pe
pep-10651 v1 CC-BY-SA-4.0

Stress-response research peptide (oxidized CRF 1-40)

A lab-only synthetic peptide, based on a pig version of a human stress hormone, that switches on a receptor (CRHR2) linked to calming anxiety and protecting the heart during stress recovery.

statussynthesized targetCRHR2 length40 aa refs1
snapshot sparse 0% confidence
Class
Corticotropin-releasing factor (CRF) variant — porcine hypothalamic peptide
Status
No approved therapeutic status identified. Catalog and database entry context only.
Best-supported effect
Isolated from porcine hypothalami and characterized as having corticotropin-releasing factor activity in a single 1986 purification study (Patthy et al.); no independent assay, animal-model, or clinical evidence is attached to this card.
Main caveat
This card is based on a single catalog/database source with one primary reference. No receptor-binding, efficacy, safety, animal-model, or human evidence is attached.
status 4 / 5
prediction metrics openfold3-mlx 0.3.1
ipTM0.802
pTM0.725
avg pLDDT52.6
ranking score0.872
STRUCTURE · PEP-10651 × CRHR2
ranking0.872
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence40 aa
1510152025303540
SEEPPISLDLTFHLLREVLE MARAEQLAQQAHSNRKLMEN
overview readme

What this is

Corticotropin-releasing factor [1–40; M38-oxidized, N40] is a 40-residue synthetic analog of porcine corticotropin-releasing factor (CRF), differing from the native sequence at position 38 where methionine has been chemically oxidized to methionine sulfoxide. The peptide was originally characterized as one of several CRF-related polypeptides isolated from porcine hypothalami by Patthy and colleagues (Patthy et al., PNAS 1986); the synthetic oxidized form is used as a research tool for probing CRF receptor pharmacology, with particular selectivity for the type-2 CRF receptor (CRHR2). The oxidized methionine at position 38 is not visible in the stored 40-letter sequence — it is a post-synthetic chemical modification that materially affects receptor subtype selectivity.

History

The sequence of porcine CRF [1–40] was established through biochemical isolation work: Patthy and colleagues (PNAS 1986) purified a series of CRF-active polypeptides from porcine hypothalami using gel filtration and reversed-phase HPLC, and confirmed their structures by sequence analysis. The isolated peptides were characterized by their ability to stimulate corticotropin (ACTH) release from superfused rat pituitary cells. The oxidized M38 variant documented here — bearing methionine sulfoxide at residue 38 and asparagine at the C-terminal position 40 — emerged from this characterization work as a structurally defined form suitable for receptor binding studies.

What it does

In biological systems, CRF [1–40] analogs act on the HPA (hypothalamic–pituitary–adrenal) axis by stimulating ACTH release from the anterior pituitary, which in turn drives cortisol production by the adrenal cortex. The [1–40; M38-oxidized, N40] variant is primarily a laboratory research reagent rather than a therapeutic agent: its value lies in its defined receptor subtype profile. By binding CRHR2 — a class B G protein-coupled receptor expressed in peripheral tissues including the heart, skeletal muscle, and gastrointestinal tract — this analog is used to investigate CRHR2-mediated roles in stress recovery, anxiolysis, and cardioprotective signaling, pathways that are distinct from the classical HPA-axis stress response mediated primarily through CRHR1.

Evidence

  • Human: No clinical trials reported for this specific analog.
  • Animal: CRF [1–40] peptides from porcine hypothalami were shown to stimulate corticotropin release from rat pituitary cells in the original isolation work (Patthy et al., PNAS 1986). Broader preclinical literature on CRHR2-selective ligands in animal models exists within the CRF receptor pharmacology field.
  • In vitro: Receptor binding characterization consistent with CRHR2 selectivity has been the primary application of this oxidized variant in research settings.

