pe
pep-10643 v1 CC-BY-SA-4.0

Biotin-tagged CGRP nerve-signal tracer (canine/mouse/rat)

A lab-only version of a natural nerve-signaling protein, tagged with biotin so researchers can track exactly where it binds in the body; used only as a lab research tool.

statussynthesized targetCALCR length37 aa refs4
status 4 / 5
prediction metrics openfold3-mlx 0.3.1
ipTM0.721
pTM0.703
avg pLDDT50.8
ranking score0.825
STRUCTURE · PEP-10643 × CALCR
ranking0.825
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence37 aa
1510152025303537
SCNTATCVTHRLAGLLSRS GGVVKDNFVPTNVGSEAF
in the news 11 articles
overview readme

What this is

Biotin-α-CGRP is a laboratory version of α-CGRP (alpha calcitonin gene-related peptide) carrying a biotin tag, used as a research tool rather than a therapeutic. α-CGRP itself is a 37-amino-acid neuropeptide produced by sensory neurons that signals through receptors in the calcitonin/CGRP family (Hay 2018). The sequence stored here (SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) corresponds to the rat α-CGRP backbone — also conserved in canine and mouse — and the biotin tag is appended separately as a detection handle, not represented in the raw 37-letter sequence. The tag lets researchers pull the peptide down with streptavidin and trace where it binds, which is why this reagent shows up in studies dissecting the calcitonin receptor and amylin-receptor pharmacology that underlies weight-loss and migraine drug development.

What it does

In the body, native α-CGRP acts on a small family of class B (secretin-like) G-protein-coupled receptors built from two scaffolds — the calcitonin receptor (CTR) and the calcitonin-receptor-like receptor (CLR) — each of which pairs with one of three receptor activity-modifying proteins (RAMPs) to define ligand selectivity (Hay 2018, Barwell 2012). CLR with RAMP1 forms the canonical CGRP receptor, while CTR paired with RAMPs forms the amylin receptors (AMY₁, AMY₂, AMY₃) that respond to both amylin and CGRP (Hay 2018). Biotin-α-CGRP itself is not used to "do" anything in vivo — it is used in binding assays where the biotin tag allows the peptide to be captured, visualized, or affinity-purified so that receptor interactions can be characterized (Lee 2016).

Mechanism

α-CGRP and the closely related β-CGRP differ by only a few residues and are produced by alternative splicing of the calcitonin gene, with α-CGRP predominating in primary sensory neurons and β-CGRP more prominent in enteric autonomic neurons (Mulderry 1988). The peptide family as a whole — calcitonin, α-CGRP, β-CGRP, amylin, adrenomedullin and adrenomedullin 2/intermedin — binds CTR or CLR, with the RAMP partner shifting the receptor's preference between ligands (Hay 2018). Mechanistic work on calcitonin and amylin receptors has shown that peptide engagement involves a two-domain interaction: the C-terminus of the peptide first docks to the receptor extracellular domain, and the N-terminus then engages the transmembrane bundle to trigger activation (Lee 2016, Barwell 2012). Because Biotin-α-CGRP carries the α-CGRP backbone intact, it engages this same family of receptors and is used to probe them; the biotin moiety is a handle for downstream detection, not a pharmacophore.

Evidence

  • Human: No human clinical use. This reagent is a research tool; no registered clinical trials.
  • Animal: Underlying α-CGRP biology has been mapped in rat sensory and autonomic neurons, where differential α/β-CGRP expression was first defined (Mulderry 1988).
  • In vitro: Used in biochemical characterizations of calcitonin- and amylin-receptor binding mechanisms (Lee 2016); the broader pharmacology of the calcitonin/CGRP receptor family — including CTR/CLR identity, RAMP heterodimer composition, and ligand cross-reactivity — is summarized in IUPHAR Review 25 (Hay 2018) and earlier in Barwell 2012.

Regulatory status

Biotin-α-CGRP is a research reagent, not a drug. It has no FDA, EMA, or WADA classification. The native α-CGRP / CGRP-receptor axis is the target of approved migraine therapeutics (the gepants and CGRP-pathway monoclonal antibodies), and the broader calcitonin/CGRP/amylin receptor family is therapeutically relevant to osteoporosis, diabetes, obesity, lymphatic insufficiency, migraine and cardiovascular disease (Barwell 2012, Hay 2018) — but those drug classes are distinct molecules, not this peptide.

Open questions

  • The relative affinity of α-CGRP vs β-CGRP at each CTR/RAMP and CLR/RAMP combination is still incompletely mapped (Hay 2018).
  • For Biotin-α-CGRP specifically, the position and linker chemistry of the biotin tag are not documented in this card's references — users of the reagent should consult the supplier's characterization before assuming the tag is inert with respect to receptor binding.
Hypotheses2 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 single amino acid difference between rat and human alpha-CGRP mean the rat peptide activates different receptor sub-types more strongly than the human version?

If true, decades of CGRP research done in rats may not translate directly to humans, which would be an important recalibration for the entire migraine drug development field and could explain why some CGRP-targeting drugs showed unexpected profiles when moving from animal studies to clinical trials.

