pe
pep-10781 v1 CC-BY-SA-4.0

Parathyroid hormone fragment that blocks its own receptor (PTH 13: 34)

A lab-made piece of parathyroid hormone, the calcium-regulating hormone, that latches onto its receptor without switching it on, blocking the hormone's normal effect; used only as a lab research tool.

statusbioassayed targetPTH1R length22 aa refs7
status 4 / 5 · 2 verified on platform
prediction metrics boltz-2 2.2.1
ipTM0.727
pTM0.716
avg pLDDT56.1
ranking score0.594
STRUCTURE · PEP-10781 × PTH1R
ranking0.594
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 2.2.1 · mmCIF ↓ download
sequence22 aa
1510152022
KHLNSMERVEW LRKKLQDVHNF
in the news 1 article
overview readme

What this is

PTH (13–34) is a 22-amino-acid fragment of parathyroid hormone — the hormone the parathyroid glands release to keep blood calcium in range. It is the back half of the active 1–34 form: the part that grips the receptor, with the front piece (residues 1–12) that switches the receptor on cut away. Because of that, PTH (13–34) can attach to the PTH1R receptor without triggering a normal hormonal response, and it has been used in laboratory research as a tool to study how PTH and its receptor interact. Its stored sequence is KHLNSMERVEWLRKKLQDVHNF.

History

The two-domain "address–message" view of parathyroid hormone — with the N-terminal residues providing receptor activation and the more C-terminal residues providing the principal binding affinity — has organized PTH structure-activity work for decades and is the basis for splitting the 1–34 sequence into 1–14 / 13–34 style fragments for mechanism studies. The Gardella and colleagues IUPHAR review (Pharmacological Reviews, 2015) summarizes this lineage of work on the parathyroid hormone receptors. The same logic underlies the design of the clinical agonist teriparatide (PTH 1–34), which keeps both halves intact.

What it does

Full-length PTH and the clinically used 1–34 fragment both activate PTH1R, a Class B G-protein-coupled receptor that controls calcium and phosphate handling in bone and kidney (Lee and colleagues, Current Opinion in Nephrology and Hypertension, 2009). PTH (13–34) keeps the receptor-binding half but loses the residues that drive activation, so in cell-based assays it occupies PTH1R without firing the canonical Gαs–cAMP cascade the way intact PTH does. That is the basis for the platform subtitle describing it as a competitive PTH1R fragment — a research tool rather than a therapeutic agonist.

Mechanism

PTH1R is a Class B GPCR with a two-site binding mode: an extracellular N-terminal domain that captures the C-terminal portion of the ligand, and a juxtamembrane region (the seven-helix bundle plus extracellular loops) that the N-terminal residues of the ligand engage to trigger activation. Dean and colleagues (Molecular Endocrinology, 2006) dissected this experimentally using a modified PTH(1–15) radioligand that bound essentially only to the juxtamembrane portion of PTHR, while 125I-PTH(1–34) bound both the N-terminal extracellular domain and the juxtamembrane region — direct evidence that the two halves of PTH 1–34 engage different parts of the receptor. PTH (13–34) is the complementary half: it carries the residues that dock into the extracellular domain but lacks the 1–12 segment that engages the juxtamembrane region to drive Gαs coupling.

Cryo-EM work by Zhao and colleagues (Science, 2019) resolved the active human PTH1R bound to a modified parathyroid hormone and stimulatory G protein, visualizing how the ligand sits across the two binding sites and how activation proceeds. Reviews by Sutkeviciute and colleagues (Trends in Endocrinology & Metabolism, 2019) and Kim and colleagues (Experimental & Molecular Medicine, 2025) place PTH1R within the broader Class B GPCR family and discuss the allosteric coupling and ligand-recognition principles that PTH-fragment studies, including 13–34, have helped establish.

Evidence

  • Human: No human clinical trials of PTH (13–34) itself were located in the dossier; the fragment is used in research, while the clinical PTH analogs at PTH1R are the full 1–34 forms teriparatide and abaloparatide (Sato and colleagues, JBMR Plus, 2021).
  • Animal / cellular: Radioligand binding studies in cell systems expressing PTHR have used PTH-fragment analogs to map the two-site binding mode of the receptor (Dean and colleagues, 2006). Structural studies on active PTH1R provide the molecular framework these binding studies are interpreted against (Zhao and colleagues, Science, 2019).
  • In vitro / structural: Reviews of PTH1R signaling, allostery, and structure (Sutkeviciute and colleagues, 2019; Gardella and colleagues, 2015; Kim and colleagues, 2025) summarize how N-terminal-truncated PTH fragments behave at the receptor.

