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 glyco... See more...

Aliases for GRPR Gene

Aliases for GRPR Gene

  • Gastrin Releasing Peptide Receptor 2 3 5
  • Gastrin-Releasing Peptide Receptor 3 4
  • GRP-Preferring Bombesin Receptor 3 4
  • Bombesin Receptor 2 2 3
  • GRP-R 3 4
  • BB2R 2 3
  • BB2 2 3
  • GRPR 5

External Ids for GRPR Gene

Previous GeneCards Identifiers for GRPR Gene

  • GC0XP015862
  • GC0XP014967
  • GC0XP015343
  • GC0XP015503
  • GC0XP015901
  • GC0XP016051
  • GC0XP013896

Summaries for GRPR Gene

Entrez Gene Summary for GRPR Gene

  • 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. [provided by RefSeq, Jul 2008]

GeneCards Summary for GRPR Gene

GRPR (Gastrin Releasing Peptide Receptor) is a Protein Coding gene. Diseases associated with GRPR include Agoraphobia and Autism. Among its related pathways are RET signaling and Signaling by GPCR. Gene Ontology (GO) annotations related to this gene include G protein-coupled receptor activity and bombesin receptor activity. An important paralog of this gene is NMBR.

UniProtKB/Swiss-Prot Summary for GRPR Gene

  • Receptor for gastrin-releasing peptide (GRP) (PubMed:1655761). Signals via association with G proteins that activate a phosphatidylinositol-calcium second messenger system, resulting in Akt phosphorylation. Contributes to the regulation of food intake. Contributes to the perception of prurient stimuli and transmission of itch signals in the spinal cord that promote scratching behavior, but does not play a role in the perception of pain. Contributes primarily to nonhistaminergic itch sensation. Contributes to long-term fear memory, but not normal spatial memory (By similarity).

Tocris Summary for GRPR Gene

  • Bombesin receptors are activated by the endogenous ligands gastrin-releasing peptide (GRP), neuromedin B (NMB) and GRP18-27 (neuromedin C). Three subtypes of bombesin receptor are known: BB1, BB2 and an orphan receptor (bb3).

Gene Wiki entry for GRPR Gene

Additional gene information for GRPR Gene

No data available for CIViC Summary , PharmGKB "VIP" Summary , Rfam classification and piRNA Summary for GRPR Gene

Genomics for GRPR Gene

GeneHancer (GH) Regulatory Elements Pubs

Promoters and enhancers for GRPR Gene
GeneHancer (GH) Identifier GH Type GH
Score
GH Sources Gene Association Score Total Score TSS distance (kb) Number of Genes Away Size (kb) Transcription Factor
Binding Sites
Gene Targets
GH0XJ015852 Promoter/Enhancer 2.2 EPDnew FANTOM5 Ensembl ENCODE CraniofacialAtlas 600.1 -269.1 -269149 5.6 CREB1 HNRNPL PRDM10 REST ZNF629 TFE3 IKZF1 ZNF692 POLR2A JUND AP1S2 lnc-ZRSR2-5 GRPR ZRSR2 CA5B lnc-CLTRN-3
GH0XJ016122 Promoter/Enhancer 1.3 EPDnew Ensembl ENCODE 600.7 +2.2 2227 5.6 CREB1 CTCF FOXA1 REST RAD21 TRIM22 SMC3 NFYB RFX5 ZNF384 GRPR ZRSR2 MAGEB17
GH0XJ016123 Promoter 0.4 EPDnew 600.7 -1.3 -1293 0.1 CTCF GRPR piR-33804-168 AP1S2
GH0XJ016184 Enhancer 1.1 Ensembl ENCODE dbSUPER 12.9 +63.1 63135 4.2 JUND PKNOX1 DPF2 YY1 ZNF37A HMBOX1 RUNX3 NFE2 ZNF316 USF1 TXLNG GRPR CTPS2 ZRSR2 ENSG00000238178 RPL6P30 MAGEB17 S100G
GH0XJ015977 Enhancer 0.9 Ensembl ENCODE 12.1 -147.9 -147864 6.2 CTCF LEF1 REST RAD21 TRIM22 DPF2 HDAC1 YY1 SOX6 TCF12 GRPR AP1S2 piR-38351-509 RF00017-8176
- Elite GeneHancer and/or Elite GeneHancer-gene association Download GeneHancer data from 2017 publication | Request up-to-date GeneHancer data (full dataset)

GeneHancers around GRPR on the GeneHancer Hub at the UCSC Golden Path

Cistromic (ChIP-Seq) regulation report from SPP (The Signaling Pathways Project) for GRPR

