pe
pep-10508 v1 CC-BY-SA-4.0

Rat parathyroid hormone fragment: lab version of Forteo (PTH 1-34)

The rat form of a natural bone-regulating hormone fragment, used in rodent studies of how bone cells build and remodel bone. Research tool only, the human version (Forteo) is FDA-approved for osteoporosis.

statussynthesized targetPTH1R length34 aa refs9
status 4 / 5
prediction metrics openfold3-mlx 0.3.1
ipTM0.867
pTM0.660
avg pLDDT47.7
ranking score0.994
STRUCTURE · PEP-10508 × PTH1R
ranking0.994
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence34 aa
15101520253034
AVSEIQLMHNLGKHLAS VERMQWLRKKLQDVHNF
in the news 1 article
overview readme

What this is

Parathyroid hormone fragment (1-34), or PTH(1-34), is the biologically active N-terminal piece of the 84-amino-acid parathyroid hormone — the calcium-regulating hormone secreted by the four small parathyroid glands in the neck. This card covers the rat form of the fragment, whose 34-residue sequence differs from the human version at five positions, making it the species-matched reagent used in rodent bone-biology research. The human equivalent — sold as Forteo and, in biosimilar form, as Bonsity — was FDA-approved in November 2002 as the first anabolic (bone-building) treatment for osteoporosis. PTH(1-34) acts on the PTH type-1 receptor (PTH1R), a class B G-protein-coupled receptor present on osteoblasts and kidney tubule cells, and its effects on bone depend critically on whether it is delivered as brief daily pulses or as a continuous signal.

History

Parathyroid hormone was first isolated in 1925 by James Collip, who used crude glandular extracts to reverse the life-threatening muscle spasms (tetany) that follow parathyroid removal. The polypeptide structure was defined by Rasmussen and Craig in the early 1960s. The amino-terminal 34-residue sequence of human PTH was determined by Potts, Niall, and colleagues at Massachusetts General Hospital — the 1972 proposal was later refined, with the sequence published in PNAS (1972) becoming the basis for synthetic work. By the mid-1970s, largely through the efforts of British pharmacologist John Parsons, researchers had established that single daily injections of PTH(1-34) dramatically increased bone mass in several mammalian species — a key observation that reversed decades of focus on PTH's calcium-mobilizing (resorptive) actions and identified it as a potential bone-building drug (Marcus 2011). The rat form of PTH(1-34) is distinguished from the human form by five amino acid substitutions; it shows 8–10-fold greater potency than human PTH(1-34) in canine and rat adenylate cyclase systems, and is therefore the preferred ligand in rodent experimental models. The 1998 paper by Gray and colleagues used the rat sequence to demonstrate that PTH(1-34) suppresses appositional bone formation in cultured rat cranial osteoblasts — an important model result for understanding the context-dependent anabolic and anti-anabolic actions of the fragment (Gray et al. 1998).

What it does

PTH(1-34) tells bone-building cells (osteoblasts) to become more active and to survive longer, ultimately increasing bone mass and improving bone architecture. Crucially, this anabolic action only emerges with intermittent, short-duration receptor activation — the kind produced by a once-daily injection. When PTH(1-34) is present continuously (as in primary hyperparathyroidism, or with sustained drug infusion), the net effect flips: bone-resorbing osteoclasts are upregulated more than osteoblasts, leading to net bone loss. This dose-timing paradox has made understanding PTH(1-34) signaling a central preoccupation of bone biology. In the kidney, PTH(1-34) increases tubular reabsorption of calcium and promotes conversion of vitamin D to its active form, supporting overall calcium homeostasis (Lee et al. 2009).