Known effects

  • Receptor binding without canonical activation — Based on the two-site PTH1R binding model, PTH fragments lacking the 1–12 activation residues are expected to engage the receptor's extracellular domain but not drive Gαs signaling the way intact PTH 1–34 does (Dean and colleagues, 2006; Gardella and colleagues, 2015).
  • Research-tool use at PTH1R — Used in mechanism studies of how ligand halves contribute to PTH1R engagement (Dean and colleagues, 2006).

Regulatory status

PTH (13–34) is a research fragment, not an approved drug. The approved PTH-pathway agents acting at PTH1R are the full 1–34 forms — teriparatide (recombinant human PTH 1–34) and abaloparatide (a PTHrP-based analog) — both used in osteoporosis (Sato and colleagues, JBMR Plus, 2021). No regulatory approvals, scheduling entries, or WADA listings specific to PTH (13–34) were identified in the dossier.

Related peptides

  • Teriparatide (PTH 1–34) — the clinically used full PTH 1–34 fragment; keeps both the activation half (1–12) and the binding half (13–34) and so acts as a PTH1R agonist (Sato and colleagues, 2021).
  • Abaloparatide — a PTHrP-derived analog also acting at PTH1R, used for osteoporosis (Sato and colleagues, 2021).
  • Long-acting PTH (LA-PTH) — a modified PTH/PTHrP hybrid used in mechanistic comparisons of PTH1R ligands (Sato and colleagues, 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

Does this peptide work by locking the PTH1R receptor into a specific inactive shape, rather than just sitting in the way of the natural hormone?

If true, it could point toward smarter drugs for hypercalcemia or excessive bone loss that dial the receptor down without fully silencing it, potentially with fewer side effects than complete blockade. Patients with conditions like hyperparathyroidism could benefit from this more nuanced approach.

The hypothesis
PTH(13-34) binds PTH1R in a receptor conformation distinct from that stabilized by full agonists, favoring the R0 ground state over the RG (G-protein-coupled) state, and this conformation-selective occupancy is responsible for its competitive antagonism rather than simple steric blockade.
Why it’s plausible
Class B GPCRs including PTH1R exist in distinct conformational pools (R0, RG, and intermediate states). The literature snippet from 10.1210/me.2005-0349 explicitly notes that binding of a truncated N-terminal PTH fragment to PTH1R is highly sensitive to GTP-gamma-S (indicating RG-state preference), whereas PTH(1-34) binding is not. PTH(13-34) lacks the N-terminal activation domain (residues 1-12) that drives receptor into the RG state, so it is expected to preferentially stabilize R0. An ipTM of 0.73 from Boltz-2 is moderate-good for a Class B GPCR peptide complex, consistent with genuine binding but without the full engagement that flips the receptor on. If PTH(13-34) is a conformation-selective binder rather than a pure competitive blocker, it would suppress tonic PTH1R signaling without fully displacing endogenous ligand.
Why it matters
Conformation-selective antagonism at PTH1R could offer a pharmacological handle to dampen pathological bone resorption or hypercalcemia while preserving partial receptor tone, a more nuanced effect than full blockade.
Plausibility.70
Novelty.40
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
paper
GTP-gamma-S sensitivity distinguishes N-terminal PTH fragment binding (RG-state) from PTH(1-34) binding (not state-sensitive), implying the C-terminal binding domain does not drive RG-state stabilization.
doi: 10.1210/me.2005-0349
[2]
structureBoltz-2 complex ipTM=0.73, pLDDT=56.1: moderate confidence in the bound pose, consistent with a real but partial engagement that does not fully activate the receptor.
[3]
notePTH(13-34) retains the receptor-binding ('address') domain but lacks the activation ('message') domain (residues 1-12), the mechanistic basis for antagonism.
openupdated 2026-06-05

Could blocking PTH1R with this peptide reduce the damage that cancer cells do when they invade bones?

Bone metastases cause severe pain and fractures in breast and prostate cancer patients, and current treatments slow but rarely stop the damage. A peptide that blocks a key receptor in bone cells could offer a new tool to help keep those metastases in check, potentially used alongside existing bone-protective drugs.

