pe
pep-10680 v1 CC-BY-SA-4.0

CGRP receptor-binding tail peptide

A small piece of a natural body-signal peptide from the calcitonin family, used only as a lab tool to study how these peptides latch onto their receptors.

statussynthesized targetCALCR length10 aa refs6
snapshot sparse 0% confidence
Class
Endogenous peptide fragment (neuroendocrine)
Status
No approved therapeutic status identified
Best-supported effect
Identified as a putative neuroendocrine regulatory peptide in a peptidomics screen; no validated bioactivity established
Main caveat
No functional assay, animal, or human evidence attached to this card
status 4 / 5
prediction metrics boltz-2 2.2.1
ipTM0.770
pTM0.769
avg pLDDT56.5
ranking score0.606
STRUCTURE · PEP-10680 × CALCR
ranking0.606
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 2.2.1 · mmCIF ↓ download
sequence10 aa
1510
VPTNVGSKAF
in the news 11 articles
overview readme

What this is

VPTNVGSKAF is a 10-residue fragment corresponding to positions 110–119 of the calcitonin gene-related peptide I (CGRP-I) precursor protein — this maps to the C-terminal decapeptide of the 37-amino-acid mature α-CGRP. It belongs to the calcitonin peptide family, which includes calcitonin, α- and β-CGRP, amylin, adrenomedullin, and adrenomedullin 2/intermedin (Hay and colleagues, British Journal of Pharmacology, 2018). The fragment is used primarily as a research tool for probing receptor interactions within this peptide family.

What it does

CGRP-derived fragments interact with receptors of the calcitonin family, principally the calcitonin receptor (CTR/CALCR) and the calcitonin receptor-like receptor (CLR). The intact C-terminal region of CGRP is known to be important for receptor engagement, and isolated C-terminal fragments of CGRP family members have been used in studies of receptor interaction mechanisms (Lee and colleagues, Journal of Biological Chemistry, 2016). The calcitonin receptor itself is expressed on osteoclasts and is progressively upregulated during RANKL-driven osteoclast differentiation (Granholm and colleagues, Journal of Cellular Biochemistry, 2008); it also has biological relevance beyond bone, including roles in the kidney and central nervous system (Pondel, International Journal of Experimental Pathology, 2000).

Evidence

  • Human: No clinical data for this isolated fragment.
  • Animal: No in vivo data specifically for VPTNVGSKAF.
  • In vitro: The fragment corresponds to a region of CGRP identified through peptidomic approaches (Yamaguchi and colleagues, Journal of Biological Chemistry, 2007). Calcitonin and amylin receptor peptide interaction mechanisms — including C-terminal peptide region contributions — have been characterized biochemically at the CALCR level (Lee and colleagues, Journal of Biological Chemistry, 2016).

Mechanism

The calcitonin receptor (CALCR) is a class B GPCR belonging to the secretin receptor family. Its pharmacological diversity arises from heterodimerization with receptor activity-modifying proteins (RAMPs): CTR paired with RAMP1, RAMP2, or RAMP3 forms the amylin receptor subtypes AMY₁, AMY₂, and AMY₃, respectively, which are also activated by amylin and, to varying degrees, by CGRP and adrenomedullin (Hay and colleagues, British Journal of Pharmacology, 2018). CLR paired with RAMP1 forms the canonical CGRP receptor, while CLR/RAMP2 and CLR/RAMP3 form the AM₁ and AM₂ adrenomedullin receptors (Hay and colleagues, 2018). CTR and CLR share structural and signaling themes common to family B GPCRs, with receptor activation engaging both cAMP and intracellular calcium pathways (Barwell and colleagues, British Journal of Pharmacology, 2012). The C-terminal region of calcitonin-family peptides — the region this fragment derives from — contributes to receptor selectivity and binding affinity across the CTR/CLR receptor system (Lee and colleagues, Journal of Biological Chemistry, 2016).

The relevance of this fragment to the amylin receptor system (CTR + RAMPs) makes it useful as a reference sequence when studying co-agonist approaches that engage CTR, such as combination therapies pairing GLP-1 and amylin receptor agonism.

Related peptides

The CGRP-I precursor gives rise to full-length α-CGRP, a major vasodilatory neuropeptide acting at CLR/RAMP1. Other calcitonin-family members that engage overlapping receptor systems include calcitonin (CTR agonist) and amylin (CTR/RAMP complex agonist).

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 this small CGRP piece sit in the calcitonin receptor on osteoclasts and prevent the signals that normally slow down bone breakdown?

If CGRP breakdown products generated naturally in the body antagonize bone-protective calcitonin signaling, this could explain why some people lose bone faster than expected. It might also point to a new way to fine-tune bone metabolism in conditions like osteoporosis.

