pe
pep-04472 v1 CC-BY-SA-4.0

Neurokinin A: natural nerve-signalling peptide

A naturally made messenger released by nerves that helps control muscle contraction, inflammation, and pain; not a drug, used mainly as a lab research tool.

statusbioassayed targetTACR2 length10 aa refs4
endogenous
status 2 / 5 · 0 verified on platform
prediction metrics boltz-2 1.0
ipTM0.927
pTM0.809
avg pLDDT72.4
ranking score0.765
STRUCTURE · PEP-04472 × TACR2
ranking0.765
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 1.0 · mmCIF ↓ download
sequence10 aa
1510
HKTDSFVGLM
in the news 1 article
overview readme

What this is

Neurokinin A (NKA) is a short, naturally occurring signalling peptide made in the human body — one of three "tachykinin" messengers that nerves use to talk to muscle, immune, and other tissues. It is co-produced with Substance P from the same gene (TAC1), released together with Substance P from the same nerve terminals, but acts on a different preferred receptor (NK2 rather than NK1). In its mature, active form NKA carries a C-terminal amide (HKTDSFVGLM-NH₂) that is required for binding to the tachykinin receptors and is not represented in the bare 10-letter sequence stored here (Steinhoff 2014). NKA and its relatives are widely studied because the tachykinin system is present throughout the nervous, immune, gastrointestinal, respiratory, and urogenital systems and contributes to pain signalling, inflammation, smooth-muscle contraction, and neurogenic disease (Steinhoff 2014).

History

Tachykinins are one of the most intensively studied neuropeptide families. The modern picture identifies Substance P, NKA, and Neurokinin B as the three primary mammalian members, traces NKA and Substance P to the preprotachykinin A gene (TAC1) and Neurokinin B to a separate gene (TAC3), and assigns each peptide a preferred receptor among the three neurokinin GPCRs NK1, NK2, and NK3 (Steinhoff 2014). Comparative work has shown that the family's C-terminal pharmacophore (Phe-X-Gly-Leu-Met-NH₂) is conserved across vertebrates and invertebrates: a midgut tachykinin from the desert locust Schistocerca gregaria was characterised by mass spectrometry (Veelaert 1999), and an integrated neuropeptidomic study of the tree shrew (Tupaia belangeri) catalogued NKA together with the longer NKA-containing fragments produced from the same precursor (Petruzziello 2012). Beyond its endogenous biology, NKA is of interest because the tachykinin system overlaps with disease pathways — including epilepsy and chronic inflammation — surveyed in reviews of neuropeptides as targets for anticonvulsant drug development (Clynen 2014).

What it does

Inside the body, NKA acts as a fast neuromodulator: it is released from nerve terminals alongside Substance P and triggers responses in nearby cells through tachykinin G-protein-coupled receptors. NKA's preferred receptor is the NK2 receptor (TACR2), which is enriched on smooth muscle and contributes to gut motility, airway tone, and bladder contractility, while Substance P is the preferred ligand at NK1 and Neurokinin B at NK3 (Steinhoff 2014). Because the same tachykinin signalling axis shows up in pain processing, neurogenic inflammation, and seizure circuits, NKA and the broader tachykinin system have been examined as therapeutic targets in respiratory disease, GI disorders, and CNS conditions including epilepsy (Steinhoff 2014; Clynen 2014).

Mechanism

NKA is one of several peptides cleaved from the preprotachykinin A precursor encoded by the TAC1 gene; alternative splicing and post-translational processing of that precursor also yield Substance P and the N-terminally extended forms neuropeptide K (NPK) and neuropeptide γ (NPγ), each of which contains the NKA decapeptide at its C-terminus (Steinhoff 2014; Petruzziello 2012). The mature peptide is C-terminally amidated; this amide, together with the conserved Phe-X-Gly-Leu-Met motif, is the structural feature recognised by the tachykinin receptors. NKA binds all three neurokinin receptors (NK1, NK2, NK3) but with a clear preference for NK2/TACR2 over NK1, which is the structural basis for its distinct physiological profile compared with Substance P (Steinhoff 2014). The conservation of the C-terminal pharmacophore across vertebrate and invertebrate tachykinins — visible in locust Schistocerca gregaria tachykinin (Veelaert 1999) and in non-mammalian vertebrate forms — underlines that the FXGLM-NH₂ end is the receptor-engaging element.