The hypothesis
PTH(13-34) could suppress pathological PTH1R signaling in cancer-driven bone metastasis independent of its calcium-lowering effect, because PTH1R activation in osteoblasts and tumor-resident stromal cells promotes pro-tumoral bone remodeling and RANKL upregulation, and competitive occupancy of PTH1R by the fragment would blunt this axis.
Why it’s plausible
PTH1R is expressed in bone stromal cells and some cancer cell lines, and PTH1R activation promotes RANKL expression, osteoclast activation, and a permissive niche for bone metastasis. The annotated target PTH1R is highly expressed in osteoblasts and in several cancer types (breast, prostate) that commonly metastasize to bone. A selective PTH1R antagonist occupying the receptor would reduce RANKL-driven osteoclastogenesis in the metastatic niche by a mechanism distinct from bisphosphonates or RANKL antibodies (which act downstream). The fragment's competitive binding at PTH1R (established in its functional description) makes this mechanistically plausible.
Why it matters
If PTH(13-34) or a stabilized analog can reduce osteolytic lesion formation in bone metastasis by blocking stromal PTH1R, it would represent a molecularly targeted approach complementary to existing anti-resorptive agents, potentially slowing the vicious cycle of tumor-driven bone destruction.
Plausibility.50
Novelty.50
Impact.70
Basis · grounding1 paper · 2 computed/notes
[1]
notePTH(13-34) occupies PTH1R as a competitive antagonist without triggering normal hormonal response, established in cell-based assays.
[2]
paper
PTH1R controls bone remodeling via osteoblasts in bone and kidney; overactivation of this receptor in bone-metastatic cancer contexts promotes osteolytic signaling.
doi: 10.1097/mnh.0b013e32832c2264
[3]
sequenceFragment retains the C-terminal binding pharmacophore (WLRK cluster at positions 9-12) sufficient for PTH1R occupancy, making it structurally capable of antagonism in osteoblast and stromal contexts.
openupdated 2026-06-05

Could attaching a small polymer handle to the free end of PTH(13-34) keep it active in the body long enough to be a practical medicine?

If this works, it could open a new class of treatment for dangerously high calcium levels in cancer patients or people with overactive parathyroid glands, conditions that currently have very limited drug options. A weekly injection rather than continuous infusion would be far more practical for patients.

The hypothesis
Replacing the N-terminal lysine (K1 of the fragment, K13 of native PTH) with a bulky non-natural amino acid or PEG handle would convert PTH(13-34) from a short-acting competitive antagonist into a long-acting receptor occupier suitable for once-weekly dosing in hypercalcemic conditions, without disrupting the C-terminal binding pharmacophore centered on W9, L10, R11.
Why it’s plausible
The N-terminus of PTH(13-34) (K13 of native PTH) is spatially proximal to the receptor entrance domain but is not the primary pharmacophore: the core binding contacts are attributed to residues 20-34 of native PTH, corresponding roughly to positions 8-22 of the fragment, which include the W-L-R-K cluster. N-terminal modification therefore carries lower risk of disrupting affinity. Adding a PEG or fatty acid at K1 would extend plasma half-life (currently very short for a 22-mer) via albumin association, a strategy validated for GLP-1 analogs and PTH(1-34) depot formulations. This is an engineering opportunity that is feasible but has not been applied to the antagonist fragment.
Why it matters
A long-acting PTH1R antagonist could address unmet clinical need in primary hyperparathyroidism or humoral hypercalcemia of malignancy where current management is largely surgical or limited to calcimimetics targeting the calcium-sensing receptor rather than PTH1R directly.
Plausibility.55
Novelty.40
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceK at position 1 of fragment (K13 native PTH) provides an accessible amine handle for N-terminal modification without disrupting the proposed W9-L10-R11-K12 binding core.
[2]
notePTH(13-34) is used as a research tool antagonist; no clinical or long-acting form is described, indicating an unoccupied engineering opportunity.
[3]
paper
PTH1R governs bone and kidney calcium handling; a durable antagonist would be clinically relevant for hypercalcemic states.
doi: 10.1097/mnh.0b013e32832c2264
openupdated 2026-06-05

Does PTH(13-34) block only the PTH1 receptor and not the closely related PTH2 receptor?

If this peptide truly ignores PTH2R, researchers could use it to study bone and kidney calcium problems with much less noise from other receptor pathways. That cleaner picture could accelerate the development of targeted treatments for osteoporosis or kidney-related calcium imbalances.

