Tchem GRPR Gastrin-releasing peptide receptor

Protein Summary

Description

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). 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]

Uniprot Accession IDs

• P30550
• B2R910
• GRP-R

Gene Name

• GRPR

Ensembl ID

• ENST00000380289
• ENSP00000369643
• ENSG00000126010

Symbol

• BB2
• BB2R

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (chemical)	0.93
small molecule perturbation	0.64
tissue	0.63
gene perturbation	0.62
protein domain	0.58

Protein Classes

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Bombesin Receptor / Gastrin-releasing Peptide Receptor

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 436.33   (req: < 5)

Gene RIFs: 43   (req: <= 3)

Antibodies: 252   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 436.33   (req: >= 5)

Gene RIFs: 43   (req: > 3)

Antibodies: 252   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 13

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 160

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0