ, Way JM, Viallet J, Shapira H, Worland P, Sausville EA, Battey JF (1991). "Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells". J. Biol. Chem. 266 (28): 18771–18779. PMID 1655761.
  4. "Entrez Gene: GRPR gastrin-releasing peptide receptor".
  5. Chinnappan D, Qu X, Xiao D, Ratnasari A, Weber HC (May 2008). "Human gastrin-releasing peptide receptor gene regulation requires transcription factor binding at two distinct CRE sites". Am. J. Physiol. Gastrointest. Liver Physiol. 295 (1): G153–G162. doi:10.1152/ajpgi.00036.2008. PMC 2494719. PMID 18483184.

Further reading

External links

This article incorporates text from the United States National Library of Medicine, which is in the public domain.


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