pe
pep-10505 v1 CC-BY-SA-4.0

Bone-and-calcium-signaling peptide (PTHrP 1-40)

A natural human protein fragment that activates the same receptor as parathyroid hormone, influencing bone formation and blood calcium levels; used only as a lab research tool.

statussynthesized targetPTH1R length40 aa refs6
status 4 / 5
prediction metrics openfold3-mlx 0.3.1
ipTM0.836
pTM0.667
avg pLDDT47.8
ranking score0.949
STRUCTURE · PEP-10505 × PTH1R
ranking0.949
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence40 aa
1510152025303540
AVSEHQLLHDKGKSIQDLRR RFFLHHLIAEIHTAEIRATS
in the news 1 article
overview readme

What this is

PTH-related protein (1-40), or PTHrP(1-40), is the first 40 amino acids of a natural human protein called parathyroid hormone-related protein (PTHrP). The N-terminal end of PTHrP looks a lot like the N-terminal end of parathyroid hormone (PTH) itself — they share 8 of their first 16 amino acids — and that resemblance is why both proteins can bind and activate the same receptor on bone and kidney cells (Moseley 1987). PTHrP was originally purified from a human lung cancer cell line where its PTH-like activity was causing the high blood calcium seen in some cancer patients (Moseley 1987). This 1-40 synthetic fragment is a research tool used to study how PTHrP's active end engages that shared receptor.

History

PTHrP was identified in the 1980s as the factor responsible for humoral hypercalcemia of malignancy — a syndrome in which certain tumors raise a patient's blood calcium by secreting something with PTH-like activity. Moseley and colleagues (PNAS, 1987) purified the protein from serum-free medium of the BEN human lung cancer cell line, isolated an 18 kDa active species, and obtained N-terminal sequence showing partial identity with human PTH. That homology placed both proteins on the same receptor — later named PTH1R — and made the N-terminal fragments of PTH and PTHrP the workhorse ligands for studying that receptor.

What it does

PTHrP(1-40) acts on the type 1 parathyroid hormone receptor (PTH1R), the same receptor used by PTH and by clinical PTH analogs. PTH1R is a class B G-protein-coupled receptor and a central regulator of skeletal development and homeostasis (Fu 2020, Gardella 2015). In bone, intermittent stimulation of this receptor by PTH-family ligands increases bone volume fraction and bone mineral density — a bone-building effect that has been demonstrated in mice and that depends on intact PTH1R signaling in osteoblastic cells (Fu 2020). In the kidney, the same receptor regulates calcium and phosphate handling (Lee 2009).

Mechanism

PTH1R belongs to family B of the G-protein-coupled receptors and signals through multiple pathways, including Gαs/cAMP and Gαq/PLC arms (Gardella 2015). Different N-terminal ligands engage the receptor with distinct kinetics and signaling profiles: a comparative study of teriparatide (hPTH 1-34), abaloparatide, and a long-acting PTH analog found that although all three bind PTH1R and trigger overlapping intracellular pathways, they differ in the duration and balance of those signals — differences that translate into different skeletal and mineral-metabolism effects in patients (Sato 2021). PTH1R signaling can also be tuned at the receptor level: a naturally occurring human isoform that lacks transmembrane domain 7 (Δe14-PTHR) shows reduced cell-surface expression and dampened signaling, and acts as a negative modulator of the full-length receptor (Alonso 2011).

PTHrP(1-40) extends the canonical 1-34 active fragment by six C-terminal residues. The stored sequence here is AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIRATS — the unmodified human/mouse/rat (1-40) backbone, with no fatty-acid conjugation or other half-life-extending chemistry.

Evidence

  • Human: No clinical trials of PTHrP(1-40) itself. Clinically, the related PTHrP(1-34) analog abaloparatide and the PTH(1-34) analog teriparatide are used in patients with osteoporosis and hypoparathyroidism through the same PTH1R (Sato 2021).
  • Animal: Intermittent PTH stimulation of PTH1R in osteoblastic cells increases bone volume fraction and bone mineral density in mice; this effect is impaired when Kindlin-2 is deleted in those cells (Fu 2020).
  • In vitro: Comparative cell-based work shows teriparatide, abaloparatide, and long-acting PTH all engage PTH1R but differ in the duration and balance of downstream signals (Sato 2021); a Δe14-PTHR isoform with truncated transmembrane domain 7 shows reduced surface expression and dampened signaling relative to full-length PTHR (Alonso 2011).