The hypothesis
VPTNVGSKAF acts as a competitive antagonist at CALCR on osteoclasts to suppress RANKL-driven osteoclast activity, because CALCR is progressively upregulated during osteoclast differentiation and the C-terminal CGRP fragment occupies the receptor binding site without triggering the cAMP signaling that mediates calcitonin's anti-resorptive effect.
Why it’s plausible
CALCR is upregulated during RANKL-driven osteoclast differentiation (Granholm et al., JCB 2008, cited in readme). Calcitonin (8-32), a similarly truncated C-terminal antagonist at CALCR, inhibits calcitonin and amylin signaling at CTR without activation (Pozvek et al., Mol Pharmacol 1997). VPTNVGSKAF is the CGRP-derived C-terminal decapeptide and would be expected to occupy the same receptor region without carrying the N-terminal activation domain. On highly CALCR-expressing osteoclasts, this could competitively reduce endogenous calcitonin efficacy, net effect being reduced bone-resorption suppression, or alternatively compete with osteoclast-targeting calcitonin-based drugs.
Why it matters
Understanding whether short CGRP C-terminal fragments antagonize CALCR on osteoclasts clarifies whether circulating CGRP fragments generated by proteolysis could modulate bone resorption, an overlooked mechanism in postmenopausal bone loss or cancer-related osteolysis.
Plausibility.55
Novelty.70
Impact.65
Basis · grounding1 paper · 2 computed/notes
[1]
noteCALCR is expressed on osteoclasts and progressively upregulated during RANKL-driven osteoclast differentiation (Granholm et al., JCB 2008).
[2]
paper
Receptor components in bone marrow macrophages form functional receptors linked to adenylate cyclase, confirming cAMP-coupled CALCR signaling in osteoclast precursors.
doi: 10.1002/jcb.21674
[3]
noteVPTNVGSKAF maps to the C-terminal decapeptide of mature alpha-CGRP, a region important for receptor engagement (readme and Lee et al., JBC 2016).
openupdated 2026-06-05

Does removing the front part of CGRP change which of the four related calcitonin-family receptors the remaining tail prefers to bind?

If the fragment hits different receptor subtypes than full CGRP, scientists could use it to study individual receptor pathways in migraine, blood vessel regulation, or bone disease without disturbing the others, making research faster and more precise.

The hypothesis
VPTNVGSKAF shows differential binding affinity across the four calcitonin-family receptor complexes (CLR/RAMP1, CLR/RAMP2, CLR/RAMP3, CALCR homodimer) in a rank order distinct from full-length alpha-CGRP, because without the N-terminal activation domain the binding is governed entirely by C-terminal ECD contacts whose geometry differs across receptor subtypes.
Why it’s plausible
Full-length alpha-CGRP shows distinct potency profiles at CGRP receptor (CLR/RAMP1), AM1 (CLR/RAMP2), and AM2 (CLR/RAMP3) receptors: pEC50 values differ markedly across these complexes (Hay et al., BJP 2018, Fig.7). The rank order of selectivity is set partly by N-terminal activation and partly by C-terminal ECD contacts. When the N-terminal domain is removed (as in VPTNVGSKAF), only C-terminal contacts remain, potentially inverting or scrambling the selectivity rank order relative to full-length CGRP.
Why it matters
A fragment with an inverted receptor-selectivity profile compared to the parent peptide would be a uniquely useful pharmacological tool for parsing the roles of individual calcitonin-family receptor subtypes in migraine, vascular tone, and bone metabolism.
Plausibility.50
Novelty.70
Impact.65
Basis · grounding2 papers · 1 computed/note
[1]
paper
Figure 7 shows AM and AM2/IMD pEC50 values for cAMP production across CGRP, AM1, and AM2 receptors, demonstrating subtype-selective pharmacology of calcitonin-family peptides.
doi: 10.1111/bph.14075
[2]
paper
Juxtamembranous region of the CLR amino terminus plays a critical role in small-molecule agonist action, indicating receptor-subtype-specific N-terminal contacts that would be bypassed by the C-terminal fragment.
doi: 10.1111/j.1476-5381.2011.01525.x
[3]
sequenceVPTNVGSKAF lacks CGRP positions 1-27 entirely, removing all N-terminal receptor-activation determinants and leaving only C-terminal ECD-contact residues.
openupdated 2026-06-05

Does this small CGRP fragment bind the calcitonin receptor specifically, avoiding the CGRP receptor that drives migraine and other effects?

If this fragment is selective for the calcitonin receptor, it could help researchers study bone loss and kidney disease pathways in isolation, without accidentally blocking migraine-related receptors that current drugs target. This could lead to cleaner research tools and more targeted drugs.