Evidence

  • Human: The pivotal Fracture Prevention Trial (Neer et al., NEJM 2001) enrolled 1,637 postmenopausal women with prior vertebral fractures and showed that the 20 µg daily dose of human PTH(1-34) reduced the risk of new vertebral fractures by 65% and non-vertebral fractures by 53% over 18 months compared with placebo, with lumbar spine bone mineral density increasing by approximately 9%. A separate randomized Japanese trial (TOWER) confirmed vertebral fracture reduction in a weekly-dosing regimen. Multiple systematic reviews have since confirmed the anti-fracture efficacy across male and postmenopausal female osteoporosis populations.
  • Animal: Appositional bone formation in rat cranial osteoblast cultures is suppressed by PTH(1-34) at pharmacologically relevant concentrations (Gray et al. 1998). Rodent ovariectomy models have extensively validated intermittent PTH(1-34) as a bone-anabolic agent, with numerous studies showing increased trabecular bone volume and bone mineral density; these models used the rat sequence at matched doses.
  • In vitro: PTH(1-34) is a full agonist at PTH1R in osteoblast-lineage cell lines, stimulating cAMP accumulation via Gαs coupling. Differential signaling through β-arrestin and G-protein pathways has been characterized in cell-based assays (Gesty-Palmer et al. 2009; Sutkeviciute et al. 2019).

Known effects

  • Vertebral and non-vertebral fracture reduction — Phase III evidence (human PTH 1-34, Neer 2001)
  • Increased bone mineral density (spine, hip) — Phase III and multiple RCTs
  • Stimulation of osteoblast differentiation and survival — Preclinical, mechanistic
  • Suppression of appositional bone formation at high/continuous exposures — Preclinical (rat cranial osteoblast model, Gray et al. 1998)
  • Calcium reabsorption in kidney — Mechanistic, supported by clinical observations

Safety signals

Transient hypercalcemia occurs in approximately 11% of patients receiving the 20 µg human dose, peaking at 4–6 hours after injection and resolving within 16–24 hours. Mild nausea, headache, dizziness, and limb pain were reported in the Fracture Prevention Trial. The original FDA approval for Forteo in 2002 carried a boxed warning about osteosarcoma based on rat carcinogenicity studies in which high-dose teriparatide caused dose- and duration-dependent bone tumors; however, a 15-year FDA-mandated post-marketing surveillance study covering approximately 2.47 million teriparatide-treated patients found no increase in osteosarcoma incidence above background population rates (Krege et al. 2022). The FDA removed the boxed warning and the 2-year cumulative lifetime use restriction in November 2020. Rat bones grow throughout life (unlike human bones), which likely explains the species-specific carcinogenicity signal.

Regulatory status

  • US: The human PTH(1-34) drug teriparatide (Forteo, Eli Lilly; Bonsity biosimilar, Alvogen) is FDA-approved as a prescription anabolic agent for osteoporosis. The original 2-year lifetime treatment limit was lifted in November 2020.
  • EU: Teriparatide (Forsteo) received EMA approval in June 2003; biosimilar versions (Terrosa, Movymia) are also approved.
  • Research use: The rat PTH(1-34) fragment on this card (AVSEIQLMHNLGKHLASVERMQWLRKKLQDVHNF) is a research reagent used in rodent bone-biology experiments; it is not a clinical drug and is not separately regulated as a pharmaceutical.
  • WADA: PTH and its fragments are listed under the WADA Prohibited List (S2, peptide hormones and related substances).

Mechanism

PTH(1-34) binds the extracellular domain of PTH1R, a class B (secretin-family) GPCR whose principal endogenous ligands are full-length PTH (1-84) and the related peptide PTHrP. Receptor engagement initiates Gαs-mediated activation of adenylyl cyclase, generating cAMP and activating protein kinase A (PKA); this PKA signal is the primary driver of the anabolic response in osteoblasts. PTH1R also signals through Gαq/11 (IP3/Ca²⁺) and, via β-arrestin recruitment, through G-protein-independent endosomal pathways. A biased agonist study showed that β-arrestin-selective PTH1R activation can stimulate bone formation independently of G-protein signaling, suggesting the two arms of the receptor's output can be pharmacologically separated (Gesty-Palmer et al. 2009).

