Target intelligence / Profile preview

Neuromedin B receptor (NMBR) (NMBR)

Target
NMBR
Molecular classification
G protein-coupled receptor, Bombesin receptor family, 7-transmembrane receptor
01

Overview

The Neuromedin B receptor (NMBR), also known as the BB1 receptor, is a member of the G protein-coupled receptor (GPCR) superfamily that specifically binds the mammalian bombesin-like peptide, neuromedin B (UniProt P08910). It is predominantly expressed in the central nervous system, particularly in the hypothalamus and hippocampus, as well as in the gastrointestinal tract and pituitary gland (IUPHAR/BPS Guide to Pharmacology). NMBR mediates several physiological functions, including the regulation of smooth muscle contraction, thermoregulation, and the modulation of the stress response and satiety (Jensen et al., 2008). In oncology, NMBR is recognized for its overexpression in various cancers, including small cell lung cancer and certain types of breast and prostate tumors, where it often functions as an autocrine growth factor (PubMed: 18434540). Therapeutic strategies targeting NMBR involve the development of selective antagonists to inhibit tumor growth or the use of radiolabeled analogs for diagnostic imaging (PubMed: 22403334).

Other names
Bombesin receptor subtype 1BB1NMB-RNeuromedin-B receptor
02

Mechanism of action

Ligand binding to the Neuromedin B receptor activates the Gq/11 signaling pathway, stimulating phospholipase C (PLC) to produce inositol trisphosphate (IP3) and diacylglycerol (DAG), which leads to the mobilization of intracellular calcium and activation of protein kinase C (PKC) (Jensen et al., 2008).

03

Biological functions

Signal transductionSmooth muscle contractionThermoregulationRegulation of food intakeExocrine secretionModulation of stress response
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Disease associations

CancerObesityAnxiety disordersSmall cell lung cancer
05

Safety considerations

Potential for central nervous system side effects due to roles in thermoregulationGastrointestinal motility disturbancesPotential for off-target effects if selectivity over the Gastrin-releasing peptide receptor (BB2) is not maintained
06

Interacting drugs

Neuromedin B

4 more in the full profile.

07

Biomarkers

NMBR mRNA expression levelsNMBR protein expression in tumor tissue

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