Top Transcription factor binding sites by QIAGEN in the GRPR gene promoter:
  • AML1a
  • c-Myb
  • CUTL1
  • E47
  • HNF-3beta
  • Lmo2
  • Nkx2-5
  • Sox5
  • STAT5A

Genomic Locations for GRPR Gene

Genomic Locations for GRPR Gene
chrX:16,123,565-16,153,518
(GRCh38/hg38)
Size:
29,954 bases
Orientation:
Plus strand
chrX:16,141,424-16,171,641
(GRCh37/hg19)
Size:
30,218 bases
Orientation:
Plus strand

Genomic View for GRPR Gene

Genes around GRPR on UCSC Golden Path with GeneCards custom track

Cytogenetic band:
GRPR Gene in genomic location: bands according to Ensembl, locations according to GeneLoc (and/or Entrez Gene and/or Ensembl if different)
Genomic Location for GRPR Gene
GeneLoc Logo Genomic Neighborhood Exon StructureGene Density

RefSeq DNA sequence for GRPR Gene

Proteins for GRPR Gene

  • Protein details for GRPR Gene (UniProtKB/Swiss-Prot)

    Protein Symbol:
    P30550-GRPR_HUMAN
    Recommended name:
    Gastrin-releasing peptide receptor
    Protein Accession:
    P30550
    Secondary Accessions:
    • B2R910

    Protein attributes for GRPR Gene

    Size:
    384 amino acids
    Molecular mass:
    43199 Da
    Quaternary structure:
    No Data Available

neXtProt entry for GRPR Gene

Post-translational modifications for GRPR Gene

  • Glycosylation at Asn20
  • Modification sites at PhosphoSitePlus

Other Protein References for GRPR Gene

ENSEMBL proteins:
REFSEQ proteins:

No data available for DME Specific Peptides for GRPR Gene

Domains & Families for GRPR Gene

Gene Families for GRPR Gene

HGNC:
IUPHAR :
Human Protein Atlas (HPA):
  • G-protein coupled receptors
  • Predicted membrane proteins

Protein Domains for GRPR Gene

InterPro:
Blocks:
  • Bombesin receptor signature
  • Gastrin-releasing peptide receptor signature
ProtoNet:

Suggested Antigen Peptide Sequences for GRPR Gene

GenScript: Design optimal peptide antigens:
  • GRP-preferring bombesin receptor (GRPR_HUMAN)

Graphical View of Domain Structure for InterPro Entry

P30550

UniProtKB/Swiss-Prot:

GRPR_HUMAN :
  • Belongs to the G-protein coupled receptor 1 family.
Family:
  • Belongs to the G-protein coupled receptor 1 family.
genes like me logo Genes that share domains with GRPR: view

Function for GRPR Gene

Molecular function for GRPR Gene

UniProtKB/Swiss-Prot Function:
Receptor for gastrin-releasing peptide (GRP) (PubMed:1655761). Signals via association with G proteins that activate a phosphatidylinositol-calcium second messenger system, resulting in Akt phosphorylation. Contributes to the regulation of food intake. Contributes to the perception of prurient stimuli and transmission of itch signals in the spinal cord that promote scratching behavior, but does not play a role in the perception of pain. Contributes primarily to nonhistaminergic itch sensation. Contributes to long-term fear memory, but not normal spatial memory (By similarity).
GENATLAS Biochemistry:
gastrin releasing peptide receptor

Phenotypes From GWAS Catalog for GRPR Gene

Gene Ontology (GO) - Molecular Function for GRPR Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0004930 G protein-coupled receptor activity IBA 21873635
GO:0008188 neuropeptide receptor activity IEA,ISS --
GO:0008528 G protein-coupled peptide receptor activity TAS,IDA 1655761
GO:0042923 neuropeptide binding IEA --
genes like me logo Genes that share ontologies with GRPR: view
genes like me logo Genes that share phenotypes with GRPR: view

Animal Models for GRPR Gene

MGI Knock Outs for GRPR:

Animal Model Products

CRISPR Products

miRNA for GRPR Gene

miRTarBase miRNAs that target GRPR

Inhibitory RNA Products

  • Search GeneCopoeia for shRNA, lentivirus and/or AAV clone products for GRPR

No data available for Enzyme Numbers (IUBMB) , Human Phenotype Ontology , Transcription Factor Targets and HOMER Transcription for GRPR Gene

Localization for GRPR Gene

Subcellular locations from UniProtKB/Swiss-Prot for GRPR Gene

Cell membrane. Multi-pass membrane protein.