PTH1R exists in at least two conformational states — a G-protein–coupled RG state and a G-protein–uncoupled R0 state. Teriparatide (human PTH 1-34) binds preferentially to the R0 conformation, producing a prolonged cAMP signal that persists from endosomes after receptor internalization. Abaloparatide, a PTHrP-based analog, binds the RG conformation more selectively, generating a more transient signal that results in less accompanying bone resorption and hypercalcemia (Hattersley et al. 2016; Sutkeviciute et al. 2019). The rat PTH(1-34) fragment shares the same receptor-activation mechanism but differs at five residues, yielding approximately 8–10-fold higher potency in rodent adenylate cyclase assays compared with the human peptide.

The CaSR (calcium-sensing receptor) modulates PTH1R signaling in skeletal development: CaSR-null models display dysregulated PTH1R activity, underlining an interplay between the two receptor systems in coordinating bone formation and calcium homeostasis (Santa Maria et al. 2016).

Related peptides

  • Teriparatide (human PTH 1-34) — the human-sequence version of this fragment; the approved drug form. See /card/pep-10509 if available, or search "teriparatide" on the platform.
  • Abaloparatide — a PTHrP(1-34) analog that preferentially engages the RG conformation of PTH1R, showing reduced hypercalcemia relative to teriparatide; reviewed in Brent (2021) and Leder (2017).
  • Full-length PTH (1-84) — the intact hormone; the (1-34) fragment retains full receptor-activation capacity because residues 1–34 carry both the receptor-binding and the activation domains.
  • PTHrP (1-36) — parathyroid hormone-related protein, the other endogenous PTH1R ligand; shares the (1-34) binding pharmacophore with structural divergence at the C-terminal end; basis for abaloparatide design.
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 rat version of this peptide trigger a different mix of bone-building versus bone-breakdown signals than the human drug Forteo?

If true, it would explain why bone treatments that look powerful in rats sometimes disappoint in human trials, and could help researchers pick a better lab model for testing future osteoporosis drugs. Patients waiting for the next generation of bone therapies could benefit from faster, more accurate preclinical screening.

The hypothesis
The rat PTH(1-34) sequence, which differs from human PTH(1-34) at five positions, produces a distinct beta-arrestin2 recruitment profile at PTH1R compared to the human sequence, such that the anabolic-to-catabolic ratio of bone remodeling differs between species at equivalent molar doses.
Why it’s plausible
Beta-arrestin2 knockout mice display elevated bone resorption markers at baseline (DPD: 37.56 vs 30.78 nM in WT), indicating that beta-arrestin2 signaling normally suppresses osteoclast activity downstream of PTH1R. The five substitutions between rat and human PTH(1-34) are not conservative at every position and could alter the receptor's intracellular conformation upon binding, shifting the balance between G-protein (cAMP/PKA, anabolic) and beta-arrestin (desensitization/catabolic) pathway engagement. If rat PTH(1-34) biases PTH1R toward less beta-arrestin2 recruitment, rodent bone studies using the rat sequence would systematically overestimate anabolic effect relative to what human teriparatide achieves clinically.
Why it matters
This would mean that rat-sequence PTH(1-34) is a biased agonist relative to the human fragment at PTH1R, and that cross-species extrapolation of bone-anabolic potency requires explicit beta-arrestin2 pathway correction. It would also reframe why rodent preclinical data for PTH analogs routinely show larger anabolic windows than human clinical outcomes.
Plausibility.70
Novelty.55
Impact.70
Basis · grounding1 paper · 2 computed/notes
[1]
paper
Beta-arrestin2 knockout mice show significantly higher urine DPD (bone resorption marker) vs WT, establishing that beta-arrestin2 normally limits resorption downstream of PTH1R signaling.
doi: 10.1126/scitranslmed.3000071
[2]
sequenceRat PTH(1-34): AVSEIQLMHNLGKHLASVERMQWLRKKLQDVHNF. Five positions differ from human hPTH(1-34) (SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF by canonical reference), including residues in the receptor-binding helix region (positions 3, 18, 22) that are known determinants of PTH1R signaling selectivity.
[3]
structureopenfold3 ipTM=0.867 for the rat peptide-PTH1R complex, indicating confident docking to PTH1R, but the pLDDT=47.7 of the peptide itself reflects intrinsic disorder consistent with a fold-on-binding mechanism where small sequence changes can meaningfully shift receptor conformation.
openupdated 2026-06-05

If a protein called beta-arrestin2 is what flips the bone-building drug into a bone-destroying one during continuous exposure, could blocking that protein make a slow-release patch or implant safe?

