pe
pep-10704 v1 CC-BY-SA-4.0

Dynorphin A: natural opioid pain and stress signal (porcine form)

A natural opioid peptide the body makes from a larger precursor; activates opioid receptors to modulate pain and stress responses. Used as a lab research tool.

statussynthesized targetOPRM1 length17 aa refs13
status 4 / 5
prediction metrics boltz-2 1.0
ipTM0.702
pTM0.794
avg pLDDT78.0
ranking score0.765
STRUCTURE · PEP-10704 × OPRM1
ranking0.765
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 1.0 · mmCIF ↓ download
sequence17 aa
15101517
YGGFLRRIRPKLKWDNQ
overview readme

What this is

Dynorphin A (1-17) is a 17-amino-acid opioid peptide that the body makes naturally — it is the cleavage product of a larger precursor protein called prodynorphin (specifically residues 209–225 of the porcine prodynorphin sequence). It was first isolated from pig pituitary glands and identified as an extraordinarily potent opioid (Goldstein 1981). The stored sequence here, YGGFLRRIRPKLKWDNQ, is the porcine form; the first five residues (YGGFL) are the same Leu-enkephalin "opioid motif" found at the start of many endogenous opioid peptides, and the C-terminal extension is what distinguishes dynorphin from the shorter enkephalins.

History

Dynorphin was named for its dynamic potency in opioid bioassays. Goldstein and colleagues determined the complete primary structure of the heptadecapeptide from porcine pituitary in 1981, reporting it as Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln and showing that the synthetic peptide of this sequence behaved identically to the natural material in the guinea pig ileum myenteric plexus–longitudinal muscle bioassay (Goldstein 1981). The same paper established that the first 13 residues account for the potency, a finding that has shaped subsequent structure–activity work on dynorphin fragments.

What it does

Dynorphin A (1-17) acts on the opioid receptor family — a set of G-protein-coupled receptors that endogenous opioid peptides use to dampen pain signaling, modulate reward and motivation, and regulate functions such as gastrointestinal motility (Sobczak 2014). Dynorphins are best known as endogenous ligands of the kappa-opioid receptor system, and the pharmacology of kappa-opioid receptor–related ligands has been studied extensively in non-human primates (Ko 2020). On this platform the card's annotated target is the mu-opioid receptor (oprm1), reflecting that dynorphin A also interacts with the broader mu-opioid receptor family whose biology has been reviewed in depth (Pasternak 2013).

Mechanism

Dynorphin A (1-17) belongs to the prodynorphin-derived family of endogenous opioid peptides, alongside dynorphin B and the related "big dynorphin" — all of which share the N-terminal YGGFL "message" sequence with the enkephalins and differ in their C-terminal "address" extensions (Clynen 2014). The Tyr-Gly-Gly-Phe motif is required for opioid receptor engagement; the basic residues that follow (Arg-Arg, Arg, Lys, Lys) form a positively charged C-terminal "address" that biases the peptide toward the kappa-opioid receptor relative to the shorter enkephalins. Goldstein (1981) showed that truncating dynorphin to its first 13 residues preserves potency in the guinea pig ileum assay, indicating that the terminal Trp-Asp-Asn-Gln tail is not essential for the bioassay activity measured there.

The mu-opioid receptor (MOR) — the target annotated on this card — and the closely related nociceptin/orphanin FQ receptor show divergent, cell-type-specific signaling within the mesocorticolimbic reward circuitry, with MOR activation enhancing reward processing and reinforcement by facilitating dopamine transmission in the ventral tegmental area and nucleus accumbens (Allichon 2026).

Evidence

  • Human: No registered clinical trials for dynorphin A (1-17) on ClinicalTrials.gov; the peptide is studied as an endogenous neuromodulator and pharmacological tool rather than as a clinical drug candidate.
  • Animal: Characterized in vivo in the guinea pig ileum bioassay at the time of structure elucidation (Goldstein 1981); kappa-opioid receptor pharmacology of related ligands extensively studied in non-human primates (Ko 2020).
  • In vitro: Engagement of opioid receptors in tissue preparations is documented; comparative opioid binding methodology in rat brain has been established for related opioid peptides such as dermorphin (Amiche 1990).

Known effects

  • Endogenous opioid signaling — Established. Acts on the opioid receptor family that mediates analgesia, reward modulation, and autonomic regulation (Pasternak 2013; Ko 2020).
  • Gastrointestinal motility modulation — Mechanistic and tissue-level evidence. Opioid receptors and their endogenous ligands modulate motility, secretion, and visceral sensation in the GI tract (Sobczak 2014).
  • Neuropeptide target for anticonvulsant research — Mechanistic. Dynorphin-A is listed among the prodynorphin-derived neuropeptides reviewed as targets for anticonvulsant drug development (Clynen 2014).
  • Mesocorticolimbic reward signaling (via mu-opioid receptor) — Mechanistic. MOR and NOPR exhibit cell-type-specific actions in the prefrontal cortex, ventral tegmental area, and nucleus accumbens (Allichon 2026).

Regulatory status

  • US (FDA): Not an approved drug. Dynorphin A (1-17) is studied as an endogenous peptide and research tool.
  • EU (EMA): Not an approved drug.
  • WADA: Not separately listed; endogenous opioid peptide.

Related peptides

  • Dermorphin — amphibian-skin opioid heptapeptide with a D-Ala residue; used as a selective mu-opioid receptor probe (Amiche 1990).

