pe
pep-10647 v1 CC-BY-SA-4.0

Stress-recovery research peptide (modified CRF fragment)

A lab-made tweak of the brain's stress-signal hormone, redesigned to switch on the body's 'calm-down after stress' receptor instead of the alarm one. Used only as a research tool, not a medicine.

statussynthesized targetCRHR2 length40 aa refs1
status 4 / 5
prediction metrics openfold3-mlx 0.3.1
ipTM0.799
pTM0.723
avg pLDDT53.1
ranking score0.869
STRUCTURE · PEP-10647 × CRHR2
ranking0.869
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence40 aa
1510152025303540
SEEPPISLDLTFHLLREVLE MARAEELAQQAHSNRKLMEI
overview readme

What this is

Corticotropin-releasing factor [1-40; E26, I40] is a synthetic, 40-residue analog of human CRF — the hypothalamic hormone that launches the body's stress response. The bracketed notation marks two amino acid substitutions from the native CRF sequence: a glutamate (E) at position 26 and an isoleucine (I) at position 40. These changes shift receptor preference toward CRHR2, the second of two CRF receptors, which is thought to counterbalance the acute stress-response drive of CRHR1. The peptide is primarily a laboratory research tool used to selectively probe CRHR2 biology. Patthy and colleagues (1986) isolated a family of CRF-related polypeptides from porcine hypothalami — including peptides sharing this sequence — and confirmed their ability to stimulate corticotropin release from rat pituitary cells, establishing the structural lineage from which designed CRHR2-selective analogs like this one descend.

What it does

In the body, CRF acts as the upstream trigger for the stress axis: the hypothalamus releases CRF, which reaches the pituitary and prompts secretion of ACTH, which in turn drives cortisol release from the adrenal glands. The two CRF receptors — CRHR1 and CRHR2 — do not play identical roles. CRHR1 is broadly linked to acute stress arousal and anxiety-like behavior, while CRHR2 is associated with physiological recovery, stress adaptation, and cardiac function. Because this analog selects preferentially for CRHR2, researchers use it to study those downstream CRHR2-mediated effects in isolation — without the confounding activity at CRHR1 that the native CRF sequence would produce.

Evidence

  • Human: No human trials reported for this analog. It is an investigational research compound.
  • Animal: The CRF peptide family from which this analog derives was characterized in porcine hypothalami and validated for CRF activity in rat pituitary superfusion experiments (Patthy and colleagues, 1986).
  • In vitro: CRHR2 binding and functional selectivity profiling are the primary experimental uses; specific binding values for this variant are not reported in the sources available here.

Mechanism

Corticotropin-releasing factor receptors (CRHR1 and CRHR2) are class B G protein-coupled receptors that signal primarily through Gs, raising intracellular cAMP and activating downstream kinase cascades. Wild-type CRF binds both receptors, but the two positions altered in this analog — 26 and 40 — influence receptor contact geometry in ways that favor CRHR2 engagement. CRHR2 is expressed in peripheral tissues including the heart, skeletal muscle, and gastrointestinal tract, as well as in select brain regions, giving it a profile more associated with peripheral physiology and stress recovery than the CNS stress-alarm role associated with CRHR1. This analog is therefore used as a pharmacological probe to dissect CRHR2-specific signaling in experimental systems where receptor subtype selectivity is required for a clean interpretation.

Open questions

  • No binding affinity data (Ki or IC50 at CRHR1 vs. CRHR2) are available in public sources for this specific variant; rigorous selectivity quantification remains to be published.
  • Functional consequences of CRHR2 engagement — anxiolysis, cardioprotective effects, energy homeostasis — have been studied with native CRHR2-preferring ligands (urocortins 2 and 3) but direct comparison of this synthetic analog against those ligands in the same assay system has not been described in the available literature.
  • The role of the I40 substitution in particular in determining receptor selectivity versus simple C-terminal stability is not resolved in the published literature accessible here.
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

Would restoring the missing chemical modification at the end of this peptide boost its binding to the recovery receptor without losing its ability to ignore the anxiety receptor?

