Human NMUR2

Figure. Concentration-dependent activation of NMUR2 by NMU‐23

Reporter cells were transfected with either the expression plasmid for human neuromedin U receptor 2 (NMUR2) or the mock plasmid and treated with various concentrations of NMU‐23. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 390 pM.

Nomenclature
neuromedin U receptor 2
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
Panels
à la carte, Human non-orphan GPCRs

Neuromedin U receptors

Neuromedin U receptors are activated by the endogenous 25 amino acid peptide neuromedin U (neuromedin U-25, NmU-25), a peptide originally isolated from pig spinal cord [1]. In humans, NmU-25 appears to be the sole product of a precursor gene (NMU, P48645) showing a broad tissue distribution, but which is expressed at highest levels in the upper gastrointestinal tract, CNS, bone marrow and fetal liver. Much shorter versions of NmU are found in some species, but not in human, and are derived at least in some instances from the proteolytic cleavage of the longer NmU. Despite species differences in NmU structure, the C-terminal region (particularly the C-terminal pentapeptide) is highly conserved and contains biological activity. Neuromedin S (neuromedin S-33) has also been identified as an endogenous agonist [2]. NmS-33 is, as its name suggests, a 33 amino-acid product of a precursor protein derived from a single gene and contains an amidated C-terminal heptapeptide identical to NmU. NmS-33 appears to activate NMU receptors with equivalent potency to NmU-25.

References

  1. Minamino N, Kangawa K, Matsuo H. Neuromedin U-8 and U-25: novel uterus stimulating and hypertensive peptides identified in porcine spinal cord. Biochem Biophys Res Commun 1985;130:1078-85.
  2. Mori K, Miyazato M, Ida T, et al. Identification of neuromedin S and its possible role in the mammalian circadian oscillator system. EMBO J 2005;24:325-35.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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