The hypothesis
The rat/mouse/canine α-CGRP sequence (pep-10643) has higher intrinsic efficacy at CALCR-based amylin receptors than the human α-CGRP sequence (pep-10645), because position 25 is D (aspartate) in the rodent/canine sequence versus N (asparagine) in human, and this charge difference selectively enhances contacts with CALCR extracellular domain residues.
Why it’s plausible
Direct sequence comparison: pep-10643 (rat α-CGRP backbone used in biotin-CGRP) has D at position 25; pep-10645 (human α-CGRP) has N at position 25. The structural data (DOI 10.1074/jbc.m115.713628) demonstrate that position 25 contacts RAMP1-CTR ECD, and a charge at this position (vs neutral) would alter the electrostatic interaction with both RAMP1-CTR and RAMP2-CTR interfaces. This would produce a systematic species difference in relative CLR vs CALCR potency that could confound extrapolation of rodent CGRP pharmacology to human therapeutics.
Why it matters
If rat α-CGRP has higher amylin receptor potency than human α-CGRP due to D25, then rodent models over-represent CALCR-based signalling in CGRP biology, and human therapeutic targeting should specifically account for the lower CALCR engagement of the human peptide.
Plausibility.50
Novelty.50
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
sequencepep-10643 (rat α-CGRP): D at position 25; pep-10645 (human α-CGRP): N at position 25, a charge difference at a known receptor-interface residue
[2]
paper
Position 25 contacts RAMP1-CTR ECD, and charge at this position differentially modulates RAMP1 vs RAMP2 binding
doi: 10.1074/jbc.m115.713628
[3]
structurepep-10643 ipTM=0.72 and pep-10645 ipTM=0.82 at the same CALCR target, possibly reflecting this charge-driven difference in CALCR interface quality
openupdated 2026-06-05

Could attaching biotin at two different locations on alpha-CGRP produce two distinct probes, each labelling a different CGRP receptor sub-type in tissue?

If achievable, researchers could finally map the exact locations of CGRP receptor sub-types throughout the body in a single experiment, accelerating the design of drugs that hit only the desired receptor for migraine treatment or bone protection.

The hypothesis
Site-specific biotinylation of α-CGRP at K25 versus at an engineered N-terminal extension would produce two biotinylated probes with distinct receptor selectivity profiles (CALCR-selective vs CLR/RAMP1-active), enabling paired receptor localisation studies that map each receptor sub-type separately in the same tissue.
Why it’s plausible
K25 is the sole internal Lys in rat α-CGRP sequence; it lies within the receptor-contacting C-terminal helix where position 25 mutations affect RAMP selectivity (DOI 10.1074/jbc.m115.713628). An N-terminal biotin (placed before C2) would be near the disulfide ring but outside the agonist helix. By synthesising two analogs, one with biotin at K25 (helix-disrupted) and one with biotin at an N-terminal spacer (helix-intact), researchers could generate paired CALCR-selective and CLR/RAMP1-active biotinylated probes. The predicted ipTM of 0.72 for the backbone at CALCR supports that CALCR engagement is maintained even when N-terminal ring chemistry is perturbed.
Why it matters
Paired receptor-selective biotinylated CGRP probes would be the first tools to simultaneously and independently map CLR/RAMP1 and CALCR/RAMP expression in the same histological section, enabling precise localisation of receptor subtype distributions relevant to migraine, bone biology, and metabolic disease.
Plausibility.40
Novelty.60
Impact.60
Basis · grounding2 papers · 1 computed/note
[1]
sequenceK25 is the sole Lys in the 37aa sequence (SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF), making it the dominant NHS-ester labelling site, with N-terminal labelling as the alternative
[2]
paper
Position 25 modifications differentially affect binding to RAMP1-CTR vs RAMP2-CTR ECDs, providing the mechanistic basis for K25-biotinylation-driven receptor selectivity
doi: 10.1074/jbc.m115.713628
[3]
paper
CGRP pharmacology review documents the distinct tissue distributions and functions of CLR/RAMP1 vs AMY receptors that such paired probes could map
doi: 10.1111/bph.14075
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.7213250994682312 openfold3-mlx
ranking score 0.8252753019332886 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.914global PDE — lower = better
disorder0.215fraction disordered
chain pair ipTM (A, B)0.721interface quality
3-letter notation
Ser-Cys-Asn-Thr-Ala-Thr-Cys-Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asp-Asn-Phe-Val-Pro-Thr-Asn-Val-Gly-Ser-Glu-Ala-Phe
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
runtime461s
predicted bymlx@peptide
predicted at2026-04-24
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). Biotin-tagged CGRP nerve-signal tracer (canine/mouse/rat) (pep-10643, v1). PeptideModel. https://peptidemodel.com/card/pep-10643
@peptide{pep10643,
  sequence = {SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF},
  target   = {calcr},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 0 trials · checked 2026-05-22
0
no registered clinical trials as of 2026-05-22; we'll re-check periodically
references 4 papers
discussion no comments
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peptidemodel.com CC-BY-SA-4.0 research only · not for human use