pe
pep-10589 v1 CC-BY-SA-4.0

Gila monster venom peptide that activates the GLP-1 diabetes target (Exendin-3)

A natural peptide from Gila monster venom that activates the same receptor targeted by diabetes drugs like semaglutide; used only as a lab research tool.

statussynthesized targetGLP-1R length39 aa refs1
status 4 / 5
prediction metrics boltz-2 1.0
ipTM0.912
pTM0.859
avg pLDDT73.7
ranking score0.772
STRUCTURE · PEP-10589 × GLP-1R
ranking0.772
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 1.0 · mmCIF ↓ download
sequence39 aa
1510152025303539
HSDGTFTSDLSKQ MEEEAVRLFIEWL KNGGPSSGAPPPS
in the news 136 articles
overview readme

Snapshot

Class: Venom-derived glucagon superfamily peptide
Evidence tier: In vitro / assay evidence
Status: No approved therapeutic status identified. Research and reference compound; not an approved drug.
Best-supported effect: Receptor-mediated cAMP stimulation in pancreatic acinar cells (in vitro, low-concentration exendin-receptor interaction) and VIP-receptor-mediated cAMP and amylase release at higher concentrations — characterized in original isolation studies.
Main caveat: No animal efficacy data or human trial data are present. All described activity is from biochemical receptor and cell-system characterization.


What this is

Exendin-3 is a 39-amino-acid peptide originally isolated from the venom of the beaded lizard (Heloderma horridum). It is a member of the glucagon superfamily, a family of structurally related peptides that includes glucagon, GLP-1, VIP, and related hormones. Exendin-3 is distinct from exendin-4 (isolated from Heloderma suspectum), which served as the structural basis for the approved GLP-1 receptor agonist exenatide; the two exendins are related but separate molecules with different sequences. Published research characterizes exendin-3 as interacting with putative exendin receptors at low concentrations and with VIP receptors at higher concentrations, producing cAMP and amylase responses in pancreatic acinar cell systems. Exendin-3 has no approved therapeutic application.


Evidence map

Evidence layerGradeWhat it supports
HumanNone identifiedNo human evidence is identifieds available literature
AnimalNone identifiedNo animal experiment data are identifieds available literature
In vitroWeakReceptor-mediated cAMP stimulation in pancreatic acinar cell systems; VIP-receptor-mediated cAMP and amylase release at higher concentrations; characterized in the original 1992 isolation paper
ComputationalNone identifiedNo structure prediction or docking data are identifieds available literature
MechanismPlausibleDual-receptor interaction model described in source: exendin-receptor at low concentrations, VIP receptor at higher concentrations; mechanistic basis consistent with glucagon superfamily pharmacology

Claim check

ClaimVerdictEvidence layerConfidence
Stimulates cAMP in pancreatic acinar cells via exendin receptorsSupported (in vitro)In vitroMedium — original isolation characterization; single available literature
Stimulates cAMP and amylase release via VIP receptors at higher concentrationsSupported (in vitro)In vitroMedium — described in original isolation source; single available literature
Therapeutic equivalence to exenatide or exendin-4Not establishedNoneHigh confidence in absence — exendin-3 is a distinct molecule; evidence from exendin-4-derived compounds cannot be applied to this card
Any human efficacy for any indicationNot establishedNoneHigh confidence in absence — no human trial data present in available literature

Assay conditions

This section reports concentrations or conditions used in assays. It does not establish animal or human exposure.

ContextSystemAssay conditionTimepointEndpointLimitation
Receptor interaction characterizationPancreatic acinar cell systemLow concentration (exendin-receptor range)Not individually extracted from sourceIncrease in cellular cAMPSource descriptor only; exact concentrations not individually extracted
Receptor interaction characterizationPancreatic acinar cell systemHigher concentration (VIP-receptor range)Not individually extracted from sourceIncrease in cellular cAMP and amylase releaseSource descriptor only; exact concentrations not individually extracted

Assay limitations

  • Assay conditions (cell system, concentration ranges, species of origin for cell preparations) are not individually extracted from the available literature.
  • receptor activity in summary terms only; no tabular assay results, MIC values, or dose-response curves are reproduced in the available literature file.
  • In vitro receptor interactions do not establish in vivo pharmacology, systemic tolerability, or therapeutic effect in any species.
  • No comparison to exendin-4 or GLP-1 receptor agonist potency is documented.

Mechanism

Exendin-3 is described in the available literature as acting through two receptor systems in a concentration-dependent manner: at low concentrations it interacts with putative exendin receptors on pancreatic acinar cells, producing an increase in intracellular cAMP; at higher concentrations it interacts with vasoactive intestinal peptide (VIP) receptors, stimulating both cAMP accumulation and amylase release. This dual-receptor pharmacology is consistent with the structural relationship of exendin-3 to the glucagon superfamily, members of which share receptor cross-reactivity at sufficient concentrations. The specific identity and classification of the "putative exendin receptor" described in the 1992 isolation paper reflects the nomenclature and receptor landscape of that period; subsequent work in the exendin field has more precisely characterized GLP-1 receptor interactions for related peptides, but the available literature does not individually document exendin-3's GLP-1 receptor affinity or selectivity data.


Chemistry

FieldValue
Sequence (one-letter)HSDGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Sequence (three-letter)H-His-Ser-Asp-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH₂
Length39 amino acids
TopologyLinear
C-terminal modificationAmide (–NH₂)
OriginVenom of Heloderma horridum (beaded lizard)
Molecular weightNot provided in source
FormulaNot provided in source
CASNot provided in source
Sequence confidenceNeeds review

Open questions

  • Animal and in vivo pharmacology: No animal experiment data are present. Whether the in vitro receptor activity translates to in vivo effects in any species is not established from the available literature.
  • GLP-1 receptor affinity: Exendin-3's affinity and selectivity for the GLP-1 receptor relative to other glucagon superfamily receptors is not documented in the available literature. The 1992 isolation paper predates precise GLP-1 receptor pharmacology; updated binding data are not individually extracted here.
  • Comparison to exendin-4: The sequence and pharmacological differences between exendin-3 and exendin-4 (the basis for exenatide) are not analyzed in the available literature. Whether exendin-3 shares exendin-4's GLP-1 receptor agonist properties is not established in this card.
  • Human relevance: No human trial, pilot, or clinical characterization is present.
  • Sequence verification: Sequence is drawn from the CU source entry only. Independent primary-source verification against the Eng 1992 original publication has not been performed in this card-writing pass.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.9116411805152893 boltz-2
ranking score 0.7716017961502075 boltz-2
3-letter notation
His-Ser-Asp-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser
recipeboltz-2 1.0
parametervalue
modelboltz-2 1.0
weights
hardwarenvidia_nim_api
mlx version
python
random seed
msa strategycolabfold_nvidia
diffusion samples1
runtime
predicted bymlx@peptide
predicted at2026-04-25
citationbibtex
peptidemodel (2026). Gila monster venom peptide that activates the GLP-1 diabetes target (Exendin-3) (pep-10589, v1). PeptideModel. https://peptidemodel.com/card/pep-10589
@peptide{pep10589,
  sequence = {HSDGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS},
  target   = {glp-1r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 0 trials · checked 2026-05-09
0
no registered clinical trials as of 2026-05-09; we'll re-check periodically
references 1 papers
discussion no comments
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peptidemodel.com CC-BY-SA-4.0 research only · not for human use