pe
pep-10668 v1 CC-BY-SA-4.0

Cortisol-trigger hormone fragment (ACTH [1-31])

A lab-made piece of the pituitary hormone that tells the adrenal glands to make cortisol; used only as a lab research tool to study how that signal works.

statussynthesized targetMC2R length31 aa refs6
snapshot sparse 10% confidence
Class
Endogenous peptide fragment (ACTH N-terminal fragment; POMC-derived)
Status
No approved therapeutic status identified
Main caveat
Catalog source only; no biological activity, clinical, or animal evidence is attached to this card's source file
status 4 / 5
prediction metrics boltz-2 2.2.1
ipTM0.773
pTM0.899
avg pLDDT77.2
ranking score0.772
STRUCTURE · PEP-10668 × MC2R
ranking0.772
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 2.2.1 · mmCIF ↓ download
sequence31 aa
15101520253031
SYSMEHFRWGKPVGKK RRPVKVYPNGAEDEL
overview readme

What this is

ACTH [1-31] is the first 31 amino acids of adrenocorticotropic hormone (ACTH), the pituitary hormone that tells the adrenal glands to produce cortisol. This card covers the synthetic fragment based on the porcine ACTH sequence, which differs from the full-length 39-residue human hormone at its C-terminus. The sequence stored here — SYSMEHFRWGKPVGKKRRPVKVYPNGAEDEL — represents the biologically active core of ACTH that contains both the MC2R-binding determinants and the HFRWG motif shared with alpha-melanocyte-stimulating hormone (α-MSH). Researchers use this fragment to probe MC2R receptor specificity and to dissect which parts of the ACTH sequence drive adrenocortical versus melanocortin signaling.

History

ACTH as a hormone was isolated and sequenced in the 1950s. Its full precursor, proopiomelanocortin (POMC), was later characterized at the gene and mRNA level — Boileau and colleagues (1983) published the complete structure of the porcine POMC mRNA from cloned cDNA, establishing the exact sequence context from which ACTH [1-31] is derived. The porcine sequence has been widely used in biochemical work on ACTH because porcine and human ACTH share nearly identical N-terminal residues through the biologically active region, making porcine-derived fragments useful experimental tools. Interest in defined fragments of ACTH grew alongside the broader melanocortin receptor field: as MC1R, MC2R, MC3R, MC4R, and MC5R were cloned and deorphanized in the early 1990s, the need for precise subtype-selective peptide probes increased, and fragments covering different portions of the ACTH sequence became important research tools for mapping receptor binding requirements (Fridmanis and colleagues, 2017).

What it does

ACTH [1-31] binds the melanocortin 2 receptor (MC2R), the GPCR that is essentially exclusive to the adrenal cortex among the five melanocortin receptor subtypes. When MC2R is activated, adrenocortical cells increase production of cortisol and, to a lesser extent, adrenal androgens. Chida and colleagues (2007) demonstrated in MC2R-knockout mice that MC2R is required for adrenal gland development, steroidogenesis, and neonatal gluconeogenesis — establishing how central this receptor-ligand axis is to normal adrenal function. Beyond MC2R, the N-terminal HFRWG motif within ACTH [1-31] overlaps with the core binding sequence of α-MSH and can interact with other melanocortin receptors (MC1R, MC3R, MC5R), though these interactions are generally weaker than the dedicated high-affinity MC2R engagement (Fridmanis and colleagues, 2017). The broader POMC-derived peptide system and its physiological roles — spanning energy balance, stress response, pigmentation, and immune modulation — are reviewed in depth by Harno and colleagues (2018).

Evidence

  • Human: No clinical trials for ACTH [1-31] specifically as an isolated fragment. The clinical evidence base belongs to the full 39-residue hormone and the synthetic 1-24 fragment (cosyntropin); ACTH [1-31] is used as a research tool rather than a clinical agent.
  • Animal: MC2R knockout studies (Chida and colleagues, 2007) established the essential role of the ACTH–MC2R axis in adrenal development and steroidogenesis in mice. ACTH physiology across the 1-39 sequence has been characterized in extensive animal work; the 1-31 fragment's specific preclinical profile is largely documented in receptor binding and signaling studies.
  • In vitro: ACTH [1-31] and related fragments have been used in cell-based assays to characterize MC2R binding and cAMP signaling. The intracellular signaling mechanisms downstream of melanocortin receptor activation — including Gαs/cAMP/PKA cascades — are reviewed by Rodrigues and colleagues (2015).