The hypothesis
PTH(13-34) binds PTH2R with measurably lower affinity than PTH1R because the mid-fragment residues W(9)L(10)R(11)K(12) in the peptide (positions 21-24 of native PTH) contribute receptor-subtype selectivity contacts that differ between PTH1R and PTH2R, making PTH(13-34) a PTH1R-selective antagonist tool.
Why it’s plausible
PTH1R and PTH2R share the same receptor class but differ substantially in their extracellular domain and transmembrane bundle residues that contact the C-terminal binding domain of PTH. The sequence KHLNSMERVEWLRKKLQDVHNF contains the tryptophan at position 9 of the fragment (W23 in native PTH numbering), a residue documented in structure-activity studies as critical for PTH1R but less so for PTH2R selectivity. If the fragment preferentially engages PTH1R, it is a selective pharmacological tool for dissecting PTH1R-specific calcium and bone biology in tissues where both receptors are co-expressed.
Why it matters
Confirming PTH1R selectivity of this fragment over PTH2R would validate it as a clean probe for PTH1R-specific pathways in bone remodeling and renal calcium handling without confounding PTH2R-mediated effects in the CNS or pancreas.
Plausibility.55
Novelty.30
Impact.50
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceFragment KHLNSMERVEWLRKKLQDVHNF contains W at position 9 (W23 of native PTH), a residue important for PTH1R engagement in structure-activity studies; PTH2R is less sensitive to this position.
[2]
notePTH(13-34) is described as a PTH1R-targeting antagonist tool, with the annotated target being solely PTH1R, implying selectivity over PTH2R.
[3]
paper
PTH1R controls calcium and phosphate handling in bone and kidney; PTH2R distribution and pharmacology are distinct, making selectivity consequential for experimental interpretation.
doi: 10.1097/mnh.0b013e32832c2264
openupdated 2026-06-05

Is most of the receptor-binding power of PTH(13-34) concentrated in just a small cluster of its amino acids?

If only a tiny part of the peptide is doing the real binding work, chemists could build a much smaller, simpler molecule that mimics the same effect. Smaller molecules are generally easier to manufacture, more stable, and potentially easier to take as a medicine rather than an injection.

The hypothesis
The W(9)-L(10)-R(11) triad within the PTH(13-34) sequence (corresponding to W23-L24-R25 of native PTH) forms the minimal hydrophobic-cationic pharmacophore required for PTH1R binding, and the surrounding residues K(1)-H(2)-L(3) and Q(16)-D(17)-V(18)-H(19)-N(20)-F(22) function as conformational scaffolding that orients this triad without contributing direct receptor contacts.
Why it’s plausible
Structure-activity analyses of PTH C-terminal domains have repeatedly pointed to the region around W23 and the basic residues flanking it as the affinity anchor. The sequence KHLNSMERVEWLRKKLQDVHNF places W at position 9, flanked by E(8) and L(10)R(11)K(12), a pattern consistent with an amphipathic face where the aromatic and basic residues project toward the receptor and the polar/small residues (S5, M6, N4) face solvent. The moderate ipTM of 0.73 suggests a defined but not rigidly constrained binding interface, consistent with a small pharmacophore core embedded in a more flexible scaffold. If the W-L-R triad is the minimal pharmacophore, truncated peptidomimetics limited to this triad plus minimal flanking residues could retain antagonist activity at a fraction of the molecular weight.
Why it matters
Identifying a minimal pharmacophore would enable design of small peptidomimetics or macrocycles that mimic PTH(13-34) antagonism at PTH1R with better oral bioavailability prospects and reduced immunogenicity compared to the 22-mer.
Plausibility.55
Novelty.30
Impact.50
Basis · grounding3 computed/notes
[1]
sequenceSequence KHLNSMERVEWLRKKLQDVHNF: W at position 9, flanked by E(8) and L(10)R(11)K(12) forms a potential amphipathic pharmacophore face when modeled as a helix.
[2]
structureBoltz-2 ipTM=0.73 indicates a real binding interface; the moderate (not high) confidence may reflect the pharmacophore being confined to a sub-region of the full 22-mer.
[3]
noteThe 'address-message' framework described in the readme defines residues 13-34 as the binding domain, implying internal sub-structure within this domain for affinity.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.72678142786026 boltz-2
ranking score 0.5942230820655823 boltz-2
3-letter notation
Lys-His-Leu-Asn-Ser-Met-Glu-Arg-Val-Glu-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Asn-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). Parathyroid hormone fragment that blocks its own receptor (PTH 13: 34) (pep-10781, v1). PeptideModel. https://peptidemodel.com/card/pep-10781
@peptide{pep10781,
  sequence = {KHLNSMERVEWLRKKLQDVHNF},
  target   = {pth1r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {bioassayed}
}
related peptides 5 by signal overlap
clinical trials 2066 on ct.gov · 191 on EUCTR · checked 2026-05-22
ct.gov trials ? 2066
with results 344
EUCTR 191
by phase
1phase 11phase 21phase 32phase 45no phase
by status
4completed3recruiting1terminated1withdrawn1unknown
references 7 papers
discussion no comments
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