Mechanism

The native CRF [1–40] peptide activates both CRHR1 and CRHR2, which are class B GPCRs that signal primarily through Gs-coupled cAMP elevation. The M38-oxidized variant alters the local structure of the C-terminal helix region of CRF, where Met38 is part of a conserved hydrophobic surface involved in receptor engagement. This modification shifts the receptor subtype selectivity profile toward CRHR2, making the [M38-oxidized, N40] form a useful probe for dissecting CRHR2-specific signaling from the CRHR1-dominated HPA-axis responses. CRHR2 is expressed peripherally — in the cardiovascular system, gut, and skeletal muscle — where it mediates stress recovery and anxiolytic responses rather than ACTH secretion.

Related peptides

The CRF/urocortin family includes several peptides with overlapping but distinct receptor pharmacology. Native porcine CRF [1–40] (the unoxidized parent sequence) was characterized in the same isolation work (Patthy et al., PNAS 1986). Urocortin peptides (urocortin I, II, and III) are endogenous mammalian ligands with preferential CRHR2 selectivity. ACTH (adrenocorticotropic hormone), the downstream pituitary hormone that CRF drives, is covered on its own platform card.

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 2026-06-05

Does the oxidized amino acid near the end of this peptide explain why it binds one stress receptor but not the other?

If confirmed, this insight could guide the design of drugs that activate the body's stress-recovery system without triggering the acute anxiety-driving receptor, potentially helping people with stress-related disorders.

The hypothesis
Oxidation of Met38 in CRF 1-40 shifts receptor subtype selectivity toward CRHR2 over CRHR1 by disrupting a hydrophobic contact in the CRHR1-specific binding pocket while preserving the CRHR2 interface geometry, and this selectivity is mechanistically distinct from the Q26E substitution used in other CRHR2-selective analogs.
Why it’s plausible
The readme states the M38 oxidation materially affects receptor subtype selectivity. Met sulfoxide is larger and more polar than Met, and the C-terminal region of CRF (residues 35-41) is known to contribute to CRHR1/CRHR2 discrimination. If CRHR1's binding cleft is more sensitive to steric/electronic change at position 38 than CRHR2's, oxidation would selectively impair CRHR1 binding. The Q26E substitution (pep-10647) achieves CRHR2 selectivity through a different position, implying multiple independent selectivity determinants.
Why it matters
Understanding which positions independently control CRHR1/CRHR2 selectivity would allow combinatorial design of highly selective CRHR2 agonists for stress-recovery and cardiac indications, without empirical screening of large analog libraries.
Plausibility.60
Novelty.70
Impact.65
Basis · grounding1 paper · 2 computed/notes
[1]
noteReadme explicitly states Met38 oxidation materially affects receptor subtype selectivity toward CRHR2
[2]
paper
Patthy et al. 1986 characterized oxidized CRF variants from porcine hypothalami; the structural identity of these variants underpins the selectivity observation
doi: 10.1073/pnas.83.9.2969
[3]
sequencePosition 38 in the 40-residue sequence maps to LMEN context (RKLMEN); the C-terminal segment is a known CRH receptor subtype discriminator
openupdated 2026-06-05

Does the oxidized form of this stress hormone keep its receptor active longer than the normal version by avoiding the cell's usual receptor-switching-off mechanism?

If so, this oxidized peptide could be a template for longer-acting drugs that support recovery after stress, with potential uses in anxiety disorders, heart failure, and metabolic conditions.

The hypothesis
CRHR2-selective signaling by oxidized CRF 1-40 is biased toward Gs-mediated cAMP production over beta-arrestin recruitment relative to native CRF 1-41, because the oxidized C-terminal helix stabilizes the receptor in a conformation that favors G-protein coupling over arrestin docking.
Why it’s plausible
Biased agonism at class B GPCRs is determined in part by how the C-terminal alpha-helix of the ligand positions the receptor transmembrane bundle. Met38 oxidation likely alters the helical dipole and packing at the C-terminal receptor interface. If this stabilizes a G-protein-coupling-competent but arrestin-disfavored receptor state, the oxidized peptide would produce more sustained cAMP without the receptor desensitization associated with arrestin recruitment.
Why it matters
Biased CRHR2 agonism favoring cAMP could sustain stress-recovery signaling without receptor internalization, which is a significant advantage for therapeutic applications targeting anxiety, cardiac function, or appetite regulation.
Plausibility.50
Novelty.65
Impact.65
Basis · grounding3 computed/notes
[1]
noteCRF acts on HPA axis via ACTH release, which is cAMP-dependent; CRHR2 is associated with stress recovery and cardiac function
[2]
sequencePosition 38 is in the C-terminal receptor-engaging helix region; Met-to-Met-sulfoxide changes helical polarity and side-chain geometry
[3]
structureipTM=0.802 with pLDDT=52.6 suggests a flexible C-terminus that could sample multiple receptor conformations, consistent with biased signaling via a partially ordered binding mode
openupdated 2026-06-05

