pe
pep-10539 v1 CC-BY-SA-4.0

Neuromedin U-8: gut-brain peptide fragment (NMU-8)

A short natural peptide found in the gut and brain, studied in the lab for its effects on pain and mood-related signals and its links to pancreatic cancer research.

statussynthesized targetNTSR1 length7 aa refs4
snapshot sparse 0% confidence
Class
Endogenous neuropeptide fragment (canine-derived)
Status
No approved therapeutic status identified
Best-supported effect
Structural characterization and reported pharmacological activity in isolation study (species: dog); specific findings not individually extracted in this card
Main caveat
Evidence content is limited to a single vendor catalog entry and one 1991 isolation paper; no assay, animal experiment, or human data are individually extracted in this card
status 4 / 5
prediction metrics boltz-2 1.0
ipTM0.919
pTM0.806
avg pLDDT75.5
ranking score0.788
STRUCTURE · PEP-10539 × NTSR1
ranking0.788
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 1.0 · mmCIF ↓ download
sequence7 aa
157
FLFRPRN
overview readme

What this is

Neuromedin U-8 (NMU-8) is the biologically active C-terminal fragment of neuromedin U, a neuropeptide first isolated and characterized in mammalian gut and brain tissue. Neuromedin U was named for its potent uterine-contracting activity in early pharmacological assays; the "-8" designation refers to the processed short form, whose seven-residue sequence (FLFRPRN) corresponds to the conserved C-terminal segment shared across human, rat, mouse, dog, and chicken neuromedin U isoforms (Minamino, Kangawa, Matsuo 1985, as referenced in the EMBO J structural atlas). The full-length precursor pro-NMU is cleaved by prohormone convertases at defined processing sites to yield the mature bioactive peptide; the fourth processing site generates the C-terminal amide (–NH₂) that caps the native peptide — that amide is absent from the stored seven-letter sequence FLFRPRN but is present on the biologically characterized form.

History

Neuromedin U was first described in the 1980s from porcine spinal cord, and the canine form was later isolated, structurally characterised, and its pharmacological activity assessed by O'Harte and colleagues (Peptides, 1991). The precursor processing pathway was systematically mapped by Kitabgi (Journal of Molecular Medicine, 2006), who showed that prohormone convertases differentially cleave pro-neurotensin/neuromedin N — a related pro-peptide — in tissue- and cell-line-specific patterns, illuminating how the mature short forms are generated from their precursors. The structural basis of receptor engagement in this peptide family was substantially advanced by White and colleagues (Nature, 2012), who resolved the structure of an agonist-bound neurotensin receptor, and subsequently by Deluigi and colleagues (Science Advances, 2021), whose crystal structures of NTSR1 bound to small-molecule full agonists, partial agonists, and inverse agonists revealed the structural determinants of graded receptor activation.

What it does

NMU-8 carries the conserved C-terminal sequence (Phe-Leu-Phe-Arg-Pro-Arg-Asn) that is shared across mammalian and avian neuromedin U isoforms and that is considered the pharmacophoric core responsible for biological activity. Across species, NMU sequences all terminate in this FLFRPRN motif, suggesting strong evolutionary conservation of the C-terminal region (EMBO J structural atlas, doi:10.1038/sj.emboj.7600526). The pharmacological activity of the canine neuromedin U form — encompassing the same conserved C-terminal — was characterised by O'Harte and colleagues (1991).

Evidence

  • Human: No human clinical trials are reported in the dossier for the isolated NMU-8 fragment.
  • Animal: Pharmacological activity of the dog neuromedin U peptide, which shares the FLFRPRN C-terminal sequence, was characterised in early work by O'Harte and colleagues (Peptides, 1991).
  • In vitro: Crystal structures of the neurotensin receptor 1 (NTSR1), the card's assigned target, with agonist and non-agonist ligands were resolved by White and colleagues (Nature, 2012) and Deluigi and colleagues (Science Advances, 2021), providing structural context for ligand engagement at this receptor class.

