pe
pep-10718 v1 CC-BY-SA-4.0

Shark adrenal-signaling peptide (alpha-MSH II from spiny dogfish)

A natural hormone fragment from dogfish shark that targets the adrenal gland's stress-hormone receptor; used only as a lab research tool to study how this receptor evolved across animals.

statussynthesized targetMC2R length12 aa refs10
snapshot sparse 15% confidence
Class
Endogenous neuropeptide (fish-derived MSH variant)
Status
No approved therapeutic status identified
Best-supported effect
Identity established by purification and sequencing from spiny dogfish (Squalus acanthias) pituitary; no functional bioactivity data attached to this card
Main caveat
This card is based on a single 1970 purification and sequencing report; no assay, animal, or human evidence is attached
status 4 / 5
prediction metrics boltz-2 1.0
ipTM0.880
pTM0.932
avg pLDDT86.3
ranking score0.866
STRUCTURE · PEP-10718 × MC2R
ranking0.866
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 1.0 · mmCIF ↓ download
sequence12 aa
151012
YSMEHFRWGKPM
overview readme

What this is

The alpha-Melanocyte Stimulating Hormone II peptide (α-MSH II) from the spiny dogfish (Squalus acanthias) is a naturally occurring 12-amino-acid fragment derived from the pituitary POMC precursor protein of an elasmobranch fish. It belongs to the melanocortin peptide family — a group of hormones that includes ACTH and the various MSH peptides, all cut from the same large precursor. Researchers use this peptide to study the pharmacology of the melanocortin 2 receptor (MC2R), the adrenal-cortex receptor that normally responds only to ACTH, and to explore how receptor selectivity for ACTH evolved across vertebrates.

History

The spiny dogfish pituitary was a productive source for early peptide hormone research because the intermediate lobe of the gland is exceptionally large and yields substantial quantities of melanotropins. In 1970, Lowry and colleagues purified and sequenced a melanocyte-stimulating hormone from dogfish pituitary extracts, reporting a core 11-residue sequence (Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Met) and noting that about one fifth of isolated molecules carried an additional N-terminal tyrosine, giving rise to the 12-residue form now cataloged here as α-MSH II (Lowry et al., 1970). They also found that roughly half the molecules had a free C-terminal carboxyl group while the other half were C-terminally amidated — a difference that distinguishes α-MSH II (free carboxyl, Tyr-extended) from α-MSH I (amidated, shorter). Follow-up structural work by Bennett, Lowry and McMartin (1974) established that the N-terminal 13 residues of dogfish ACTH are identical to dogfish α-MSH, confirming ACTH as its biosynthetic precursor in the pars distalis. Eberle and colleagues (1978) then chemically synthesized both dogfish α-melanotropin I and II and tested a series of analogs, demonstrating that removal of the N-terminal acetyl group strongly reduces melanotropic potency and that substitution at the C-terminus (amide vs. free acid) has comparatively modest effects.

What it does

In a research setting, α-MSH II from dogfish is used as a pharmacological probe at MC2R — the receptor responsible for driving glucocorticoid production in the adrenal cortex. Unlike ACTH, α-MSH peptides naturally lack the tetrabasic "address" sequence (Lys-Lys-Arg-Arg) that mammalian and most bony-vertebrate MC2R orthologs require for full activation; α-MSH II therefore binds the receptor but activates it with dramatically lower potency than the intact ACTH molecule (Fridmanis et al., 2017). Studies on the closely related Pacific spiny dogfish MC2R showed approximately 1000-fold greater sensitivity to ACTH(1-24) compared with α-MSH-sized ligands. This selectivity gap makes the dogfish peptide a useful tool for separating the contributions of the shared HFRW "message" motif from the KKRR "address" motif in receptor activation experiments.

Evidence

  • Human: No human studies. This peptide is a non-human research tool, not a clinical compound.
  • Animal / in vitro: Used in receptor pharmacology experiments to probe MC2R activation. The Squalus acanthias pituitary was the original biological source; receptor assays in transfected cell lines have compared its potency to ACTH and other melanocortin ligands. Eberle and colleagues (1978) reported melanocyte-dispersing bioactay data for synthetic α-MSH I, α-MSH II, and analogs, confirming the structural assignments made by Lowry and colleagues. No registered trials on ClinicalTrials.gov for "alpha-melanocyte stimulating hormone II."

