pe
pep-10502 v1 CC-BY-SA-4.0

Bone-building cancer-calcium peptide: PTHrP (1-34) fragment

A fragment of a protein that some tumors release to raise blood calcium; in controlled doses it stimulates bone growth by activating the same receptor as parathyroid hormone. Experimental, not an approved drug.

statussynthesized targetPTH1R length34 aa refs6
status 4 / 5
prediction metrics openfold3-mlx 0.3.1
ipTM0.844
pTM0.647
avg pLDDT45.7
ranking score0.960
STRUCTURE · PEP-10502 × PTH1R
ranking0.960
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence34 aa
15101520253034
AVSEHQLLHDKGKSIQD LRRRFFLHHLIAEIHTA
in the news 1 article
overview readme

What this is

This is the N-terminal 1–34 fragment of parathyroid hormone-related protein (PTHrP), the factor historically called "humoral hypercalcemia of malignancy factor" — the substance that certain tumors secrete to drive blood calcium upward in cancer patients. PTHrP was purified from a human lung cancer cell line and named for this clinical syndrome, but it later turned out to be a normal developmental and skeletal hormone in its own right (Moseley 1987). The 1–34 fragment retains the receptor-binding activity of the full protein and is built around the same parathyroid hormone 1 receptor (PTH1R) that PTH itself uses (Gardella 2015). The stored sequence is shown here as a 34-residue chain with a C-terminal amide cap, which is how this fragment is typically synthesized for laboratory and pharmacological use; the -NH₂ cap is not visible in the raw single-letter sequence.

History

PTHrP was identified in 1987 when Moseley and colleagues purified an 18 kDa protein from the conditioned medium of the BEN human lung cancer cell line, a tumor type associated with paraneoplastic hypercalcemia (Moseley 1987). N-terminal sequencing of the purified factor showed that 8 of the first 16 residues were identical to human PTH, immediately establishing the molecule as a structural cousin of parathyroid hormone — and explaining why tumors expressing it could mimic primary hyperparathyroidism. That discovery opened a long arc of work on the PTH/PTHrP receptor and on synthetic 1–34 fragments as bone-anabolic drug leads, eventually leading to the development of abaloparatide, a clinical PTHrP(1–34) analog (Brent 2021).

What it does

PTHrP(1–34) binds and activates PTH1R, a class B G-protein-coupled receptor expressed on osteoblasts, kidney tubule cells, and chondrocytes (Gardella 2015). PTH1R is the same receptor used by parathyroid hormone — the two ligands share the same binding site even though their full-length sequences diverge after the N-terminus. Through PTH1R, intermittent exposure to PTH or PTHrP(1–34) stimulates bone formation: in mice, intermittent PTH increases bone volume fraction and bone mineral density, an effect that depends on intact PTH1R signaling in osteoblastic cells (Fu 2020). This is the same biology that underpins the bone-anabolic drug class to which the closely related synthetic analog abaloparatide belongs (Brent 2021).

Mechanism

PTHrP(1–34) and PTH(1–34) bind PTH1R in two interconverting conformations, conventionally labeled R⁰ (a high-affinity, more stable complex) and RG (a G-protein-coupled, transient complex). Hattersley and colleagues (2016) showed that abaloparatide — a synthetic PTHrP(1–34) analog — preferentially selects the RG conformation, producing more transient cAMP signaling than PTH(1–34), and proposed that this kinetic difference underlies abaloparatide's more anabolic, less resorptive, less hypercalcemic profile in animal models. The native PTHrP(1–34) fragment represented by this card sits in the same conformational landscape and engages the same Gαs-cAMP output, but without the rebalanced kinetics introduced by the abaloparatide substitutions. Downstream of PTH1R in bone, intact integrin adaptor signaling is required for the anabolic response: deletion of Kindlin-2 in osteoblastic cells in mice largely neutralizes intermittent PTH's effect on bone volume and BMD by impairing both osteoblast and osteoclast formation (Fu 2020).

Evidence

  • Human: No clinical-trial data on PTHrP(1–34) itself as a drug in the references for this card. The clinical evidence base for the closely related synthetic PTHrP(1–34) analog abaloparatide is summarized in a dedicated review (Brent 2021). A separate small clinical study in hypercalcemic hyperparathyroid patients tested a PTH receptor antagonist, BIM-44002, and observed acute effects on serum calcium and PTH levels (Rosen 1997) — relevant as proof-of-concept for PTH1R pharmacology in humans, not as evidence for the agonist 1–34 fragment.
  • Animal: Intermittent PTH increases bone volume fraction and bone mineral density in adult mice through PTH1R on osteoblastic cells; this response is largely lost when the integrin adaptor Kindlin-2 is deleted in those cells (Fu 2020). Preclinical work on the synthetic PTHrP(1–34) analog abaloparatide is reviewed by Brent (2021).
  • In vitro: PTHrP(1–34) and the abaloparatide analog engage PTH1R in two conformations (R⁰ and RG) with different selectivities, producing different cAMP-signaling kinetics in receptor-expressing cells (Hattersley 2016). The native PTHrP factor was first purified to homogeneity from BEN human lung carcinoma cell culture medium, where it migrated as an 18 kDa band on SDS-PAGE and shared 8 of 16 N-terminal residues with human PTH (Moseley 1987).

