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Target intelligence / Profile preview
Bombesin Receptor Subtype 3 (BRS-3)
- Target
- BRS-3
- Molecular classification
- G protein-coupled receptor
01
Overview
Bombesin receptor subtype 3 (BRS-3) is a G protein-coupled receptor (GPCR) classified as an orphan receptor because no high-affinity endogenous ligand has been identified for it in mammals. It is primarily expressed in the CNS, particularly the hypothalamus, and plays key roles in regulating food intake, energy expenditure, body temperature, and cardiovascular function. BRS-3 couples to Gq proteins, activating phospholipase C and increasing intracellular calcium levels. Research indicates that altered BRS-3 function is linked to obesity, diabetes mellitus, lung cancer, asthma, and kidney diseases, making it a potential therapeutic target for these conditions.
- Other names
- BB3bombesin-like receptor 3BB3RBBR3
02
Mechanism of action
Activation of Gq proteins, leading to increased intracellular calcium levels and activation of downstream signaling pathways such as PLC/PKC and MAPK pathways.
03
Biological functions
Regulation of food intake/appetite controlEnergy expenditure/metabolic rate regulationBody temperature homeostasisHeart rate and blood pressure modulationSignal transduction
04
Disease associations
ObesityDiabetes mellitusLung cancerAsthmaKidney diseases
05
Safety considerations
Limited selectivity of some ligands due to cross-reactivity with other bombesin receptors.Species-specific differences in binding affinities.Potential for off-target effects due to widespread tissue distribution.
06
Interacting drugs
[D-Tyr^6,^β-Ala^11,^Phe^13,^Nle^14]Bn-(6–14)
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