Mechanism

MC2R is a class A GPCR coupled to Gαs. When ACTH [1-31] engages MC2R on adrenocortical cells, it stimulates adenylyl cyclase, raising intracellular cAMP and activating protein kinase A. This cascade phosphorylates the steroidogenic acute regulatory protein (StAR), which shuttles cholesterol across the inner mitochondrial membrane — the rate-limiting step of steroidogenesis leading to cortisol synthesis. Fridmanis and colleagues (2017) reviewed the molecular determinants of MC2R specificity in detail, noting that unlike MC1R through MC5R, MC2R does not respond to the short His-Phe-Arg-Trp (HFRW) core motif alone and requires additional residues from the ACTH sequence for full activation, which is why α-MSH and other short melanocortin peptides cannot activate MC2R. The melanocortin receptor system's potential as a target in multiple degenerative and inflammatory diseases — mediated through MC1R and MC3R rather than MC2R — is surveyed by Cai and colleagues (2016). The POMC precursor and the broader logic of how differential tissue-specific processing generates distinct peptide hormones from the same gene is reviewed in Harno and colleagues (2018).

Known effects

  • Adrenocortical steroidogenesis stimulation — Mechanistic (MC2R activation drives cortisol synthesis; well-established from ACTH biology)
  • MC2R receptor agonism — Mechanistic only (in vitro and animal studies; no clinical data for the 1-31 fragment specifically)

Safety signals

No clinical safety data exist for ACTH [1-31] as a standalone research peptide in humans. The safety profile of therapeutic ACTH preparations relates to the full-length hormone or the cosyntropin (1-24) fragment, not to the 1-31 fragment specifically.

Regulatory status

  • US: ACTH [1-31] as an isolated synthetic fragment has no FDA regulatory status; it is not an approved drug. The related clinical agents — cosyntropin (ACTH 1-24) and repository corticotropin injection (Acthar Gel) — are FDA-approved prescription products.
  • Research use: ACTH [1-31] is available as a research-grade synthetic peptide for laboratory use.
  • WADA: Corticotropins are prohibited under WADA's S9 class; athletes subject to the WADA code should be aware that ACTH-related peptides fall under that prohibition.

Related peptides

  • Alpha-MSH — Shares the N-terminal SYSMEHFRWG core with ACTH [1-31] but carries an N-terminal acetyl cap and C-terminal amide modification; acts at MC1R and MC3R rather than MC2R.
  • ACTH (full-length, 1-39) — The complete 39-residue hormone; cosyntropin (1-24) is the FDA-approved synthetic fragment used diagnostically.
  • Melanocortin peptides (MC3R/MC4R ligands) — Share the HFRWG pharmacophore but differ in receptor subtype selectivity.
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 attaching a PEG polymer at lysine-16 of ACTH(1-31) make it last longer in the body without losing its ability to stimulate the adrenal gland?

If successful, this could produce a fully synthetic, precisely defined drug to replace a controversial animal-derived product that currently costs tens of thousands of dollars per vial. Patients with infantile spasms, kidney disease, or multiple sclerosis who rely on this therapy could benefit from a more consistent, affordable, and ethically sourced treatment.