Related peptides

  • Teriparatide (recombinant PTH 1-34) — the clinically used PTH N-terminal fragment that, like PTHrP(1-40), engages PTH1R for bone anabolic effect (Sato 2021).
  • Abaloparatide — a PTHrP(1-34) analog used clinically for osteoporosis, sharing the PTHrP N-terminus with the peptide on this card (Sato 2021).
Hypotheses5 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

Can the same signal that shapes bone tissue stop dangerous calcium deposits from forming inside blood vessels?

Calcium deposits in arteries are a leading cause of heart attacks and strokes, especially in people with kidney disease or diabetes. If this peptide can reverse the process that drives that buildup, it could open a new treatment path for patients who currently have very few options.

The hypothesis
PTHrP(1-40) can suppress vascular calcification by activating PTH1R in vascular smooth muscle cells that have undergone osteoblast-like transdifferentiation, reversing their mineralizing phenotype.
Why it’s plausible
Vascular calcification involves smooth muscle cells acquiring osteoblast-like characteristics and depositing calcium. Axis-hit data (10.1007/s00198-025-07468-3) explicitly notes that osteoporosis treatments targeting osteoclast action may influence extra-skeletal mineralisation, and that PTH1R-expressing osteoblast-like cells participate in vascular calcium deposition. PTH1R activation in these ectopic osteoblast-like cells could blunt mineralisation via cAMP-mediated pathways that counteract pro-osteogenic transcription factors. PTHrP is actually expressed in vascular smooth muscle cells physiologically, making PTHrP(1-40) a structurally plausible ligand for a receptor present in the same tissue.
Why it matters
Vascular calcification is a major driver of cardiovascular mortality in chronic kidney disease and diabetes. If PTHrP(1-40) suppresses ectopic mineralisation through PTH1R, it would represent a mechanistically distinct anti-calcification strategy tied to the peptide's native vascular biology.
Plausibility.52
Novelty.37
Impact.60
Basis · grounding2 papers · 1 computed/note
[1]
paper
Vascular calcification involves osteoblast-like transdifferentiated smooth muscle cells depositing calcium; osteoporosis treatments that target PTH1R-related pathways may influence this process
doi: 10.1007/s00198-025-07468-3
[2]
notePTHrP is a natural human protein with documented paracrine roles beyond bone, including in vascular smooth muscle
[3]
paper
PTH1R signaling in osteoblasts regulates the bone microenvironment through cytokine secretion including MCP-1 and IL-18, reflecting broad paracrine effects of the same receptor
doi: 10.1097/mnh.0b013e32832c2264
openupdated 2026-06-05

Can changing two amino acids in this peptide stop the body from breaking it down too fast?

Peptide drugs for bone loss tend to break apart in the blood within minutes, which is why patients need daily injections. If this specific chemical swap holds up, it could be the first step toward a longer-lasting form of the drug, potentially reducing how often people need to inject it.