If so, chemists have a simple one-step improvement to convert this research compound into a high-quality therapeutic candidate for stress, cardiac, and metabolic conditions, saving significant time and cost compared to designing a new peptide from scratch.

The hypothesis
Combining the E26 substitution of this peptide with a C-terminal amide (converting Ile40 to Ile40-NH2) would restore CRHR2 binding to the affinity level of urocortin 2 while retaining the CRHR2 selectivity conferred by E26, because the amide correction would fix C-terminal docking deficiency without reversing the mid-helix selectivity mechanism.
Why it’s plausible
This peptide lacks the C-terminal amide present in human CRF (Ile41-NH2) that is essential for receptor binding. If the amide is a general class B GPCR binding enhancer rather than a CRHR1-specific element, adding it back would increase CRHR2 affinity without restoring CRHR1 affinity (because E26 would still impair CRHR1 binding). The result would be a higher-affinity, equally selective CRHR2 agonist.
Why it matters
A high-affinity E26-amidated CRHR2 agonist would be a superior research tool and a more tractable therapeutic lead than either the parent porcine sequence or the urocortins, combining natural CRF-family structural features with engineered selectivity.
Plausibility.65
Novelty.55
Impact.60
Basis · grounding3 computed/notes
[1]
notePep-10650 readme states the C-terminal amide of CRF is essential for receptor binding; this peptide (pep-10647) ends in Ile40 without amide, likely reducing receptor affinity
[2]
sequenceSequence ends at position 40 (I); adding NH2 to Ile40 would mimic the human CRF C-terminal amide without changing the backbone, preserving E26 selectivity
[3]
structureipTM=0.799 may underestimate the true binding of an amidated version; the moderate score is consistent with a C-terminal docking penalty that amidation could correct
openupdated 2026-06-05

Does adding a negative electrical charge at position 26 of this stress peptide push it away from the anxiety-driving receptor and toward the calming one?

If charge at position 26 is the key, chemists could design new stress-hormone drugs with precise receptor targeting by adding or removing charges at this position, leading to more specific treatments for stress disorders with fewer off-target effects.

The hypothesis
The Q26E substitution in CRF [1-40; E26, I40] confers CRHR2 selectivity by introducing a negative charge at position 26 that is repelled by an acidic residue in the CRHR1 binding interface but accommodated by a complementary basic residue in the CRHR2 interface, making this a charge-based rather than steric-based selectivity mechanism.
Why it’s plausible
Position 26 in CRF falls in the amphipathic helix (sequence context: ARAEELAQQAHSNRK; E26 replaces the native Q26). Glutamine to glutamate substitution introduces a negative charge. If CRHR1 presents an acidic residue at the complementary binding site, electrostatic repulsion would reduce CRHR1 affinity. CRHR2, presenting a basic residue at the equivalent position, would be compatible or even enhanced. This is distinct from the steric disruption proposed for Met30 and Met38 oxidation.
Why it matters
Establishing charge complementarity as a CRHR2 selectivity mechanism would enable rational design of salt-bridge-forming CRHR2-selective analogs, and would predict which other positions in CRF can be substituted with charged residues to achieve selectivity without structural disruption.
Plausibility.60
Novelty.60
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
noteE26 substitution (Q to E, neutral to negative) is described as shifting receptor preference toward CRHR2; the peptide is a CRHR2-selective research tool
[2]
sequencePosition 26 in SEEPPISLDLTFHLLREVLEMARAEELAQQ reads as E (from the substitution); native Q26 is neutral while E26 carries a negative charge at physiological pH
[3]
paper
Patthy et al. 1986 established porcine CRF structural variants including peptides sharing this sequence as CRF-active, confirming the biological activity of this backbone
doi: 10.1073/pnas.83.9.2969
openupdated 2026-06-05

Does this modified CRF peptide attach to the recovery receptor without fully activating it, producing only a partial signal?

Partial activators can sometimes be better drugs than full activators because they produce a controlled, moderate response. If confirmed, this peptide could serve as a template for safer stress-recovery drugs that avoid the risks of over-stimulating the CRHR2 system in the heart and brain.