Mechanism

NMU-8 is a seven-residue peptide (FLFRPRN) corresponding to the conserved C-terminal segment of full-length neuromedin U. The native bioactive form carries a C-terminal amide cap (–NH₂) generated when prohormone convertases cleave the precursor at the fourth processing site, with glycine serving as the amide donor; this modification is not encoded in the stored raw sequence. The FLFRPRN core is invariant across human, rat, mouse, dog, and chicken NMU sequences, consistent with it constituting the minimal receptor-engagement motif (EMBO J structural atlas). The card's assigned target is NTSR1 (neurotensin receptor type 1), a class A GPCR whose agonist-bound structure and ligand-recognition determinants have been characterised crystallographically (White et al., Nature, 2012; Deluigi et al., Science Advances, 2021).

Open questions

  • The structural basis of NMU-8 binding to its receptor(s) has not been resolved at atomic resolution.
  • Activity of the isolated seven-residue fragment (vs. the longer NMU forms) in human cell systems has not been reported in the available literature.
  • The contribution of the C-terminal amide cap to receptor selectivity and potency of NMU-8 has not been systematically quantified in published sources available in the dossier.
Hypotheses3 directions▾ collapse

Research directions for this peptide, selected from the current sources — hypotheses you can explore and model. None of it is proven yet; tap any one to see the full thinking.

openupdated 2026-06-11

Could this short fragment suppress appetite as well as the full neuromedin U hormone but with less stress and anxiety as side effects?

If true, NMU-8 or a stabilized version could become a starting point for obesity drugs that curb hunger without triggering the anxiety and stress responses that have held back full-length neuromedin U from clinical use.

The hypothesis
NMU-8 has therapeutic potential as a short-acting anorectic agent for obesity because its seven-residue length confers faster renal clearance than full-length NMU-25, reducing sustained hypothalamic activation that causes anxiety-like side effects while preserving acute appetite-suppressive signaling.
Why it’s plausible
Full-length neuromedin U (NMU-25) causes robust anorexia but also elevates stress hormones via prolonged NMUR2 activation in CRH neurons. NMU-8 retains the C-terminal pharmacophore responsible for receptor activation but lacks the N-terminal extension. Shorter peptides are cleared faster, meaning NMUR2 activation would be transient. Transient activation may achieve appetite suppression (fast onset) without sustained CRH/ACTH stress axis engagement.
Why it matters
If NMU-8 captures the appetite-suppressive benefit with reduced stress-axis activation, it would address the key safety liability of NMU-based obesity drugs, a therapeutic space with no approved peptide drug despite decades of interest.
Plausibility.50
Novelty.55
Impact.70
Basis · grounding1 paper · 2 computed/notes
[1]
noteNMU-8 is the biologically active C-terminal fragment conserved across mammalian species, suggesting it represents the minimal active pharmacophore of the full neuropeptide
[2]
paper
Kitabgi 2006 identifies tissue-specific processing generating short vs long forms, implying the organism itself uses fragment length to tune signal duration
doi: 10.1007/s00109-006-0044-6
[3]
sequenceFLFRPRN is only 7 residues; smaller peptides have shorter plasma half-lives, supporting hypothesis of reduced sustained receptor activation
openupdated 2026-06-11

Could this short gut peptide also bind the neurotensin receptor in addition to its own receptors?

If it does, NMU-8 could act through an extra pathway not yet mapped, which might help explain uneven responses to neuromedin U in animal studies and point to new drug targets. This is an untested prediction from a structure model, not a confirmed interaction.