Mechanism

MC2R (the ACTH receptor) is a class A GPCR expressed almost exclusively in the zona fasciculata of the adrenal cortex, where it drives steroidogenesis via Gαs → cAMP → PKA signaling. All five melanocortin receptors share the His-Phe-Arg-Trp (HFRW) core pharmacophore, which is present in ACTH, α-MSH, β-MSH, γ-MSH, and δ-MSH. What makes MC2R unique is that it additionally requires the basic Lys-Lys-Arg-Arg "address" motif found only in ACTH (residues 15–18) for high-potency activation; without it, HFRW-containing peptides like α-MSH II can engage the receptor but fail to activate it efficiently in bony-vertebrate orthologs (Fridmanis et al., 2017). MC2R cannot reach the cell surface without co-expression of the melanocortin receptor accessory protein MRAP1, a single-transmembrane protein that facilitates receptor trafficking from the endoplasmic reticulum and enhances ACTH recognition (Hinkle et al., 2009). Loss-of-function mutations in either MC2R or MRAP cause familial glucocorticoid deficiency (FGD), an inherited inability to produce cortisol in response to ACTH. The raw sequence stored here (YSMEHFRWGKPM) is the free-acid form (α-MSH II); the biologically related α-MSH I has one fewer residue at the N-terminus and a C-terminal amide rather than a free carboxyl group — modifications that are absent from the stored 1-letter sequence but are relevant to potency comparisons (Eberle et al., 1978).

Known effects

  • Melanocyte stimulation (in vitro / frog/lizard bioassay) — melanocyte-dispersing activity confirmed for synthetic dogfish α-MSH I and II; substantially weaker than N-terminally acetylated mammalian α-MSH (Eberle et al., 1978) — Preclinical only
  • MC2R partial activation — dogfish MSH-sized ligands engage elasmobranch MC2R with 100–1000-fold lower potency than ACTH(1-24); useful as a pharmacological control — Mechanistic/in vitro only
  • POMC processing research tool — used to characterize tissue-specific cleavage patterns in pituitary intermediate vs. anterior lobes (Lowry et al., 1970; Bennett et al., 1974; Harno et al., 2018) — Experimental

Regulatory status

  • US / EU: Not a regulated pharmaceutical; no INN. Research reagent only.
  • WADA: Not listed on the WADA prohibited list (peptide hormone fragments without established performance-related effect).

Related peptides

The melanocortin family shares the HFRW pharmacophore and POMC precursor origin. Related cards on this platform include α-MSH and ACTH-derived peptides that act at overlapping receptor sets. For the receptor context, see the MC2R-targeting ACTH family; for broader melanocortin pharmacology including MC4R and energy balance, see the melanocortin receptor system review cards (Ericson et al., 2017; Cai et al., 2016; Prindle et al., 2026).

Hypotheses4 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

Could the body's stress-hormone switch be set to "picky" by a helper protein, not just by the receptor it plugs into?

If this holds, a protein called MRAP1 acts as a selectivity filter, deciding which signals are allowed through, not just a delivery vehicle. That could open a path to drugs that tweak this filter and help people with adrenal insufficiency respond to their own hormones again, instead of relying on hormone replacement.

The hypothesis
MRAP1 co-expression with elasmobranch MC2R reduces, rather than enhances, the relative efficacy of alpha-MSH II compared with ACTH, because MRAP1 selectively stabilizes receptor conformations that are only productively occupied by the KKRR-containing address region.
Why it’s plausible
In mammalian systems MRAP1 is required for MC2R surface trafficking and enhances ACTH recognition. The mechanism by which MRAP1 discriminates ACTH from MSH-sized ligands is not established. If MRAP1 allosterically biases MC2R toward a high-address-requirement conformation, then in its absence (or when replaced by elasmobranch MRAP1) the receptor might be more permissive toward HFRW-only peptides. This would mean the evolutionary loss of MRAP1-mediated gating, not changes in the receptor binding pocket alone, underlies the gradual acquisition of strict KKRR dependence in vertebrate MC2R lineages.
Why it matters
Demonstrating that MRAP1 shifts the address-requirement threshold would recast MRAP1 as a selectivity filter, not merely a trafficking chaperone, with implications for FGD genetics and for designing small-molecule MRAP1 modulators that could sensitize MC2R to endogenous MSH in adrenal insufficiency.
Plausibility.63
Novelty.71
Impact.64
Basis · grounding2 papers · 1 computed/note
[1]
paper
MRAP N- and C-terminal ends both face extracellularly; both MRAP and MRAP2 support cAMP generation by MC2R with small quantitative differences in ACTH efficacy and potency.
doi: 10.1016/j.mce.2008.10.041
[2]
noteMC2R cannot reach the cell surface without MRAP1; MRAP1 enhances ACTH recognition.
[3]
paper
Loss-of-function mutations in MC2R or MRAP cause familial glucocorticoid deficiency; selectivity gap between ACTH and MSH is established in bony-vertebrate MC2R.
doi: 10.3389/fendo.2017.00013
openupdated 2026-06-05