Forteo currently requires daily injections for up to two years, limiting patient compliance. If this mechanism holds, a slow-release implant delivering PTH continuously could become safe, meaning osteoporosis patients could receive months of treatment from a single procedure instead of hundreds of self-injections.

The hypothesis
Continuous low-dose infusion of rat PTH(1-34) in rodents exerts a bone-catabolic rather than anabolic effect specifically through a beta-arrestin2-dependent pathway, such that beta-arrestin2 knockout rescues the catabolic phenotype of continuous PTH exposure and restores net anabolic signaling even under infusion conditions.
Why it’s plausible
The pulse-versus-infusion dichotomy of PTH(1-34) is well established: intermittent dosing is anabolic, continuous exposure is catabolic. Beta-arrestin2 knockout mice already show elevated bone resorption at baseline, but paradoxically, if PTH-driven beta-arrestin2 recruitment is what mediates the catabolic switch during continuous PTH exposure (by internalizing and desensitizing the receptor on osteoblasts while leaving osteoclast-activating RANKL signaling intact), then beta-arrestin2 loss should partially uncouple the catabolic response to continuous PTH. This would reframe the pulse-infusion switch not as a simple cAMP kinetics phenomenon but as a beta-arrestin2-gated pathway decision at PTH1R.
Why it matters
If confirmed, beta-arrestin2 itself becomes a drug target to convert continuous PTH exposure from catabolic to anabolic, potentially enabling implantable slow-release PTH formulations (which are far more patient-friendly than daily injections) without bone loss. This is directly relevant to the clinical limitation of Forteo requiring daily self-injection.
Plausibility.50
Novelty.60
Impact.75
Basis · grounding1 paper · 2 computed/notes
[1]
paper
Beta-arrestin2 knockout mice show elevated urine DPD (resorption marker) vs WT at baseline (37.56 vs 30.78 nM, p=0.038), establishing that beta-arrestin2 normally restrains bone resorption in the PTH1R signaling context.
doi: 10.1126/scitranslmed.3000071
[2]
noteEffects on bone depend critically on whether PTH(1-34) is delivered as brief daily pulses or as a continuous signal, explicitly framing the pulse-infusion switch as the central therapeutic variable for this peptide.
[3]
sequenceRat PTH(1-34) AVSEIQLMHNLGKHLASVERMQWLRKKLQDVHNF is the species-matched form for rodent experiments, making it the appropriate peptide for testing this hypothesis in beta-arrestin2 knockout mouse models already available in the field.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8666156530380249 openfold3-mlx
ranking score 0.9935994148254395 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.823global PDE — lower = better
disorder0.337! high disorder
chain pair ipTM (A, B)0.867interface quality
3-letter notation
Ala-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn-Leu-Gly-Lys-His-Leu-Ala-Ser-Val-Glu-Arg-Met-Gln-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Asn-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
runtime755s
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). Rat parathyroid hormone fragment: lab version of Forteo (PTH 1-34) (pep-10508, v1). PeptideModel. https://peptidemodel.com/card/pep-10508
@peptide{pep10508,
  sequence = {AVSEIQLMHNLGKHLASVERMQWLRKKLQDVHNF},
  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 9 papers
[3] supporting
[6]
PTH/PTHrP Receptor Signaling, Allostery, and Structures
Sutkeviciute, I. et al. Trends in Endocrinology & Metabolism 2019
supporting
[7] supporting
[9]
Parathyroid hormone signaling in bone and kidney
Lee, M. et al. Current Opinion in Nephrology and Hypertension 2009
supporting
discussion no comments
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peptidemodel.com CC-BY-SA-4.0 research only · not for human use