Known effects

  • Bone-anabolic signaling at PTH1R — established in vitro and in animal models for PTH/PTHrP(1–34) and for the synthetic analog abaloparatide (Hattersley 2016; Fu 2020; Brent 2021).
  • Hypercalcemic / PTH-mimetic activity — PTHrP is the founding factor of the humoral hypercalcemia of malignancy syndrome and was originally purified on the strength of its PTH-like bioactivity (Moseley 1987).
  • Receptor pharmacology distinct from PTH(1–34) — preferential engagement of the RG conformation of PTH1R relative to the R⁰ state, characterized for the abaloparatide analog (Hattersley 2016).

Regulatory status

The native peptide represented by this card — synthetic PTHrP(1–34) amide — is not itself an approved drug. The clinically developed PTHrP(1–34) analog abaloparatide is reviewed by Brent (2021) and is the relevant entry point for the regulatory and clinical context of this molecular family; structural parathyroid-hormone-receptor pharmacology for the broader class is set out in the IUPHAR receptor review (Gardella 2015). This card does not provide dosing, route-of-use, or treatment guidance.

Related peptides

  • Abaloparatide — synthetic PTHrP(1–34) analog with PTH1R-RG-selective signaling characterized in detail (Hattersley 2016; Brent 2021).
  • Parathyroid hormone (PTH) and PTH(1–34) / teriparatide — the other endogenous PTH1R ligand and its bone-anabolic 1–34 fragment, sharing the PTH1R binding site with PTHrP(1–34) (Gardella 2015).
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 2026-06-11

Does the run of three arginine residues in PTHrP(1-34) help decide whether the peptide favors bone-building signals over receptor-shutdown signals?

If this patch helps balance the two signals, changing one or two amino acids might let PTHrP-based osteoporosis drugs keep working longer before bone stops responding. That could help patients who need safer, longer-lasting treatment.

The hypothesis
The RRR cluster at positions 20-22 of PTHrP(1-34) contributes a secondary electrostatic anchoring interaction with the extracellular domain of PTH1R that is distinct from the N-terminal activation epitope, and its disruption would shift the peptide from full agonism toward biased agonism by decoupling Gs from beta-arrestin signaling.
Why it’s plausible
PTH1R is a class B GPCR with a large extracellular domain. The sequence contains a dense Arg20-Arg21-Arg22 triplet flanked by hydrophobic residues (Phe23-Phe24-Leu25). This cationic cluster likely docks into the negatively charged extracellular loop or ECD cleft, influencing how the receptor is stabilized in its active conformation. Biased agonism at PTH1R is pharmacologically relevant and poorly mapped for this fragment.
Why it matters
If the RRR cluster independently controls beta-arrestin recruitment versus G-protein activation, single point substitutions could create PTHrP analogs with improved anabolic bone activity and reduced receptor internalization, a major limitation of current osteoporosis peptide therapies.
Plausibility.62
Novelty.70
Impact.70
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceArg20-Arg21-Arg22 triplet at positions 20-22 is directly readable in AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTA
[2]
structureipTM=0.844 supports a high-confidence complex with PTH1R, consistent with a well-defined binding interface containing multiple contact residues
[3]
paper
Gardella et al. describe the PTH/PTHrP receptor pharmacology including receptor domains involved in ligand binding
doi: 10.1124/pr.114.009464
openupdated 2026-06-11

Can PTHrP(1-34) also act on pancreatic cells that carry the bone receptor, helping them release insulin?

If so, patients on PTHrP-based bone drugs might also get a blood-sugar benefit. Older adults often have both conditions, so one treatment touching both would mean fewer medicines.

The hypothesis
PTHrP(1-34) activates PTH1R on pancreatic beta cells and thereby augments glucose-stimulated insulin secretion via cAMP-PKA sensitization of the secretory machinery, suggesting a repurposing potential as an adjunct treatment for type 2 diabetes independent of its bone-anabolic activity.
Why it’s plausible
PTH1R is expressed on pancreatic islet beta cells. Gs-coupled receptor agonism in beta cells (as with GLP-1R or GIP-R) potentiates insulin secretion via cAMP elevation. PTHrP is locally produced in the pancreas and islet PTH1R expression is documented. If PTHrP(1-34) engages islet PTH1R with the same high-affinity binding predicted by ipTM=0.844, it would produce glucose-dependent insulin sensitization via the same pathway exploited by incretin drugs.
Why it matters
If PTHrP(1-34) has dual bone-anabolic and insulinotropic activity through a single receptor, it could address the common comorbidity of osteoporosis and type 2 diabetes in older adults with a single peptide, and might explain why paraneoplastic PTHrP elevation occasionally presents with altered glucose metabolism.
Plausibility.55
Novelty.68
Impact.65
Basis · grounding1 paper · 2 computed/notes
[1]
structureipTM=0.844 supports high-confidence PTH1R engagement; if PTH1R is expressed on beta cells, the same binding interface would be operative
[2]
paper
PTHrP identified as a secreted factor from tumor cells with systemic endocrine actions, establishing its capacity for receptor-mediated effects in non-skeletal tissues
doi: 10.1073/pnas.84.14.5048
[3]
noteREADME notes PTHrP is a normal developmental and skeletal hormone with roles beyond hypercalcemia, opening space for non-skeletal PTH1R biology
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8442076444625854 openfold3-mlx
ranking score 0.9602436423301697 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.839global PDE — lower = better
disorder0.311! high disorder
chain pair ipTM (A, B)0.844interface 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
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
runtime847s
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-building cancer-calcium peptide: PTHrP (1-34) fragment (pep-10502, v1). PeptideModel. https://peptidemodel.com/card/pep-10502
@peptide{pep10502,
  sequence = {AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTA},
  target   = {pth1r},
  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 6 papers
discussion no comments
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peptidemodel.com CC-BY-SA-4.0 research only · not for human use