Other prodynorphin-derived peptides (dynorphin B, big dynorphin, α-neoendorphin) and the enkephalins share the N-terminal YGGF "opioid motif" and represent the broader endogenous opioid system around this card (Clynen 2014).

Hypotheses2 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 2026-06-05

Does the rigid proline at position 10 act like a switch that separates two functional regions of dynorphin, letting the peptide choose between different pain receptors?

Understanding this hinge could let chemists design short dynorphin-inspired peptides that precisely target one receptor subtype over another, opening a path to more targeted painkillers or anti-addiction medicines with fewer side effects.

The hypothesis
The Pro10 residue in dynorphin A (1-17) acts as a structural hinge that decouples the N-terminal opioid message (YGGFL) from the basic C-terminal address region, allowing each region to adopt independent conformations upon receptor binding, such that substitution of Pro10 with a flexible Gly or a rigid Aze would measurably shift receptor subtype selectivity.
Why it’s plausible
Proline introduces a rigid, cyclic constraint that disrupts alpha-helical and extended-strand continuity. In YGGFLRRIRPKLKWDNQ, Pro10 sits between the Arg-rich cluster (R6-R9) and the Lys-rich segment (K11-K13), potentially acting as a pivot. The C-terminal portion of the molecule (K11-Q17) is retained in pep-10704 but absent from pep-10700 (YGGFLRRIRP), and that 10-residue form shows notably higher ipTM (0.88) at OPRM1, consistent with Pro10 terminating the MOR-favoring conformation.
Why it matters
A proline-hinge model for dynorphin selectivity is not established in structural terms and would provide a generalizable design principle for engineering selectivity switches into other bifunctional opioid peptides.
Plausibility.55
Novelty.70
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
sequencePro10 is at position 10 in YGGFLRRIRPKLKWDNQ; the 1-10 fragment YGGFLRRIRP ends exactly at this Pro, and its OPRM1 ipTM (0.88) is substantially higher than the full 17-mer (0.70), consistent with Pro10 marking a domain boundary.
[2]
structureBoltz-2 pLDDT=78.0 for full 17-mer vs 81.4 for the 1-10 fragment, suggesting the additional C-terminal residues add structural ambiguity when docked at MOR.
[3]
paper
Goldstein 1981 noted residues 1-13 carry potency; Pro10 lies within this active core, implicating it in the conformational organization of the binding-competent segment.
doi: 10.1073/pnas.78.11.7219
openupdated 2026-06-05

Could dynorphin A, already known as a pain signal, also directly kill bacteria through its positively charged amino acids?

If dynorphin A has antimicrobial properties, it could inspire peptide drugs that simultaneously reduce pain and fight infection at wound sites or in the gut, addressing two problems with one molecule and potentially reducing the need for separate antibiotic treatments.

The hypothesis
The cationic basic cluster of dynorphin A (1-17) (R6-R7-I8-R9-P10-K11-L12-K13) confers membrane-active properties sufficient to disrupt bacterial membranes at concentrations below those causing opioid receptor saturation, making the peptide a dual-function analgesic/antimicrobial agent relevant to infected wound or gut contexts where both activities could be simultaneously beneficial.
Why it’s plausible
Cationic amphipathic peptides with clusters of Arg and Lys residues are a hallmark of antimicrobial peptides. Dynorphin A (1-17) has five cationic residues concentrated between positions 6-13, a net positive charge sufficient for membrane interaction. Endogenous opioids including beta-defensins and some neuropeptides show antimicrobial activity; dynorphin's cationic region is structurally analogous to the membrane-binding domains of known antimicrobial peptides. Gut opioid peptides already modulate intestinal barrier function (Sobczak 2014), placing dynorphin in a context where antimicrobial activity would be biologically relevant.
Why it matters
If dynorphin A (1-17) has antimicrobial activity via its basic C-terminal domain, the peptide exemplifies a class of neuro-immune-antimicrobial mediators, and minimized analogs preserving the cationic cluster could be developed as non-antibiotic peptide therapeutics for infected wounds or gut dysbiosis.
Plausibility.40
Novelty.60
Impact.45
Basis · grounding2 computed/notes
[1]
sequenceYGGFLRRIRPKLKWDNQ contains R6, R7, R9, K11, K13 yielding net charge approximately +5 at physiological pH, above the +4 threshold commonly associated with membrane-disruptive activity in AMPs.
[2]
sourceSobczak 2014 reviews dynorphin family effects on gastrointestinal function, a site where antimicrobial and opioid activities could converge at the mucosal barrier.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.7024305462837219 boltz-2
ranking score 0.7648069262504578 boltz-2
structural qualityopenfold3
metricvaluenote
gpde1.100global PDE — lower = better
disorderNaNfraction disordered
3-letter notation
Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln
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). Dynorphin A: natural opioid pain and stress signal (porcine form) (pep-10704, v1). PeptideModel. https://peptidemodel.com/card/pep-10704
@peptide{pep10704,
  sequence = {YGGFLRRIRPKLKWDNQ},
  target   = {oprm1},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 0 trials · checked 2026-05-22
0
no registered clinical trials as of 2026-05-22; we'll re-check periodically
references 13 papers
[1] evidence
[4] supporting
[6] supporting
[7]
Anti-angiogenic peptides identified in thrombospondin type I domains
Karagiannis, E. et al. Biochemical and Biophysical Research Communications 2007
supporting
[9] supporting
[13] supporting
discussion no comments
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