Why do human adrenal receptors demand a very specific hormone signal when shark versions work with a simpler one?

If this structural difference is confirmed, researchers would know the exact molecular feature that makes human cortisol receptors so selective. That knowledge could guide the design of smaller, simpler hormone-like drugs for familial glucocorticoid deficiency, a rare condition where the adrenal gland ignores its normal hormonal trigger.

The hypothesis
The elasmobranch MC2R ortholog accepts HFRW-only ligands such as alpha-MSH II with substantially higher efficacy than any bony-vertebrate MC2R because the elasmobranch receptor lacks a steric gating mechanism that, in teleosts and tetrapods, requires the KKRR address sequence to reposition transmembrane helix 6 for productive G-protein coupling.
Why it’s plausible
Fridmanis et al. (2017) document that dogfish MC2R is 100-1000-fold more sensitive to ACTH than to MSH-sized peptides, but that gap is far smaller than the effective zero-efficacy observed for MSH peptides at human MC2R. This implies a graded, not binary, dependence on the address motif across vertebrate evolution. Cartilaginous fish diverged from bony vertebrates roughly 450 million years ago, and the MC2R ortholog may retain an ancestral conformation where HFRW alone can produce partial helix 6 displacement. This is consistent with the known importance of TM6 in class A GPCR activation and the documented role of extracellular loop 2 in MC2R selectivity.
Why it matters
A structural explanation for graded address-dependence would identify the minimum receptor determinants needed for HFRW-only activation, directly informing the design of minimally-addressed synthetic ACTH analogs useful in familial glucocorticoid deficiency (FGD) therapy where full ACTH-sized peptides are immunogenic.
Plausibility.71
Novelty.58
Impact.61
Basis · grounding2 papers · 1 computed/note
[1]
paper
Molecular determinants of MC2R specificity for ACTH versus MSH-sized ligands; transmembrane domain residues alter Rmax and potency.
doi: 10.3389/fendo.2017.00013
[2]
noteDogfish MC2R approximately 1000-fold more sensitive to ACTH than MSH-sized ligands, indicating partial but non-zero efficacy for alpha-MSH II.
[3]
paper
MRAP N-terminal and transmembrane domains are highly conserved while C-terminal regions diverge; MRAP2 supports MC2R cAMP generation with small quantitative differences.
doi: 10.1016/j.mce.2008.10.041
openupdated 2026-06-05

What if a hormone discovered in sharks is binding most tightly to a skin and immune receptor, not the stress-response receptor scientists assumed?

If MC1R turns out to be the real target, the whole story of why sharks process this hormone would need rewriting: it might be about color or immunity, not cortisol. For drug developers, it would also clarify where this peptide actually works, avoiding wasted effort chasing the wrong receptor.