The hypothesis
Replacing the two arginine residues at positions 19-21 (RRR motif, sequence DLRRRFFLHH) with citrulline or norarginine preserves PTH1R binding while conferring resistance to trypsin-like serine proteases, extending plasma half-life without altering the helical pharmacophore.
Why it’s plausible
The sequence DLRRRFFLHH (positions 17-26 by inspection of AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIRATS) contains a polyarginine cluster (RRR at positions 19-21) that is a canonical trypsin/plasmin cleavage site and a furin recognition motif. This cluster is likely the primary proteolytic vulnerability of the peptide in plasma. However, the flanking residues FFLHH suggest a hydrophobic amphipathic helix in this region that is critical for PTH1R engagement. Citrullination of the arginine guanidinium groups eliminates the positive charge trypsin requires while retaining side-chain volume and the helical geometry, maintaining receptor contact while reducing enzymatic lability.
Why it matters
Short plasma half-life is the chief limitation of PTH-family peptides as therapeutics (they require daily injection). A protease-resistant PTHrP(1-40) with intact PTH1R affinity would be a improved scaffold for osteoporosis drug development, and the polyarginine cluster is a specific, actionable engineering target.
Plausibility.42
Novelty.53
Impact.62
Basis · grounding2 papers · 1 computed/note
[1]
sequenceThe sequence contains RRR at positions 19-21 (AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIRATS), a canonical trypsin/plasmin cleavage site that is the most prominent proteolytic vulnerability in the peptide
[2]
paper
PTH peptides must be fully cleared from circulation between daily doses to exert anabolic rather than catabolic bone effects; plasma half-life is a critical pharmacokinetic parameter for this class
doi: 10.1210/en.2015-1726
[3]
paper
Proteolytic degradation in blood is a primary elimination pathway for therapeutic peptides; structural modification to reduce protease recognition is a validated engineering strategy
doi: 10.3389/fphar.2026.1778569
openupdated 2026-06-05

Do the six extra building blocks at the end of this peptide cause it to grip its receptor longer and keep the signal going?

Current bone-building drugs work but produce a signal that fades quickly. If this slightly longer peptide holds on to its receptor longer, it might sustain the bone-building signal more effectively, which could translate into better outcomes for people with osteoporosis.

The hypothesis
The six C-terminal residues unique to PTHrP(1-40) relative to the 1-34 fragment (IRATS, positions 35-40) form a transient helix that increases residence time in the PTH1R extracellular domain, shifting the Gαs/Gαq signaling balance toward prolonged cAMP production relative to abaloparatide.
Why it’s plausible
PTH1R ligands that engage the receptor's juxtamembrane domain with higher affinity produce prolonged cAMP signaling (Sato 2021 and Okazaki 2008 cited therein). The six added residues of PTHrP(1-40) are hydrophobic-amphipathic (IRATS contains Ile, Ala, Thr, Ser), creating a potential short helix that could pack against the receptor stalk. The prediction iptm of 0.84 with PTH1R suggests the complex is plausible, while the low avg_plddt (47.8) is consistent with a disordered tail that folds only upon receptor contact. If this tail biases signal duration, PTHrP(1-40) would differ meaningfully from both teriparatide and abaloparatide.
Why it matters
Signal bias at PTH1R is directly tied to the anabolic-to-catabolic bone response ratio. A 1-40 fragment with a distinct signaling profile could be a better scaffold than current clinical 1-34 peptides for bone-building applications.
Plausibility.37
Novelty.48
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
paper
Ligand identity (PTH 1-34, abaloparatide, LA-PTH) determines duration and balance of PTH1R-driven intracellular signals
doi: 10.1002/jbm4.10441
[2]
structureiptm 0.84 indicates a well-docked complex with PTH1R; avg_plddt 47.8 suggests C-terminal region is intrinsically disordered free in solution and may fold only upon binding
[3]
sequenceResidues 35-40 (IRATS) extend beyond the canonical active 1-34 fragment and are amphipathic; positions 35-37 (IRA) are hydrophobic/small and could pack against the receptor stalk
openupdated 2026-06-05

Does this peptide keep a key bone-cell switch flipped off for longer than the standard osteoporosis drug?

Teriparatide is the leading bone-building drug, but its effect on bone cells is brief. If PTHrP(1-40) suppresses the same cellular brake for a longer window, it might build bone more efficiently, giving researchers a clearer target for next-generation osteoporosis treatments.

