pe
pep-10504 v1 CC-BY-SA-4.0

Bone & calcium signaling peptide (PTHrP 1-37)

A natural protein fragment that activates the same bone-building receptor as parathyroid hormone, helping scientists study how the skeleton grows and how cancer can raise calcium levels; used only as a lab research tool.

statusbioassayed targetPTH1R length37 aa refs5
status 4 / 5 · 2 verified on platform
prediction metrics openfold3-mlx 0.3.1
ipTM0.837
pTM0.650
avg pLDDT46.5
ranking score0.954
STRUCTURE · PEP-10504 × PTH1R
ranking0.954
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence37 aa
1510152025303537
AVSEHQLLHDKGKSIQDLR RRFFLHHLIAEIHTAEIR
in the news 1 article
overview readme

What this is

PTHrP (1-37) is the first 37 amino acids of parathyroid hormone-related protein, a hormone that the body makes naturally. It is the part of the molecule that binds and switches on the same receptor as parathyroid hormone (PTH) — a receptor called PTH1R that sits on bone and kidney cells and controls how the skeleton is built and how calcium is handled (Gardella 2015). The sequence stored here is the human/mouse/rat form (AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIR), a research peptide used to dissect PTH/PTHrP signaling rather than a marketed drug.

What it does

PTHrP (1-37) binds PTH1R, a class B G-protein-coupled receptor that lives on osteoblasts (bone-building cells) and kidney tubule cells. Activating that receptor drives the cAMP/PKA arm of bone-remodeling signaling and, in pathology, underlies the hypercalcemia seen in cancers that secrete PTHrP (Gardella 2015; Zhao 2019). Because PTHrP (1-37) and the clinical PTH analogs share this same receptor, the 1-37 fragment is widely used in the lab as a comparator for understanding bone-active PTH1R drugs such as teriparatide and abaloparatide (Sato 2021).

Mechanism

PTH1R is a class B GPCR. Cryo-EM structural work on the active human PTH1R-Gs complex shows how the N-terminal residues of PTH-family ligands insert into the seven-transmembrane bundle to trigger Gs coupling and downstream cAMP production (Zhao 2019). PTHrP and PTH share their first ~13 residues in functional identity even though primary sequences diverge, which is why PTHrP (1-37) is competent to fully activate PTH1R the way PTH (1-34) does (Gardella 2015).

Signal duration at PTH1R is itself a regulated variable. Comparative work on three PTH1R ligands — teriparatide (PTH 1-34), abaloparatide (a PTHrP-derived analog), and long-acting PTH — found that all three initiate cAMP signaling with comparable kinetics at the receptor, but differ in how long signaling persists after ligand washout, which contributes to their different effects on bone and mineral metabolism in patients (Sato 2021). PTHrP (1-37) sits in the same pharmacological family and serves as a reference compound for that comparison.

Receptor availability at the cell surface is a second layer of control. A naturally occurring PTH1R isoform missing transmembrane domain 7 (Δe14-PTHR) is expressed in human kidney and buccal epithelial cells; it traffics poorly to the cell surface and dampens signaling by the full-length receptor (Alonso 2011). In bone, the integrin-binding adapter Kindlin-2 modulates PTH1R-driven anabolic signaling in osteoblastic cells, and its loss in mice blunts the bone-mineral-density gain normally produced by intermittent PTH stimulation (Fu 2020). These findings position PTH1R not as an on/off switch but as a node whose output depends on receptor isoform, surface expression, and accessory proteins.

Evidence

  • Human: No clinical trials of PTHrP (1-37) as a therapeutic; it is a research tool peptide. Clinical PTH1R agonists in the same pharmacological family (teriparatide, abaloparatide) are approved drugs for osteoporosis; PTHrP (1-37) is used preclinically as their comparator (Sato 2021).
  • Animal: PTH1R signaling in bone has been dissected in mouse models, including conditional deletion of Kindlin-2 in osteoblastic cells, where it blunts the bone-volume and bone-mineral-density gain from intermittent PTH stimulation (Fu 2020).
  • In vitro: Receptor pharmacology of PTHrP-family ligands at PTH1R is well characterized in heterologous expression systems, including the active-state cryo-EM structure of human PTH1R (Zhao 2019) and side-by-side kinetic comparisons of PTH1R ligands (Sato 2021).

