Target intelligence / Profile preview

Neuromedin U receptor 1 (NMUR1)

Target
NMUR1
Molecular classification
G protein-coupled receptor, Membrane receptor, Family A GPCR, Receptor
01

Overview

Neuromedin U receptor 1 (NMUR1) is a G protein-coupled receptor that binds the neuropeptides neuromedin U (NMU) and neuromedin S (NMS)[3][7][10]. It is predominantly expressed in peripheral tissues, notably the gastrointestinal tract, adipose tissue, pancreas, immune cells, heart, and vascular tissue, where it regulates a broad spectrum of physiological processes, including smooth muscle contraction, energy homeostasis, vasoconstriction, stress response, and immune modulation[2][10]. NMUR1 is implicated as a therapeutic target for metabolic disorders such as obesity, as well as for certain cancers and cardiovascular diseases[3][7][9]. Selective NMUR1 agonists and antagonists are studied for their potential to modulate these processes and as tools to elucidate NMUR1 function. Importantly, the receptor’s widespread distribution necessitates caution in drug development due to possible off-target or systemic effects[6][7].

Other names
NMU1 receptorGPR66FM-3SNORF62
02

Mechanism of action

Receptor agonists/antagonists modulate signal transduction via Gq/11 protein coupling, affecting calcium signaling, smooth muscle activity, and metabolic regulation[3][6].

03

Biological functions

Signal transductionSmooth muscle contractionRegulation of energy balanceVasoconstrictionRegulation of blood pressure and local blood flowIon transport in the gutStress responseImmune response (notably in T and NK cells)
04

Disease associations

ObesityCancerInflammationSeptic shockCardiovascular diseaseBone remodeling disorders
05

Safety considerations

Cardiovascular effects (elevated blood pressure, increased heart rate with some antagonists)[6]Peripheral and central tissue distribution raising concern for off-target effects
06

Interacting drugs

Synthetic NMUR1-selective peptide agonists and antagonists (e.g., Ac-Dmt-Phe-Leu-Dmt-Arg-Pro-Arg-Asn-NH2 reported as a highly selective NMUR1 agonist)

1 more in the full profile.

07

Biomarkers

NMUR1 mRNA/protein expression in gut, adipose tissue, pancreas, cardiovascular tissue, and immune cells as potential biomarkers for efficacy monitoring or disease association[2][7].

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