Evidence

  • Human: No human clinical trials of Neurokinin A itself are represented in this dossier. Its role in human physiology and disease is established through endogenous-peptide biology and tissue-distribution studies summarised in the tachykinin literature (Steinhoff 2014).
  • Animal: Tachykinins including NKA have been studied across mammalian and non-mammalian models, with neuropeptidomic surveys cataloguing NKA and its extended forms in tree shrew brain (Petruzziello 2012) and demonstrating the conservation of the tachykinin family into invertebrates (Veelaert 1999).
  • In vitro / reviews: The comprehensive Physiological Reviews synthesis of tachykinins and their receptors covers signalling, trafficking, and disease relevance across the nervous, immune, GI, respiratory, and urogenital systems (Steinhoff 2014); the role of NKA and other neuropeptides as anticonvulsant-drug targets is reviewed in the epilepsy context (Clynen 2014).

Known effects

  • Smooth-muscle contraction (gut, airway, bladder) — Mechanistically established via NK2/TACR2 across multiple organ systems (Steinhoff 2014).
  • Neurogenic inflammation and pain signalling — Part of the broader tachykinin axis with Substance P (Steinhoff 2014).
  • Modulation of seizure-circuit excitability — Proposed target area for anticonvulsant drug development; preclinical and mechanistic (Clynen 2014).

Regulatory status

Neurokinin A is an endogenous human peptide, not a marketed drug. There is no FDA or EMA approval, and no WADA listing, for NKA itself. (Tachykinin-system drugs that have reached the clinic typically act as receptor antagonists — e.g. NK1 antagonists used as antiemetics — rather than as NKA itself; those are separate compounds and outside the scope of this card.)

Related peptides

  • Substance P — the most-studied tachykinin; produced from the same TAC1 precursor as NKA and preferring the NK1 receptor (Steinhoff 2014).
  • Neurokinin B — third primary mammalian tachykinin, encoded by TAC3, preferring the NK3 receptor (Steinhoff 2014).
  • Neuropeptide K (NPK) and Neuropeptide γ (NPγ) — N-terminally extended forms produced from the same preprotachykinin precursor that contain the NKA decapeptide at their C-terminus (Steinhoff 2014; Petruzziello 2012).
Hypotheses6 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

Do NKA and Substance P work together in a multiplying rather than additive way during inflammation?

If these two peptides amplify each other, blocking only one might be nearly useless, suggesting that asthma or chronic pain drugs need to hit both targets at once to work.

The hypothesis
Co-release of NKA and Substance P from the same nerve terminal produces a synergistic inflammatory response at sites of neurogenic inflammation because NK2 activation prolongs or amplifies the NK1-mediated vasodilation and plasma extravasation initiated by Substance P, rather than acting as a redundant parallel signal.
Why it’s plausible
NKA and SP are co-stored and co-released from TAC1-expressing sensory neurons. Neurogenic inflammation involves both vasodilation (predominantly NK1) and smooth-muscle contraction (predominantly NK2). If NK2 signalling upregulates downstream cAMP or PKC pathways that sensitise NK1-bearing endothelial cells, the two peptides would act synergistically rather than additively, explaining why tachykinin blockade requires dual NK1+NK2 antagonism for full efficacy in inflammatory models.
Why it matters
If NKA acts as a potentiator of Substance P rather than a redundant signal, combination NK1+NK2 blockade would be necessary for effective anti-neuroinflammatory therapy, and NKA levels could serve as a biomarker for refractory neurogenic inflammation.
Plausibility.72
Novelty.60
Impact.75
Basis · grounding1 paper · 1 computed/note
[1]
noteNKA is co-produced and co-released with Substance P from TAC1-expressing nerve terminals; system contributes to pain, inflammation, smooth-muscle contraction, and neurogenic disease
[2]
paper
Tachykinin system literature reference documenting distribution and mechanism of action relevant to co-release biology
doi: 10.1007/s12035-014-8669-x
openupdated 2026-06-11

Does the charged front portion of NKA prevent it from activating the wrong receptor?

If the front of NKA is a natural selectivity filter, mimicking it could help design drugs that target airway inflammation without triggering pain signalling, benefiting asthma and COPD patients.