Does the oxidized form of this peptide attach to the CRHR2 receptor in a different physical orientation than the normal version?

Understanding this could allow chemists to engineer stress-hormone drugs with a built-in chemical modification that makes them more stable in the body while still selectively calming the stress response.

The hypothesis
The moderate ipTM (0.802) of oxidized CRF 1-40 at CRHR2 reflects genuine binding but with a C-terminal pose that differs from canonical urocortin 2/3 binding, because the oxidized Met38 sulfoxide forces a backbone reorientation in the C-terminal alpha-helix that opens a non-native contact surface.
Why it’s plausible
Class B GPCRs bind their peptide ligands with the C-terminus engaging the receptor ECD and the N-terminus engaging the transmembrane bundle. ipTM of 0.802 (vs 0.919 for pTH 3-34 at PTH1R) suggests the oxidized C-terminal region is less precisely placed. Met sulfoxide introduces a carbonyl-like oxygen that can form an unexpected hydrogen bond or alter helical backbone geometry. This would produce a subtly different binding pose compared to native CRF or urocortin, potentially explaining altered receptor selectivity.
Why it matters
A C-terminal backbone reorientation driven by a post-translational-mimicking oxidation could be exploited to generate CRHR2-biased agonists that are metabolically stable by design, using sulfoxide isosteres.
Plausibility.55
Novelty.60
Impact.50
Basis · grounding3 computed/notes
[1]
structureopenfold3-mlx ipTM=0.802, lower than what class B peptide-GPCR complexes with canonical ligands typically show, suggesting C-terminal pose uncertainty
[2]
noteOxidized Met38 (methionine sulfoxide) materially affects receptor subtype selectivity; the sulfoxide is not visible in the stored sequence but is present in the synthesized peptide
[3]
sequenceThe 40-residue sequence SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEN; position 38 (M in raw sequence) is the site of oxidation in the synthesized variant
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8020362854003906 openfold3-mlx
ranking score 0.8720787167549133 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.709global PDE — lower = better
disorder0.171fraction disordered
chain pair ipTM (A, B)0.802interface quality
3-letter notation
Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Met-Glu-Asn
recipeopenfold3-mlx 0.3.1
parametervalue
modelopenfold3-mlx 0.3.1
weightsaedd8f3eb814e392…
hardwareapple_m4_base_16gb
mlx version0.31.1
python3.14.3
random seed42
msa strategycolabfold
diffusion samples1
runtime350s
predicted bymlx@peptide
predicted at2026-04-22
python3 openfold3/run_openfold.py predict --query_json {query.json} --runner_yaml examples/example_runner_yamls/mlx_runner.yml --output_dir {output_dir} --num_diffusion_samples 1
citationbibtex
peptidemodel (2026). Stress-response research peptide (oxidized CRF 1-40) (pep-10651, v1). PeptideModel. https://peptidemodel.com/card/pep-10651
@peptide{pep10651,
  sequence = {SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEN},
  target   = {crhr2},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 104 on ct.gov · 3 on EUCTR · checked 2026-05-09
ct.gov trials 104
with results 14
EUCTR 3
PubMed RCT 20
by phase
1phase 21phase 31early phase 17no phase
by status
7completed2recruiting1unknown
references 1 papers
discussion no comments
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