Gastrin-releasing peptide receptor

GRPR
Identifiers
Aliases	GRPR, BB2, gastrin releasing peptide receptor, BB2R, BRS2
External IDs	OMIM: 305670; MGI: 95836; HomoloGene: 21098; GeneCards: GRPR; OMA:GRPR - orthologs
Gene location (Human)
Chr.	X chromosome (human)
End	16,153,518 bp
Gene location (Mouse)
Chr.	X chromosome (mouse)
End	162,332,673 bp
RNA expression pattern
	Top expressed in
	gonad; ; testicle; ; buccal mucosa cell; ; body of pancreas; ; pancreatic ductal cell; ; stromal cell of endometrium; ; deltoid muscle; ; epithelium of colon; ; gastric mucosa; ; smooth muscle tissue;
	Top expressed in
	lumbar spinal ganglion; ; lumbar subsegment of spinal cord; ; supraoptic nucleus; ; embryo; ; dentate gyrus of hippocampal formation granule cell; ; vestibular membrane of cochlear duct; ; ankle joint; ; tibiofemoral joint; ; genital tubercle; ; suprachiasmatic nucleus;
	More reference expression data
	More reference expression data
Gene ontology
Molecular function	signal transducer activity; G protein-coupled receptor activity; G protein-coupled peptide receptor activity; neuropeptide receptor activity; neuropeptide binding;
Cellular component	membrane; integral component of membrane; plasma membrane; integral component of plasma membrane;
Biological process	regulation of cell population proliferation; signal transduction; cell population proliferation; G protein-coupled receptor signaling pathway; psychomotor behavior; response to external biotic stimulus; phospholipase C-activating G protein-coupled receptor signaling pathway; neuropeptide signaling pathway; social behavior; motor behavior; learning or memory;
	Sources:Amigo / QuickGO
Orthologs
	2925
	14829
	ENSG00000126010
	ENSMUSG00000031364
	P30550
	P21729
	NM_005314
	NM_008177
	NP_005305; NP_005305.1
	NP_032203
	Wikidata
View/Edit Human	View/Edit Mouse

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]

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.^[8]

The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.^[9]

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

^ ^a ^b ^c GRCh38: Ensembl release 89: ENSG00000126010 – Ensembl, May 2017
^ ^a ^b ^c GRCm38: Ensembl release 89: ENSMUSG00000031364 – Ensembl, May 2017
^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ "Bombesin Receptors: BB₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
^ 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.
^ 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. doi:10.1016/S0021-9258(18)55129-2. PMID 1655761.
^ "Entrez Gene: GRPR gastrin-releasing peptide receptor".
^ 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.

[refGRCh38Ensembl-1] GRCh38: Ensembl release 89: ENSG00000126010 – Ensembl, May 2017

[refGRCm38Ensembl-2] GRCm38: Ensembl release 89: ENSMUSG00000031364 – Ensembl, May 2017

[3] "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[4] "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[IUPHAR-DB-5] "Bombesin Receptors: BB₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

[pmid7838118-6] 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.

[pmid1655761-7] 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. doi:10.1016/S0021-9258(18)55129-2. PMID 1655761.

[entrez-8] "Entrez Gene: GRPR gastrin-releasing peptide receptor".

[pmid18483184-9] 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.

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