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Target intelligence / Profile preview
Bombesin Receptor Subtype 2 (BB2)
- Target
- BB2
- Molecular classification
- G protein-coupled receptor (GPCR), Receptor
01
Overview
Bombesin receptor subtype 2, also known as the gastrin-releasing peptide receptor (GRPR), is a G protein-coupled receptor primarily activated by gastrin-releasing peptide (GRP). It mediates a wide range of physiological and pathophysiological processes including stimulation of tissue growth, smooth muscle contraction, regulation of gastrointestinal motility, modulation of feeding behavior, respiratory regulation, central nervous system effects, and immune system modulation. Its involvement in cancer and pruritus makes it a target for diagnostic imaging and therapy.
- Other names
- Gastrin-releasing peptide receptorGRPR
02
Mechanism of action
Antagonism of GRPR, blocking GRP binding and downstream signaling
03
Biological functions
Signal transductionSmooth muscle contractionRegulation of gastrointestinal motilityRegulation of secretionModulation of feeding behaviorRespiratory regulationMemory processingCircadian rhythm regulationBody temperature controlMediation of pruritusLymphoid function regulationNeutrophil function regulationCell proliferation
04
Disease associations
CancerPruritusLung development and injuryGastrointestinal disordersCNS Disorders
05
Safety considerations
Off-target effects of antagonists
06
Interacting drugs
Selective GRPR antagonists
07
Biomarkers
GRPR overexpression in tumors (e.g., small cell lung cancer, prostate cancer, breast cancer, pancreatic cancer)
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