The hypothesis
VPTNVGSKAF, as the isolated C-terminal decapeptide of alpha-CGRP, binds the calcitonin receptor (CALCR) with higher selectivity for CALCR homodimer than for CLR-RAMP heterodimers (CGRP receptor proper), because the C-terminal SKAF motif contacts CALCR ECD residues that diverge from CLR, making this fragment a naturally selectivity-filtered probe for CALCR versus CLR.
Why it’s plausible
Full-length alpha-CGRP binds both CLR/RAMP1 (canonical CGRP receptor) and CALCR with RAMP modifications. The C-terminal region of calcitonin-family peptides is known to determine receptor-family selectivity: Y25A mutation in calcitonin (8-32) differentially affects RAMP1-CTR binding versus other ECD complexes (Lee et al., JBC 2016). VPTNVGSKAF spans CGRP positions 28-37 and contains the SKAF C-terminus that is known to contribute to receptor engagement. Without the N-terminal activation domain, specificity would be dominated by C-terminal ECD contacts, which differ between CALCR and CLR.
Why it matters
A fragment that selectively labels or blocks CALCR without affecting the CGRP receptor (CLR/RAMP1) would be a valuable tool for dissecting CALCR-specific biology in bone, kidney, and CNS, and could serve as a scaffold for CALCR-selective antagonists.
Plausibility.50
Novelty.65
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
paper
Y25A mutation in calcitonin (8-32) differentially affects binding to RAMP1-CTR ECD versus RAMP2/RAMP3-CTR ECDs, demonstrating that single C-terminal residues encode CALCR complex selectivity.
doi: 10.1074/jbc.m115.713628
[2]
noteThe C-terminal region of CGRP is known to be important for receptor engagement; isolated C-terminal fragments have been used in receptor interaction studies (Lee et al., JBC 2016).
[3]
structureboltz-2 ipTM=0.7702 for CALCR complex; pLDDT=56.5 reflects the short, flexible nature of the decapeptide but the complex confidence is moderate.
openupdated 2026-06-05

If a fatty or polymer chain is attached to the end of this 10-residue peptide, would it stay active in the body long enough to be useful as a research or therapeutic tool?

Long-lasting peptide tools that target this receptor could help researchers track or block bone-loss signaling over extended periods in animal models, accelerating the search for new osteoporosis treatments.

The hypothesis
The SKAF C-terminal tetrapeptide of VPTNVGSKAF is the minimal pharmacophoric unit responsible for CALCR ECD anchoring, and extending it with a lipid or PEG tail at the C-terminus would yield a long-acting CALCR-targeted probe without disrupting the binding determinants that reside in this region.
Why it’s plausible
Systematic truncation studies of calcitonin-family peptides consistently show that C-terminal residues make critical ECD contacts. In calcitonin (8-32), F at the C-terminus (equivalent to SKAF's F) is a key contact point, and its modification is tolerated in some but not all receptor subtypes (Lee et al., JBC 2016). VPTNVGSKAF ends in SKAF, which corresponds to CGRP 34-37. PEGylation or lipidation at the C-terminus of short GPCR-binding peptides is a validated strategy for extending plasma half-life. The low pLDDT (56.5) confirms the fragment is flexible, making it amenable to C-terminal conjugation without disturbing a rigid fold.
Why it matters
A lipidated or PEGylated SKAF-anchored peptide could serve as a long-acting CALCR imaging or blocking agent for in vivo studies of osteoclast activity, cancer-induced bone disease, or CNS calcitonin signaling.
Plausibility.55
Novelty.50
Impact.55
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceVPTNVGSKAF: the SKAF tetrapeptide at the C-terminus is the most receptor-proximal element and the most likely ECD anchor.
[2]
paper
Y25A (C-terminal Phe equivalent in calcitonin 8-32) differentially affects binding across CALCR ECD complexes, confirming C-terminal residues drive selectivity contacts.
doi: 10.1074/jbc.m115.713628
[3]
structurepLDDT=56.5 indicates a disordered/flexible peptide backbone, compatible with C-terminal modification without disrupting a rigid core.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.7701838612556458 boltz-2
ranking score 0.6057608127593994 boltz-2
3-letter notation
Val-Pro-Thr-Asn-Val-Gly-Ser-Lys-Ala-Phe
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). CGRP receptor-binding tail peptide (pep-10680, v1). PeptideModel. https://peptidemodel.com/card/pep-10680
@peptide{pep10680,
  sequence = {VPTNVGSKAF},
  target   = {calcr},
  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 6 papers
discussion no comments
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