The hypothesis
NMU-8 (FLFRPRN) binds NTSR1 with measurable affinity, not just its canonical receptors NMUR1/NMUR2, because the conserved C-terminal Arg-Pro-Asn motif partially mimics the pharmacophoric Arg-Ile-Leu motif of neurotensin that anchors into the NTSR1 orthosteric pocket.
Why it’s plausible
The boltz-2 complex ipTM of 0.919 against NTSR1 is unusually high for an off-target prediction, suggesting a geometrically compatible interface. NTSR1 and NMUR share structural family features in TM5-ECL2-TM7 that accommodate C-terminally amidated neuropeptides. The Pro-Arg-Asn C-terminus of NMU-8 could engage the same F331(6.58) van der Waals contact identified for neurotensin fragments in the structural atlas.
Why it matters
If NMU-8 is a dual NMUR/NTSR1 ligand, its energy-balance and appetite effects would operate through an unexpected second receptor axis, changing the pharmacological model for NMU-based therapeutics targeting obesity and food intake.
Plausibility.45
Novelty.70
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
structureboltz-2 complex ipTM=0.9191 against NTSR1, indicating high-confidence predicted binding pose
[2]
paper
F331(6.58) van der Waals contact identified as a conserved anchor in the NTSR1 ligand pocket, consistent with C-terminal peptide engagement
doi: 10.1126/sciadv.abe5504
[3]
sequenceFLFRPRN C-terminal Arg-Pro-Asn shares basic and polar residues with neurotensin's C-terminal pharmacophore Arg-Ile-Leu
openupdated 2026-06-11

Does this small peptide preferentially activate one of its two receptor subtypes, and does the missing chemical cap change that preference?

Knowing which subtype NMU-8 prefers could help design selective drugs that, for example, curb appetite without gut side effects. The specific binding-pocket explanation here is a proposed idea that would need experimental testing.

The hypothesis
NMU-8 shows greater selectivity for NMUR2 over NMUR1 in gut tissue because the Phe-Leu N-terminal di-residue of FLFRPRN engages an extended hydrophobic sub-pocket present in NMUR2 but not NMUR1, and this selectivity is abolished when the peptide is tested without its C-terminal amide.
Why it’s plausible
NMUR1 is peripherally expressed in gut/kidney while NMUR2 is predominantly central. The conserved C-terminal segment (FLFRPRN) drives high-potency agonism, but selectivity between the two receptor subtypes is less studied for the short form. The N-terminal FL di-residue is a distinguishing feature relative to shorter active fragments; NMUR2 is known to accommodate the full C-terminal octapeptide more tightly based on competitive binding data in the literature.
Why it matters
Subtype selectivity determines whether NMU-8 analogs would act peripherally (appetite suppression, gut motility via NMUR1) or centrally (energy expenditure, stress via NMUR2), which defines the therapeutic window and CNS side-effect risk.
Plausibility.40
Novelty.55
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceFLFRPRN N-terminal FL residues provide hydrophobic bulk absent in shorter NMU fragments; selectivity implications depend on subpocket geometry of NMUR1 vs NMUR2
[2]
paper
Kitabgi 2006 maps tissue-specific prohormone convertase cleavage yielding different peptide products in peripheral vs central tissue, implying biological context matters for which receptor subtype is engaged
doi: 10.1007/s00109-006-0044-6
[3]
noteC-terminal amide absent from stored sequence; amidation known to influence receptor subtype selectivity in neuropeptide families
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.9191594123840332 boltz-2
ranking score 0.7879095673561096 boltz-2
structural qualityopenfold3
metricvaluenote
gpde1.067global PDE — lower = better
disorderNaNfraction disordered
3-letter notation
Phe-Leu-Phe-Arg-Pro-Arg-Asn
recipeboltz-2 1.0
parametervalue
modelboltz-2 1.0
weights
hardwarenvidia_nim_api
mlx version
python
random seed
msa strategynone
diffusion samples1
runtime
predicted bymlx@peptide
predicted at2026-04-24
citationbibtex
peptidemodel (2026). Neuromedin U-8: gut-brain peptide fragment (NMU-8) (pep-10539, v1). PeptideModel. https://peptidemodel.com/card/pep-10539
@peptide{pep10539,
  sequence = {FLFRPRN},
  target   = {ntsr1},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 3 by signal overlap
clinical trials 0 trials · checked 2026-05-09
0
no registered clinical trials as of 2026-05-09; we'll re-check periodically
references 4 papers
discussion no comments
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