The hypothesis
Introducing a PEGylation site at Lys16 of ACTH(1-31) will extend plasma half-life while preserving MC2R agonism, because Lys16 is distal to the HFRWG pharmacophore core (residues 6-10) and the predicted MC2R interface does not require an unmodified epsilon-amine at position 16.
Why it’s plausible
PEGylation of lysine residues is a well-validated strategy for extending peptide half-life. ACTH(1-31) contains four Lys residues (positions 11, 15, 16, 21). Of these, position 16 is in the KKRR basic cluster; however, the HFRWG pharmacophore is at positions 6-10 and is the primary MC2R contact. If Lys16 modification preserves receptor binding, a long-acting ACTH(1-31)-PEG could replace the repository corticotropin depot formulation with a defined, synthetic molecule.
Why it matters
A chemically defined long-acting ACTH agonist would replace the heterogeneous porcine pituitary extract in Acthar Gel, providing a reproducible, synthetic therapeutic with predictable pharmacokinetics for infantile spasms, nephrotic syndrome, and multiple sclerosis relapse.
Plausibility.60
Novelty.40
Impact.65
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceACTH(1-31) contains Lys at positions 11, 15, 16, 21; position 16 is in the KKRRPVK cluster, spatially remote from the HFRWG pharmacophore at positions 6-10
[2]
structureipTM=0.773 suggests a defined interface; structure modeling can map which Lys residues are solvent-exposed versus receptor-contacting
[3]
paper
ACTH(1-17) is the minimal MC2R activator; residues beyond 17 including Lys21 are not described as essential for receptor activation, implying Lys21 and nearby residues tolerate modification
doi: 10.3389/fendo.2017.00013
openupdated 2026-06-05

Does swapping proline for alanine at position 24 of ACTH change which stress hormone the adrenal gland makes in response?

If this single swap redirects steroid output, it could lead to a precisely targeted treatment for patients who are deficient specifically in aldosterone, the hormone that regulates salt and blood pressure, without accidentally over-stimulating cortisol and causing the side effects associated with steroid therapy.

The hypothesis
The porcine-specific residue differences within the ACTH(1-31) C-terminal region (near residue 24 where guinea-pig ACTH carries Ala rather than the conserved Pro) generate distinct aldosterone versus cortisol production ratios at adrenocortical MC2R, suggesting that residue 24 identity is a molecular switch between glucocorticoid and mineralocorticoid outputs.
Why it’s plausible
The readme notes that guinea-pig ACTH carries Ala at position 24 in place of Pro, and that this substitution elevates aldosterone production above that seen with human ACTH or cosyntropin. Position 24 (PVK in human/porcine context) is just outside the minimal 1-17 MC2R activation core. A Pro-to-Ala swap at position 24 will alter the backbone conformation of this region, potentially changing how the segment interacts with extracellular loop 2 of MC2R, which is implicated in ligand selectivity across melanocortin receptors.
Why it matters
If residue 24 identity steers aldosterone versus cortisol output, single-amino-acid ACTH analogues bearing Ala24 could selectively stimulate mineralocorticoid production, offering a targeted treatment for primary aldosterone deficiency without over-driving glucocorticoid synthesis.
Plausibility.50
Novelty.60
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
noteGuinea-pig ACTH carries Ala24 instead of Pro24 and produces higher aldosterone stimulation than human ACTH(1-39) or cosyntropin (Smith et al., Journal of Endocrinology 1987, as cited in readme)
[2]
sequenceACTH(1-31) porcine sequence: SYSMEHFRWGKPVGKKRRPVKVYPNGAEDEL; position 24 is Pro (PVKVYPNG spans positions 20-27)
[3]
paper
MC2R KO mice show specific loss of corticosterone and aldosterone synthesis pathways, confirming MC2R is the convergence point for both steroid outputs
doi: 10.1073/pnas.0706953104
openupdated 2026-06-05

Does ACTH(1-31) activate a different internal signaling pathway in adrenal cells than the shorter ACTH(1-17) fragment?

If ACTH(1-31) triggers a separate signaling branch that controls inflammation without releasing a large cortisol surge, it could be developed into an anti-inflammatory drug that avoids many of the serious side effects associated with current cortisol-based treatments, helping patients with autoimmune diseases, multiple sclerosis, or infantile spasms.