Subcellular locations from

COMPARTMENTS
Extracellular space Cytosol Plasma membrane Cytoskeleton Lysosome Endosome Peroxisome ER Golgi Apparatus Nucleus Mitochondrion 0 1 2 3 4 5 Confidence
COMPARTMENTS Subcellular localization image for GRPR gene
Compartment Confidence
plasma membrane 5
extracellular 2
nucleus 2
cytoskeleton 1
mitochondrion 1
endoplasmic reticulum 1
endosome 1
cytosol 1
lysosome 1

Subcellular locations from the

Human Protein Atlas (HPA)
  • Plasma membrane (3)
See all subcellular structures

Gene Ontology (GO) - Cellular Components for GRPR Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0005886 plasma membrane TAS --
GO:0005887 integral component of plasma membrane IEA,ISS --
GO:0016020 membrane IEA --
GO:0016021 integral component of membrane IEA --
genes like me logo Genes that share ontologies with GRPR: view

Pathways & Interactions for GRPR Gene

genes like me logo Genes that share pathways with GRPR: view

SIGNOR curated interactions for GRPR Gene

Activates:
Is activated by:

Gene Ontology (GO) - Biological Process for GRPR Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0007165 signal transduction IEA --
GO:0007186 G protein-coupled receptor signaling pathway TAS --
GO:0007200 phospholipase C-activating G protein-coupled receptor signaling pathway IEA,ISS --
GO:0007218 neuropeptide signaling pathway IEA --
GO:0007611 learning or memory IEA --
genes like me logo Genes that share ontologies with GRPR: view

Drugs & Compounds for GRPR Gene

(42) Drugs for GRPR Gene - From: ApexBio, DGIdb, IUPHAR, HMDB, Tocris, and Novoseek

Name Status Disease Links Group Role Mechanism of Action Clinical Trials
Bombesin Investigational Pharma Agonist, Full agonist Involved in gastrointestinal tract function 16
ranatensin Pharma Agonist, Full agonist 0
BIM 187 Pharma Bombesin/GRP receptor agonist 0
(D-Ala<sup>11</sup>]bombesin Pharma Agonist, Full agonist 0
[(3-Ph-Pr<sup>6</sup>), His<sup>7</sup>,D-Ala<sup>11</sup>,D-Pro<sup>13</sup>,&psi;13-14),Phe<sup>14</sup>]bombesin-(6-14) Pharma Antagonist 0

(14) Additional Compounds for GRPR Gene - From: IUPHAR, Novoseek, and Tocris

Name Synonyms Role CAS Number PubChem IDs PubMed IDs
10-OBn-7&alpha;-F-gingkolide B
Agonist, Full agonist
D-Tpi<sup>6</sup>, Leu13 &psi;(CH<sub>2</sub>NH)-Leu14)bombesin (6-14)
Antagonist
gastrin releasing peptide (14-27) (human)
Agonist, Full agonist
JMV641
Antagonist
BA 1
183241-31-8

(5) Tocris Compounds for GRPR Gene

Compound Action Cas Number
BA 1 Potent BRS-3 agonist; also NMBR and GRPR agonist 183241-31-8
BIM 187 Bombesin/GRP receptor agonist 137734-88-4
Bombesin Involved in gastrointestinal tract function 31362-50-2
GRP (human) Endogenous GRP receptor agonist 93755-85-2
GRP (porcine) Endogenous GRP receptor agonist 74815-57-9

(1) ApexBio Compounds for GRPR Gene

Compound Action Cas Number
BIM 187 Bombesin/GRP receptor agonist 137734-88-4
genes like me logo Genes that share compounds with GRPR: view

Drug Products

Transcripts for GRPR Gene

mRNA/cDNA for GRPR Gene

1 REFSEQ mRNAs :
7 NCBI additional mRNA sequence :
1 Ensembl transcripts including schematic representations, and UCSC links to gene/alias where relevant :

CRISPR Products

Inhibitory RNA Products

  • Search GeneCopoeia for shRNA, lentivirus and/or AAV clone products for GRPR

Alternative Splicing Database (ASD) splice patterns (SP) for GRPR Gene

No ASD Table

Relevant External Links for GRPR Gene

GeneLoc Exon Structure for
GRPR

Expression for GRPR Gene

mRNA expression in normal human tissues from GTEx, Illumina, BioGPS, and SAGE for GRPR Gene

mRNA expression in embryonic tissues and stem cells from LifeMap Discovery

mRNA differential expression in normal tissues according to GTEx for GRPR Gene

This gene is overexpressed in Pancreas (x18.2), Esophagus - Gastroesophageal Junction (x7.9), and Esophagus - Muscularis (x7.0).

