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Target intelligence / Profile preview
Bombesin BB2 Receptor (BB2R)
- Target
- BB2R
- Molecular classification
- G protein-coupled receptor, GPCR, Bombesin receptor family
01
Overview
The Bombesin BB2 Receptor (BB2R), also known as the gastrin-releasing peptide receptor (GRPR), is a G protein-coupled receptor that binds to gastrin-releasing peptide (GRP). It plays diverse roles in the gastrointestinal system, central nervous system, and other tissues. BB2R is overexpressed in several human tumors, making it a potential target for diagnostic imaging and targeted therapy.
- Other names
- Gastrin-releasing peptide receptorGRPR
02
Mechanism of action
Gq/11 protein activation, leading to phospholipase C activation and increased intracellular calcium; Inhibition of mitogenic effects via antagonists.
03
Biological functions
Signal transductionGastrointestinal hormone release/regulationSmooth muscle contractionEpithelial cell proliferationPancreatic enzyme secretionSatiety signalingThermoregulationLearning/memoryPruritus mediationBlood pressure regulationSucrose metabolism
04
Disease associations
CancerLung cancerColon cancerProstate cancerPruritus
05
Safety considerations
Potential off-target effects of antagonists.Therapeutic challenges in delivering drugs specifically to tumor cells.
06
Interacting drugs
Gastrin-releasing peptide (GRP)
2 more in the full profile.
07
Biomarkers
BB2R overexpression in tumors
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