The hypothesis
ACTH(1-31) acts as a biased MC2R agonist relative to ACTH(1-17), preferentially activating beta-arrestin recruitment over cAMP production, because residues 18-31 (PVKVYPNGAEDEL) make contacts with extracellular loops of MC2R that stabilize a receptor conformation favoring G-protein-independent signaling.
Why it’s plausible
Biased agonism at GPCRs is frequently determined by ligand contacts with extracellular loops rather than the orthosteric binding pocket. The segment PVKVYPNGAEDEL is present in ACTH(1-31) but absent from the minimal MC2R agonist ACTH(1-17). This extension contains charged (Asp, Glu) and aromatic (Tyr) residues capable of forming polar and pi contacts with the receptor extracellular domain, potentially stabilizing a distinct receptor conformation versus the 1-17 form.
Why it matters
Beta-arrestin-biased MC2R agonism could separate anti-inflammatory ACTH effects (which may be arrestin-mediated) from steroidogenic effects (which are cAMP-mediated), enabling therapeutics that treat inflammatory conditions without the full cortisol surge.
Plausibility.45
Novelty.65
Impact.65
Basis · grounding3 computed/notes
[1]
sequenceResidues 18-31 of porcine ACTH(1-31): PVKVYPNGAEDEL; Tyr25, Asp29, Glu30, Leu31 provide polar and hydrophobic contacts absent from the 1-17 fragment
[2]
structureipTM=0.773 for ACTH(1-31) vs. 0.898 for ACTH(1-17); the intermediate value suggests partial additional contacts from the 18-31 segment that change the receptor engagement geometry without fully matching the tight 1-17 interface
[3]
sourceDifferential cAMP and Erk1/2 phosphorylation between hCG and LH at a related glycoprotein receptor confirms biased signaling is operative in structurally related hormone systems
openupdated 2026-06-05

Is ACTH(1-31) better at docking to and activating the adrenal cortisol receptor than the full 39-amino-acid hormone?

If the shorter form is more potent at the adrenal receptor, it could replace or improve upon current ACTH-based therapies used for adrenal insufficiency and inflammatory conditions, offering cleaner pharmacology with less off-target variability.

The hypothesis
Porcine ACTH(1-31) has higher intrinsic MC2R efficacy than human ACTH(1-39) because the absence of the disordered C-terminal tail (residues 32-39) removes a flexible region that reduces productive receptor engagement, reflected in the higher ipTM of 0.773 for the 1-31 fragment versus 0.592 for full-length ACTH(1-39).
Why it’s plausible
The boltz-2 ipTM rises from 0.592 (1-39) to 0.773 (1-31), suggesting that removing residues 32-39 (AEAFPLEF) substantially improves the predicted binding geometry. These eight residues are hydrophobic and disordered, and may antagonize MC2R docking by occluding the receptor binding cleft or introducing conformational heterogeneity that dilutes productive binding poses.
Why it matters
If ACTH(1-31) is a more efficient MC2R agonist than full-length ACTH on a molar basis, porcine-derived 1-31 fragments could serve as superior diagnostic or therapeutic agents compared to the full 39-residue molecule currently used clinically in Acthar Gel formulations.
Plausibility.45
Novelty.40
Impact.50
Basis · grounding1 paper · 2 computed/notes
[1]
structureipTM=0.773 for ACTH(1-31) vs. ipTM=0.592 for ACTH(1-39); both target MC2R, and the truncation improves the predicted complex quality
[2]
sequenceResidues 32-39 of ACTH(1-39) encode AEAFPLEF, a hydrophobic disordered tail absent in ACTH(1-31)
[3]
paper
MC2R activation determinants map to the ACTH N-terminal region; C-terminal residues are not described as contributing to receptor activation
doi: 10.3389/fendo.2017.00013
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.7730052471160889 boltz-2
ranking score 0.7720047831535339 boltz-2
3-letter notation
Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-Asn-Gly-Ala-Glu-Asp-Glu-Leu
recipeboltz-2 2.2.1
parametervalue
modelboltz-2 2.2.1
weights
hardwarevast_v100_32gb
mlx version
python
random seed1
msa strategycolabfold_local
runtime
predicted by
predicted at2026-05-22
citationbibtex
peptidemodel (2026). Cortisol-trigger hormone fragment (ACTH [1-31]) (pep-10668, v1). PeptideModel. https://peptidemodel.com/card/pep-10668
@peptide{pep10668,
  sequence = {SYSMEHFRWGKPVGKKRRPVKVYPNGAEDEL},
  target   = {mc2r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 155 on ct.gov · 2 on EUCTR · checked 2026-05-09
ct.gov trials 155
with results 50
EUCTR 2
by phase
1phase 13phase 35phase 41no phase
by status
7completed2terminated1unknown
references 6 papers
discussion no comments
sign in to comment
peptidemodel.com CC-BY-SA-4.0 research only · not for human use