The hypothesis
CRF [1-40; E26, I40] behaves as a partial agonist rather than a full agonist at CRHR2, because the double modification (E26 substitution and Ile40 C-terminus without amidation) collectively reduces the maximum signaling efficacy even as receptor binding affinity is maintained, producing a submaximal cAMP response.
Why it’s plausible
Full agonism at CRHR2 requires both high-affinity receptor engagement (driven by C-terminal docking) and efficient G-protein coupling (driven by N-terminal activation). The E26 substitution alters the mid-helix charge landscape that may influence receptor TM bundle opening geometry, and the absence of C-terminal amide (Ile40, no amide vs human CRF Ile41-NH2) reduces receptor docking efficiency. Together, these features may produce high occupancy but submaximal activation, the hallmark of partial agonism.
Why it matters
If E26,I40-CRF is a partial agonist at CRHR2, it could have therapeutic value as a partial agonist where full CRHR2 activation is excessive (e.g., in cardiac overstimulation models), and would need to be re-characterized in assays that distinguish affinity from efficacy.
Plausibility.55
Novelty.55
Impact.55
Basis · grounding3 computed/notes
[1]
structureipTM=0.799, moderate, consistent with receptor engagement but not fully optimized interface, compatible with partial agonism
[2]
notePeptide is described as CRHR2-preferring and as a laboratory research tool; literature on CRHR2 partial agonism in the CRF family is sparse
[3]
sequenceE26 changes mid-helix charge; I40 C-terminus lacks amide; both modifications diverge from the optimal human CRF CRHR2-stimulating scaffold
openupdated 2026-06-05

Can this modified stress hormone reduce food intake by activating hunger-control circuits in the brain without triggering the anxiety effects of the stress hormone system?

If this peptide suppresses appetite via CRHR2 without anxiety side effects, it could serve as a model for a new class of weight-control drugs that tap into the brain's stress-recovery system rather than the anxiety-driving stress system, potentially offering a safer path to treating obesity.

The hypothesis
CRF [1-40; E26, I40] selectively activates CRHR2 on hypothalamic neurons that control feeding and energy balance, suppressing appetite and increasing energy expenditure without engaging CRHR1-mediated anxiety circuits, making it a candidate probe for dissecting the CRHR2 satiety pathway in obesity research.
Why it’s plausible
CRHR2 in the hypothalamus, particularly in the dorsomedial hypothalamus and ventromedial hypothalamus, modulates food intake and energy expenditure. CRHR1 drives anxiety and HPA activation. A CRHR2-selective agonist like this peptide would activate the anorexigenic CRHR2 pathway without the stress/anxiety confound that makes non-selective CRF analogs unsuitable for appetite studies. The E26 substitution's selectivity would make results interpretable as purely CRHR2-mediated.
Why it matters
Understanding the CRHR2 satiety axis with a selective pharmacological tool could accelerate identification of anti-obesity targets in the CRF system, an underexplored neuropeptide family for metabolic therapeutics.
Plausibility.50
Novelty.55
Impact.60
Basis · grounding2 computed/notes
[1]
noteCRHR2 is described as associated with physiological recovery and stress adaptation; CRHR2 is expressed in hypothalamic energy-regulation circuits
[2]
sequenceE26 confers CRHR2 selectivity on a CRF scaffold; selective CRHR2 agonism in the hypothalamus is mechanistically linked to appetite suppression via known signaling pathways
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.7991151213645935 openfold3-mlx
ranking score 0.8691758513450623 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.717global PDE — lower = better
disorder0.171fraction disordered
chain pair ipTM (A, B)0.799interface 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-Glu-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Met-Glu-Ile
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
runtime349s
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-recovery research peptide (modified CRF fragment) (pep-10647, v1). PeptideModel. https://peptidemodel.com/card/pep-10647
@peptide{pep10647,
  sequence = {SEEPPISLDLTFHLLREVLEMARAEELAQQAHSNRKLMEI},
  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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peptidemodel.com CC-BY-SA-4.0 research only · not for human use