Known effects

  • PTH1R activation / cAMP signaling — Mechanistic, in vitro (Gardella 2015; Zhao 2019)
  • Osteoblast signaling / bone anabolism (PTH/PTHrP family) — Preclinical (Fu 2020)
  • Hypercalcemia driver in PTHrP-secreting tumors (parent protein PTHrP) — Clinical biology (Gardella 2015)
  • Reference ligand for teriparatide/abaloparatide comparison — Preclinical (Sato 2021)

Regulatory status

  • US: Not a drug. PTHrP (1-37) is a research-grade peptide, not FDA-approved for any indication. PTH1R agonists in the same family that ARE approved drugs include teriparatide (PTH 1-34, approved 2002 for osteoporosis) and abaloparatide (PTHrP-derived analog, approved 2017); PTHrP (1-37) itself is not among them.
  • WADA: Not specifically listed by name.

Related peptides

  • Teriparatide (PTH 1-34) — the clinically used N-terminal PTH fragment that activates the same PTH1R; the most direct pharmacological cousin.
  • Abaloparatide — a PTHrP-derived analog approved for osteoporosis, designed from the same N-terminal PTHrP region as PTHrP (1-37) (Sato 2021).
  • Long-acting PTH (LA-PTH) — engineered PTH1R agonist used alongside PTHrP (1-37) in receptor-kinetics studies (Sato 2021).
Hypotheses3 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 PTHrP(1-37) cause bone cells to receive a different, more sustained signal from inside the cell compared to the current bone drug PTH(1-34)?

If PTHrP(1-37) drives a stronger internal signal, it could explain why natural PTHrP promotes bone growth in a subtly different way, and could inspire better bone-loss treatments that work longer with fewer daily doses.

The hypothesis
PTHrP(1-37) activates a sustained endosomal cAMP signal from PTH1R that is quantitatively greater than that produced by PTH(1-34) at equimolar concentrations, because the additional C-terminal residues slow receptor internalization by reducing beta-arrestin recruitment efficiency.
Why it’s plausible
Pioneering work established that PTH1R can continue signaling from endosomes after internalization, generating a second wave of cAMP distinct from the plasma-membrane phase. Beta-arrestin recruitment to class B GPCRs depends partly on the phosphorylation pattern induced by each individual agonist, which is itself ligand-dependent (biased agonism). PTHrP(1-37) and PTH(1-34) differ structurally beyond residue 14 (where primary sequences diverge) and at the C-terminus, meaning they may induce different receptor conformations that differentially recruit GRKs and beta-arrestins. A ligand that slows beta-arrestin engagement would remain at the plasma membrane longer, reduce the internalized fraction, and thus produce a weaker but more prolonged endosomal cAMP pool, a mechanistically distinct profile.
Why it matters
Endosomal PTH1R signaling has been linked specifically to trabecular bone anabolic effects in vivo. If PTHrP(1-37) and PTH(1-34) differ in their endosomal cAMP kinetics, the native PTHrP fragment could serve as a reference for designing endosome-biased analogs with superior bone-building and reduced systemic calcium effects.
Plausibility.55
Novelty.55
Impact.70
Basis · grounding2 papers · 1 computed/note
[1]
paper
Gardella and Vilardaga review covers PTH1R endosomal signaling and ligand-specific differences in receptor trafficking and cAMP kinetics.
doi: 10.1124/pr.114.009464
[2]
paper
Cryo-EM active-state structure shows the Gs-coupling conformation stabilized differently by PTH vs. PTHrP-derived ligands, implying different efficacies at downstream effectors including arrestins.
doi: 10.1126/science.aav7942
[3]
sequenceC-terminal divergence at positions 15-37 relative to PTH(1-34) means PTHrP(1-37) presents a distinct molecular surface to intracellular scaffolds that read receptor conformation.
openupdated 2026-06-05

Could locking part of PTHrP(1-37) into a rigid ring shape make it survive in the bloodstream long enough to be a once-weekly bone treatment?

If this works, patients with osteoporosis might switch from daily injections to weekly or monthly ones, a significant quality-of-life improvement for the large number of people who find daily self-injection burdensome.