Transcriptomic regulation report from SPP (The Signaling Pathways Project) for GRPR

SOURCE GeneReport for Unigene cluster for GRPR Gene:

Hs.567282

mRNA Expression by UniProt/SwissProt for GRPR Gene:

P30550-GRPR_HUMAN
Tissue specificity: Highly expressed in pancreas. Also expressed in stomach, adrenal cortex and brain.

Evidence on tissue expression from TISSUES for GRPR Gene

  • Nervous system(4.5)
  • Lung(4.3)
  • Pancreas(2.7)
  • Muscle(2.2)
  • Intestine(2.1)
  • Kidney(2)
genes like me logo Genes that share expression patterns with GRPR: view

No data available for Protein differential expression in normal tissues , Protein expression , Protein tissue co-expression partners and Phenotype-based relationships between genes and organs from Gene ORGANizer for GRPR Gene

Orthologs for GRPR Gene

This gene was present in the common ancestor of animals.

Orthologs for GRPR Gene

Organism Taxonomy Gene Similarity Type Details
Chimpanzee
(Pan troglodytes)
Mammalia GRPR 30 31
  • 99.39 (n)
OneToOne
Cow
(Bos Taurus)
Mammalia GRPR 30 31
  • 90.71 (n)
OneToOne
Dog
(Canis familiaris)
Mammalia GRPR 30 31
  • 90.54 (n)
OneToOne
Mouse
(Mus musculus)
Mammalia Grpr 30 17 31
  • 87.73 (n)
OneToOne
Rat
(Rattus norvegicus)
Mammalia Grpr 30
  • 87.64 (n)
Oppossum
(Monodelphis domestica)
Mammalia GRPR 31
  • 86 (a)
OneToOne
Platypus
(Ornithorhynchus anatinus)
Mammalia GRPR 31
  • 77 (a)
OneToOne
Chicken
(Gallus gallus)
Aves GRPR 30 31
  • 77.6 (n)
OneToOne
Lizard
(Anolis carolinensis)
Reptilia GRPR 31
  • 67 (a)
OneToOne
Tropical Clawed Frog
(Silurana tropicalis)
Amphibia grpr 30
  • 72.11 (n)
Zebrafish
(Danio rerio)
Actinopterygii grpr 30 31
  • 71.47 (n)
OneToOne
Fruit Fly
(Drosophila melanogaster)
Insecta CG30106 32
  • 37 (a)
CCHa2r 31
  • 27 (a)
ManyToMany
CCHa1r 31
  • 27 (a)
ManyToMany
Worm
(Caenorhabditis elegans)
Secernentea ZK455.3 32
  • 29 (a)
Species where no ortholog for GRPR was found in the sources mined by GeneCards:
  • A. gosspyii yeast (Eremothecium gossypii)
  • Actinobacteria (Mycobacterium tuberculosis)
  • African clawed frog (Xenopus laevis)
  • African malaria mosquito (Anopheles gambiae)
  • Alicante grape (Vitis vinifera)
  • Alpha proteobacteria (Wolbachia pipientis)
  • Amoeba (Dictyostelium discoideum)
  • Archea (Pyrococcus horikoshii)
  • Baker's yeast (Saccharomyces cerevisiae)
  • Barley (Hordeum vulgare)
  • Beta proteobacteria (Neisseria meningitidis)
  • Bread mold (Neurospora crassa)
  • Chromalveolata (Phytophthora infestans)
  • Common water flea (Daphnia pulex)
  • Corn (Zea mays)
  • E. coli (Escherichia coli)
  • Filamentous fungi (Aspergillus nidulans)
  • Firmicute Bacteria (Streptococcus pneumoniae)
  • Fission Yeast (Schizosaccharomyces pombe)
  • Green Algae (Chlamydomonas reinhardtii)
  • Honey Bee (Apis mellifera)
  • K. Lactis Yeast (Kluyveromyces lactis)
  • Loblloly Pine (Pinus taeda)
  • Malaria Parasite (Plasmodium falciparum)
  • Medicago Trunc (Medicago Truncatula)
  • Moss (Physcomitrella patens)
  • Orangutan (Pongo pygmaeus)
  • Pig (Sus scrofa)
  • Rainbow Trout (Oncorhynchus mykiss)
  • Rice (Oryza sativa)
  • Rice Blast Fungus (Magnaporthe grisea)
  • Schistosome Parasite (Schistosoma mansoni)
  • Sea Anemone (Nematostella vectensis)
  • Sea Vase (Ciona intestinalis)
  • Sea Squirt (Ciona savignyi)
  • Sea Urchin (Strongylocentrotus purpuratus)
  • Sorghum (Sorghum bicolor)
  • Soybean (Glycine max)
  • Stem Rust Fungus (Puccinia graminis)
  • Sugarcane (Saccharum officinarum)
  • Thale Cress (Arabidopsis thaliana)
  • Tomato (Lycopersicon esculentum)
  • Toxoplasmosis (Toxoplasma gondii)
  • Trichoplax (Trichoplax adhaerens)
  • Wheat (Triticum aestivum)