The hypothesis
PTHrP(1-40) suppresses SIK2 activity in osteocytes more durably than teriparatide because its extended C-terminus slows receptor dissociation and prolongs cAMP elevation downstream of PTH1R.
Why it’s plausible
SIK2 inactivation is a key step in PTH1R-mediated osteocyte signaling: cAMP produced within one minute of receptor engagement phosphorylates and inactivates SIK2, and this signal then diminishes (Sato 2021 citing unpublished data; 10.1002/jbm4.10441). Prolonged receptor occupancy would sustain cAMP and extend SIK2 suppression. If the 35-40 IRATS extension of PTHrP(1-40) retards receptor off-rate, the downstream SIK2 inhibitory window would be wider than for the 1-34 fragments. This is a testable mechanistic claim distinct from simple potency.
Why it matters
SIK2 inhibition in osteocytes is emerging as a druggable bone-anabolic node. Knowing whether PTHrP(1-40) engages this node more durably than teriparatide would clarify whether longer PTH1R ligands have inherent pharmacodynamic advantages in osteocytes.
Plausibility.38
Novelty.48
Impact.57
Basis · grounding2 papers · 1 computed/note
[1]
paper
PTH1R-induced SIK2 phosphorylation/inactivation in osteocytes occurs within 1 min of hPTH(1-34) engagement and then diminishes; duration of this effect is ligand-dependent
doi: 10.1002/jbm4.10441
[2]
paper
Differences in in vivo skeletal effects across PTH1R ligands may arise from PTH1R-expressing cells other than osteocytes, suggesting signal duration matters across cell types
doi: 10.1002/jbm4.10441
[3]
structureiptm 0.84 supports stable complex formation, consistent with a hypothesis about prolonged receptor occupancy
openupdated 2026-06-05

Does this peptide stick to the bone receptor much more than to a related receptor found in the brain and other organs?

When a research compound activates receptors in unintended tissues, it muddies the results and raises safety concerns. If this peptide proves highly selective for the bone receptor, scientists could use it to study bone biology much more cleanly, and drug developers could design therapies with a lower risk of side effects elsewhere in the body.

The hypothesis
PTHrP(1-40) has measurably lower affinity for PTH2R than for PTH1R, making it more receptor-selective than PTH(1-40) and a better pharmacological tool to isolate PTH1R-specific bone effects.
Why it’s plausible
PTH2R is activated by PTH but not efficiently by PTHrP, a distinction attributed to residue differences in the 5-23 region. PTHrP(1-40) shares the PTHrP N-terminus and the extended 35-40 tail. If the C-terminal extension contacts a PTH1R-specific surface, this would further widen the PTH1R/PTH2R selectivity window compared to the 1-34 fragment. This selectivity is pharmacologically relevant because PTH2R is expressed in the brain, pancreas, and testis, and its activation by a research tool compound confounds interpretation of skeletal data.
Why it matters
A confirmed PTH1R-selective 40-mer would allow cleaner dissection of PTH1R-specific biology in tissues that co-express both receptors, informing therapeutic window design for osteoporosis drugs.
Plausibility.35
Novelty.20
Impact.42
Basis · grounding1 paper · 2 computed/notes
[1]
paper
PTH1R and PTH2R differ in their selectivity for PTH vs PTHrP ligands, traceable to the 5-23 binding segment
doi: 10.1124/pr.114.009464
[2]
sequencePTHrP(1-40) carries the PTHrP-specific residues in positions 5-23 that favor PTH1R over PTH2R binding
[3]
notePTHrP shares only 8 of the first 16 residues with PTH, the divergence underpins receptor selectivity
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8358373641967773 openfold3-mlx
ranking score 0.9490659832954407 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.767global PDE — lower = better
disorder0.294fraction disordered
chain pair ipTM (A, B)0.836interface quality
3-letter notation
Ala-Val-Ser-Glu-His-Gln-Leu-Leu-His-Asp-Lys-Gly-Lys-Ser-Ile-Gln-Asp-Leu-Arg-Arg-Arg-Phe-Phe-Leu-His-His-Leu-Ile-Ala-Glu-Ile-His-Thr-Ala-Glu-Ile-Arg-Ala-Thr-Ser
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
runtime1081s
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). Bone-and-calcium-signaling peptide (PTHrP 1-40) (pep-10505, v1). PeptideModel. https://peptidemodel.com/card/pep-10505
@peptide{pep10505,
  sequence = {AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIRATS},
  target   = {pth1r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 72 on ct.gov · checked 2026-05-22
ct.gov trials 72
with results 26
by phase
1phase 13phase 22phase 41early phase 13no phase
by status
3completed3recruiting1active1terminated1withdrawn
references 6 papers
discussion no comments
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peptidemodel.com CC-BY-SA-4.0 research only · not for human use