The hypothesis
The N-terminal HKTD sequence of NKA encodes NK2-over-NK1 selectivity by forming contacts that sterically exclude the wider NK1 binding pocket, not by enhancing NK2 affinity per se.
Why it’s plausible
NKA and Substance P share the same C-terminal pharmacophore but differ at their N-termini (NKA: HKTDSFVG vs SP: RPKPQQFFG), yet NKA prefers NK2 while SP prefers NK1. The selectivity must be encoded in the divergent N-terminal region. His1 and Asp4 in NKA carry charge not present in SP's equivalent positions, which could create repulsive interactions with charged residues in the NK1 extracellular loops while fitting the NK2 pocket.
Why it matters
Understanding the structural basis for NK2 vs NK1 selectivity would allow rational design of selective NK2 agonists or antagonists for conditions like asthma (NK2-driven bronchoconstriction) without the cardiovascular side-effects associated with NK1 activation.
Plausibility.80
Novelty.50
Impact.70
Basis · grounding2 computed/notes
[1]
sequenceNKA sequence HKTDSFVGLM contains His1 and Asp4 giving a charged N-terminus distinct from Substance P (RPKPQQFFGLM-NH2); both share the Phe-Gly-Leu-Met-NH2 C-terminal pharmacophore
[2]
noteNKA preferred receptor is NK2 (TACR2) while co-released Substance P prefers NK1 (TACR1), despite both deriving from TAC1 gene
openupdated 2026-06-11

Could a single chemical swap make NKA resist destruction in inflamed tissue?

Inflamed tissues destroy NKA quickly by oxidizing one atom in its tail. A stabilized version could stay active longer where it is needed most, potentially improving treatments for asthma or bowel inflammation.

The hypothesis
Replacing the Met10 residue of NKA with an oxidation-resistant norleucine or selenomethionine analogue would preserve full NK2 receptor potency while substantially increasing metabolic half-life in inflamed tissue, where reactive oxygen species rapidly oxidize the native methionine sulfur.
Why it’s plausible
Met10 (the C-terminal residue, bearing the amide) is part of the conserved Phe-X-Gly-Leu-Met-NH2 pharmacophore. Methionine is highly susceptible to oxidation to methionine sulfoxide in inflammatory microenvironments, which likely inactivates NKA at the sites where it would be most therapeutically relevant. Norleucine is a bioisostere that maintains the hydrophobic side chain length without an oxidisable sulfur.
Why it matters
An oxidation-stable NKA analogue would remain active in inflamed tissue, potentially enabling long-acting NK2 agonist therapy for respiratory disease or a stable research probe for dissecting tachykinin signalling in inflammatory contexts.
Plausibility.82
Novelty.50
Impact.65
Basis · grounding2 computed/notes
[1]
sequenceNKA terminal sequence is ...FVGLM-NH2 with Met10 as the invariant C-terminal residue of the conserved pharmacophore across all tachykinins
[2]
noteC-terminal amide on Met is required for receptor binding; conserved pharmacophore Phe-X-Gly-Leu-Met-NH2 identified across vertebrates and invertebrates
openupdated 2026-06-11

Does NKA cause normal gut movement at low levels but painful spasms at high levels?

If confirmed, this could explain GI symptoms in Crohn's disease and IBS, and point toward fine-tuned NK2-targeting treatments that restore normal digestion rather than just blocking all gut contractions.

The hypothesis
NKA's NK2 agonism in the gastrointestinal tract is pro-kinetic at low physiological concentrations but becomes pathological at the elevated concentrations seen in inflammatory bowel disease, meaning NKA acts as a concentration-dependent switch between normal motility and dysmotility.
Why it’s plausible
NK2 receptors are densely expressed on GI smooth muscle and regulate normal peristalsis. In inflammatory states, neurogenic up-regulation of NKA release is documented. If the NK2 dose-response curve on GI smooth muscle is non-linear with a steep Hill coefficient, low NKA could drive normal contraction amplitude while excess NKA drives sustained spasm, explaining why both NK2 agonists (pro-kinetic) and antagonists (anti-spasmodic) have been explored therapeutically in GI disease.
Why it matters
If NKA is a concentration-dependent motility switch, titrating NK2 receptor occupancy rather than blocking it entirely could restore normal GI function in IBD or IBS patients while avoiding the constipation seen with complete NK2 blockade.
Plausibility.70
Novelty.60
Impact.65
Basis · grounding2 computed/notes
[1]
noteTachykinin system including NKA is active in GI tract and contributes to smooth-muscle contraction and neurogenic disease
[2]
structureHigh ipTM=0.93 with TACR2 supports stable NKA-NK2 interaction relevant to GI pharmacology
openupdated 2026-06-11

Could NKA released by airway nerves push the immune system into allergy mode?