Evolution for GRPR Gene

ENSEMBL:
Gene Tree for GRPR (if available)
TreeFam:
Gene Tree for GRPR (if available)
Aminode:
Evolutionary constrained regions (ECRs) for GRPR: view image

Paralogs for GRPR Gene

(7) SIMAP similar genes for GRPR Gene using alignment to 1 proteins:

  • GRPR_HUMAN
genes like me logo Genes that share paralogs with GRPR: view

Variants for GRPR Gene

Sequence variations, with clinical significance, from ClinVar and Humsavar, with links to dbSNP for GRPR Gene

SNP ID Clinical significance and condition Chr 0X pos Variation AA Info Type
721453 Likely Benign: not provided 16,123,970(+) G/C MISSENSE_VARIANT
745044 Likely Benign: not provided 16,152,642(+) C/G SYNONYMOUS_VARIANT
748394 Likely Benign: not provided 16,152,576(+) G/A SYNONYMOUS_VARIANT
753760 Likely Benign: not provided 16,150,395(+) C/T SYNONYMOUS_VARIANT
780684 Likely Benign: not provided 16,150,549(+) G/A MISSENSE_VARIANT

Additional dbSNP identifiers (rs#s) for GRPR Gene

Structural Variations from Database of Genomic Variants (DGV) for GRPR Gene

Variant ID Type Subtype PubMed ID
nsv436917 CNV insertion 17901297

Variation tolerance for GRPR Gene

Residual Variation Intolerance Score: 39.5% of all genes are more intolerant (likely to be disease-causing)
Gene Damage Index Score: 1.24; 24.77% of all genes are more intolerant (likely to be disease-causing)

Additional Variant Information for GRPR Gene

Human Gene Mutation Database (HGMD)
GRPR
SNPedia medical, phenotypic, and genealogical associations of SNPs for
GRPR

SNP Genotyping and Copy Number Assay Products

No data available for Polymorphic Variants from UniProtKB/Swiss-Prot for GRPR Gene

Disorders for GRPR Gene

MalaCards: The human disease database

(10) MalaCards diseases for GRPR Gene - From: DISEASES, Novoseek, and GeneCards

Disorder Aliases PubMed IDs
agoraphobia
  • fear of open spaces
autism
  • autistic disorder
small cell cancer of the lung
  • sclc1
prostate cancer
  • prostate cancer, somatic
lung cancer
  • adenocarcinoma of lung
- elite association - COSMIC cancer census association via MalaCards
Search GRPR in MalaCards View complete list of genes associated with diseases

Additional Disease Information for GRPR

Genetic Association Database
(GAD)
Human Genome Epidemiology Navigator
(HuGE)
ATLAS of Genetics and Cytogenetics in Oncology and Haematology
Open Targets Platform
genes like me logo Genes that share disorders with GRPR: view

No data available for UniProtKB/Swiss-Prot and Genatlas for GRPR Gene

Publications for GRPR Gene

  1. Panic disorder is associated with the serotonin transporter gene (SLC6A4) but not the promoter region (5-HTTLPR). (PMID: 18663369) Strug LJ … Weissman MM (Molecular psychiatry 2010) 3 23 41
  2. Association and linkage analysis of candidate genes GRP, GRPR, CRHR1, and TACR1 in panic disorder. (PMID: 18452185) Hodges LM … Hamilton SP (American journal of medical genetics. Part B, Neuropsychiatric genetics : the official publication of the International Society of Psychiatric Genetics 2009) 3 23 41
  3. Gastrin-releasing peptide receptor (GRPR) locus in Japanese subjects with autism. (PMID: 14729406) Marui T … Sasaki T (Brain & development 2004) 3 23 41
  4. The human gastrin-releasing peptide receptor gene structure, its tissue expression and promoter. (PMID: 11245983) Xiao D … Weber HC (Gene 2001) 3 4 23
  5. Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells. (PMID: 1655761) Corjay MH … Battey JF (The Journal of biological chemistry 1991) 3 4 23

Products for GRPR Gene

Sources for GRPR Gene