The hypothesis
The N-terminal Tyr residue of alpha-MSH II (YSMEHFRWGKPM) confers measurably higher binding affinity at MC1R than at MC2R, making MC1R, rather than the annotated MC2R, the receptor at which this peptide achieves its tightest interaction.
Why it’s plausible
MC1R, unlike MC2R, does not require a basic KKRR address sequence for high-affinity engagement; it responds to HFRW-containing peptides with potency comparable to full ACTH. The free N-terminal Tyr in alpha-MSH II, absent from the predominant mammalian alpha-MSH (which is N-acetylated), could act as an additional hydrogen-bond donor that fits the more open MC1R binding pocket better than it fits the more restrictive MC2R orthosteric site. The high ipTM (0.88) from the boltz-2 prediction of the MC2R complex does not rule out an even higher affinity mode at MC1R, since that receptor was not modeled. Literature confirms ACTH and MSH-sized peptides act at MC1R with similar potency (physrev 2017 ref).
Why it matters
If MC1R is the primary binding target, the peptide's reported adrenal pharmacology would reflect low-potency off-target activity, and its true biological role in the elasmobranch could involve pigmentation or immune modulation rather than steroidogenesis, reframing the evolutionary interpretation of shark POMC processing.
Plausibility.75
Novelty.43
Impact.57
Basis · grounding2 papers · 2 computed/notes
[1]
paper
ACTH acts at MC1R in skin with potency similar to alpha-MSH; MSH-sized peptides do not require the KKRR address for MC1R activation.
doi: 10.1152/physrev.00024.2017
[2]
paper
MC1R on human melanocytes stimulates proliferation and melanogenesis in response to melanotropic peptides including alpha-MSH fragments.
doi: 10.1210/endo.137.5.8612494
[3]
structureipTM 0.88 for MC2R complex modeled by boltz-2; no MC1R complex was modeled for comparison.
[4]
noteElasmobranch MC2R shows approximately 1000-fold greater sensitivity to ACTH(1-24) than to MSH-sized ligands, implying weak MC2R engagement.
openupdated 2026-06-05

Could a peptide from shark hormones quiet runaway brain immune cells, independently of the stress-hormone system?

If this pans out, even a raw, unmodified version of this peptide might dial down the kind of chronic brain inflammation linked to conditions like Alzheimer's or Parkinson's. It would also show that a simpler, shorter hormone fragment, without the chemical tweaks usually needed for potency, might still be enough to do useful anti-inflammatory work.

The hypothesis
Alpha-MSH II (YSMEHFRWGKPM) suppresses NF-kB-driven neuroinflammation via MC1R on microglia at concentrations achievable with the free-acid form, and this anti-inflammatory action is independent of steroidogenesis because the peptide lacks MC2R efficacy in CNS cells that do not express functional adrenal machinery.
Why it’s plausible
Alpha-MSH peptides are well-documented anti-inflammatory agents acting through MC1R and MC3R on macrophages and microglia, driving cAMP-mediated suppression of TNF-alpha and IL-6. The HFRW pharmacophore is sufficient for MC1R activation. Alpha-MSH II carries the full HFRW sequence and would be expected to retain this activity. Because MC2R is essentially absent from CNS tissue and requires adrenal-specific MRAP1, any CNS effect of this peptide would be purely HFRW-mediated and thus separable from the glucocorticoid axis. The lack of N-terminal acetylation reduces potency but the peptide still acts as a partial agonist at MC1R per the melanocyte dispersal data of Eberle et al. (1978).
Why it matters
Establishing MC1R-mediated neuroinflammatory activity for the unmodified dogfish sequence would demonstrate that HFRW alone, without acetylation or C-terminal amidation, retains therapeutically relevant anti-inflammatory potency, directly bearing on the minimum pharmacophore requirements for developing CNS-active melanocortin analogs in neurodegeneration.
Plausibility.75
Novelty.25
Impact.40
Basis · grounding2 papers · 1 computed/note
[1]
paper
Melanocortin receptor system as target for multiple degenerative diseases; MC1R-mediated anti-inflammatory signaling documented.
doi: 10.2174/1389203717666160226145330
[2]
noteEberle 1978 confirmed melanocyte-dispersing activity for synthetic alpha-MSH II; HFRW pharmacophore is shared by all five melanocortin receptors.
[3]
paper
MC1R on human melanocytes responds to melanotropic peptides driving proliferation and melanogenesis via cAMP signaling.
doi: 10.1210/endo.137.5.8612494
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8795090913772583 boltz-2
ranking score 0.8664582371711731 boltz-2
structural qualityopenfold3
metricvaluenote
gpde0.451global PDE — lower = better
disorderNaNfraction disordered
3-letter notation
Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-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). Shark adrenal-signaling peptide (alpha-MSH II from spiny dogfish) (pep-10718, v1). PeptideModel. https://peptidemodel.com/card/pep-10718
@peptide{pep10718,
  sequence = {YSMEHFRWGKPM},
  target   = {mc2r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 7 on ct.gov · checked 2026-05-09
ct.gov trials 7
by phase
2phase 11phase 24no phase
by status
5completed2recruiting
references 10 papers
[3] supporting
[4]
Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016
Ericson, M. et al. Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease 2017
supporting
[10] supporting
discussion no comments
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