The hypothesis
Cyclization of PTHrP(1-37) via a lactam bridge between K13 and D17, stabilizing the central alpha-helix, would produce a conformationally constrained analog with improved plasma half-life and retention of full PTH1R agonist potency, because this helix is the primary determinant of receptor activation geometry as revealed by the cryo-EM active-state structure.
Why it’s plausible
Native PTHrP(1-37) is a linear peptide vulnerable to rapid proteolytic degradation, limiting its pharmacokinetic utility. The cryo-EM structure of PTH1R bound to a PTH-derived ligand (Zhao 2019) shows that the helical segment spanning roughly residues 10-20 inserts into the TMD bundle as the activation trigger. The PTHrP sequence contains K13 and D17 at i and i+4 positions, a classic geometry for i-to-i+4 lactam bridges that lock helical peptides without disrupting side chains projecting toward the receptor interface. Abaloparatide, the second approved PTH1R agonist, already demonstrates that helix-stabilizing modifications in this region improve both potency and duration, validating the approach.
Why it matters
A cyclized PTHrP(1-37) analog with extended half-life could serve as a once-weekly or longer-acting bone anabolic agent, addressing the key limitation of current daily-injection teriparatide therapy and competing with the investigational long-acting PTH1R agonists currently in development.
Plausibility.60
Novelty.45
Impact.65
Basis · grounding2 papers · 1 computed/note
[1]
sequenceSequence AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIR places K at position 13 and D at position 17, confirming an i/i+4 pair suitable for lactam bridge cyclization without disrupting the receptor-facing residues.
[2]
paper
Cryo-EM active PTH1R complex shows residues 10-20 of the bound ligand forming the helix that inserts into the TMD bundle, making this region the primary activation pharmacophore.
doi: 10.1126/science.aav7942
[3]
paper
Review discusses abaloparatide's helix-stabilized design as a proof of concept that conformational constraint in the PTHrP mid-region improves pharmacology without sacrificing PTH1R potency.
doi: 10.1124/pr.114.009464
openupdated 2026-06-05

Do the three extra amino acids at the end of PTHrP(1-37), compared to existing bone drugs, cause the receptor to stay switched on for a different amount of time?

If true, it could explain why natural PTHrP has different effects on bone than synthetic drugs, and might guide the design of next-generation bone-building medicines with fewer calcium-related side effects.

The hypothesis
The C-terminal extension of PTHrP(1-37) beyond residue 34 (residues 35-37: EIR) forms a transient contact with the extracellular domain of PTH1R that slows dissociation rate relative to PTH(1-34), producing a kinetically distinct receptor occupancy profile despite similar peak cAMP output.
Why it’s plausible
PTH(1-34) is the clinical comparator and truncates at residue 34. PTHrP(1-37) carries three additional residues (E35-I36-R37). The high ipTM of 0.8368 indicates a confident complex prediction, while the low pLDDT of 46.5 flags the C-terminal tail as disordered in isolation. Disorder-to-order transitions upon receptor engagement are a known feature of class B GPCR ligands, where the ECD clamp can stabilize otherwise floppy C-terminal extensions (Zhao 2019). If E35-I36-R37 makes even transient ECD contacts, it would alter koff without necessarily changing Emax, a distinction invisible to endpoint cAMP assays but relevant to duration of bone-anabolic signaling.
Why it matters
Residence time on PTH1R is a critical pharmacological variable: abaloparatide was optimized partly for faster dissociation to reduce hypercalcemia risk, while long-acting PTH1R agonists are being developed for hypoparathyroidism. Establishing that the native 37-aa PTHrP form has a distinct kinetic fingerprint from PTH(1-34) would reframe PTHrP(1-37) as a kinetic template rather than a mere truncation variant.
Plausibility.55
Novelty.50
Impact.60
Basis · grounding2 papers · 2 computed/notes
[1]
paper
Cryo-EM of PTH1R-Gs complex shows N-terminal ligand residues insert into TMD bundle; ECD clamps the mid-region, implying C-terminal extensions contact the ECD hinge region.
doi: 10.1126/science.aav7942
[2]
paper
Gardella review details how ligand residence time on PTH1R influences downstream cAMP kinetics and physiological outcome.
doi: 10.1124/pr.114.009464
[3]
sequenceSequence AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIR confirms residues 35-37 are EIR, adding a charged glutamate and basic arginine beyond the PTH(1-34) pharmacophore boundary.
[4]
structureipTM=0.84 supports a real complex pose; pLDDT=46.5 flags the C-terminal region as locally disordered, consistent with a conditional-folding tail.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8368420004844666 openfold3-mlx
ranking score 0.9542047381401062 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.821global PDE — lower = better
disorder0.310! high disorder
chain pair ipTM (A, B)0.837interface 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
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
runtime868s
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 & calcium signaling peptide (PTHrP 1-37) (pep-10504, v1). PeptideModel. https://peptidemodel.com/card/pep-10504
@peptide{pep10504,
  sequence = {AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTAEIR},
  target   = {pth1r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {bioassayed}
}
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 5 papers
discussion no comments
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peptidemodel.com CC-BY-SA-4.0 research only · not for human use