If NKA steers the immune system toward allergy during early exposures, blocking it at that stage could prevent asthma and hay fever from developing in the first place, not just treat symptoms after they appear.

The hypothesis
NKA, acting via NK2 receptors expressed on dendritic cells and T-helper cells, could modulate adaptive immune polarization toward Th2 in airways, providing a mechanistic link between sensory nerve activation and the allergic immune phenotype in asthma.
Why it’s plausible
NK2 receptor expression has been documented on immune cells beyond smooth muscle. If dendritic cell NK2 engagement shifts cytokine output toward IL-4/IL-13 production, neurogenic NKA release during early allergen exposure could prime the adaptive immune response toward Th2, making NKA a causal actor in allergy sensitization rather than merely a downstream effector of established allergy. This would be distinct from NKA's known bronchoconstrictive role.
Why it matters
If NKA drives Th2 polarization upstream of the allergic response, NK2 antagonism during initial allergen sensitization could prevent allergy development entirely rather than only treating established symptoms, repositioning NK2 blockers as preventive rather than rescue agents.
Plausibility.55
Novelty.75
Impact.70
Basis · grounding1 paper · 1 computed/note
[1]
noteTachykinin system is active in immune tissues and contributes to inflammation; NKA co-released at sensory nerve terminals in respiratory tissue
[2]
paper
Literature documents tachykinin distribution and mechanism of action in immune and neural contexts
doi: 10.1007/s12035-014-8669-x
openupdated 2026-06-11

Does the front half of NKA matter at all for gripping the NK2 receptor?

If only the last few amino acids of NKA do the work, drug designers could build much shorter, cheaper molecules that mimic this peptide to treat asthma or irritable bowel syndrome.

The hypothesis
The high ipTM (0.93) predicted for NKA binding TACR2 reflects primarily C-terminal contacts, meaning the bare sequence HKTDSFVGLM without its amide cap structurally underpredicts binding affinity and the pLDDT=72 disorder at the N-terminus is irrelevant to receptor engagement.
Why it’s plausible
The C-terminal pharmacophore Phe-X-Gly-Leu-Met-NH2 drives tachykinin receptor docking across vertebrates and invertebrates. The N-terminal residues HKTD of NKA are divergent across family members and likely contribute selectivity rather than affinity. A prediction run on the bare, unamidated sequence could still yield high complex confidence if the folding engine correctly places the C-terminal residues in the binding pocket, making the strong ipTM meaningful.
Why it matters
If binding is genuinely C-terminus-dominant, truncated or N-terminally modified NKA analogs retaining only the pharmacophore tail would preserve full NK2 potency, directly guiding minimal-peptide therapeutic design.
Plausibility.85
Novelty.35
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
structureboltz-2 complex ipTM=0.93 predicts high-confidence NKA-TACR2 interaction despite pLDDT=72.4 indicating partial N-terminal disorder
[2]
noteC-terminal pharmacophore Phe-X-Gly-Leu-Met-NH2 is conserved across vertebrates and invertebrates; C-terminal amide is stated as required for receptor binding
[3]
paper
Invertebrate tachykinin from locust retains the conserved C-terminal motif, supporting evolutionary primacy of the C-terminal pharmacophore
doi: 10.1006/bbrc.1999.1808
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.92710942029953 boltz-2
ranking score 0.7645934820175171 boltz-2
structural qualityopenfold3
metricvaluenote
gpde1.317global PDE — lower = better
disorderNaNfraction disordered
3-letter notation
His-Lys-Thr-Asp-Ser-Phe-Val-Gly-Leu-Met
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). Neurokinin A: natural nerve-signalling peptide (pep-04472, v1). PeptideModel. https://peptidemodel.com/card/pep-04472
@peptide{pep04472,
  sequence = {HKTDSFVGLM},
  target   = {tacr2},
  author   = {peptidemodel},
  year     = {2026},
  status   = {bioassayed}
}
related peptides 1 by signal overlap
clinical trials 259 on ct.gov · 3 on EUCTR · checked 2026-05-22
ct.gov trials 259
with results 30
EUCTR 3
PubMed RCT 20
by phase
2phase 12phase 27no phase
by status
5completed2recruiting3unknown
references 4 papers
discussion no comments
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