pe
pep-10619 v1 CC-BY-SA-4.0

Kisspeptin-13: natural fragment that triggers the reproductive hormone system

A short piece of kisspeptin, the body's master signal for puberty and fertility; activates the brain's hormone-release cycle. Used mainly as a lab research tool.

statussynthesized targetKISS1R length13 aa refs14
status 4 / 5
prediction metrics boltz-2 2.2.1
ipTM0.913
pTM0.806
avg pLDDT70.3
ranking score0.745
STRUCTURE · PEP-10619 × KISS1R
ranking0.745
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 2.2.1 · mmCIF ↓ download
sequence13 aa
151013
LPNYNWNSFGLRF
overview readme

What this is

Kisspeptin-13 (Kp-13) is a 13-amino-acid fragment of kisspeptin, a naturally occurring signaling peptide that acts as the master switch for the human reproductive hormone system. The body produces several kisspeptin isoforms — all cleaved from the same 54-residue precursor — and Kp-13 is the second-shortest of them, consisting of the C-terminal 13 residues (LPNYNWNSFGLRF). Like the better-studied Kp-10 and Kp-54 isoforms, Kp-13 binds the kisspeptin receptor KISS1R (formerly called GPR54) and can trigger the hormonal cascade that drives reproduction (Kirby and colleagues, Pharmacological Reviews 2010). Kisspeptin itself was first identified as a cancer metastasis-suppressor gene (KISS1) before its central reproductive role was recognized — the nomenclature and early history of these peptides are reviewed in Gottsch and colleagues (Peptides 2009).

History

The KISS1 gene was discovered in 1996 during a screen for metastasis-suppressor factors in melanoma cells — the name "kisspeptin" was coined as a nod to the chocolate brand made in Hershey, Pennsylvania, where the discovery was made. The encoded peptide was initially catalogued as a tumor biology factor. The reproductive endocrinology chapter opened in 2003, when independent research teams showed that loss-of-function mutations in KISS1R (GPR54) caused hypogonadotropic hypogonadism, placing kisspeptin signaling at the top of the hormonal axis governing puberty, fertility, and gonadal function. A historical review of this trajectory from KISS1 to the kisspeptin peptide family and the naming conventions for isoforms is given in Gottsch and colleagues (Peptides 2009). The IUPHAR receptor nomenclature committee formally codified KISS1R distribution and function in Kirby and colleagues (Pharmacological Reviews 2010), providing the pharmacological framework used in subsequent research. Most of the clinical human work has been done with Kp-54 and Kp-10; Kp-13 has been studied primarily in the context of cross-species sequence conservation and receptor pharmacology (Okamura and colleagues, Animal Science Journal 2013; Akazome and colleagues, Journal of Fish Biology 2010).

What it does

Kisspeptin-13 binds KISS1R on neurons in the hypothalamus, prompting them to release gonadotropin-releasing hormone (GnRH) — the hormone that then drives the pituitary to produce LH and FSH, the hormones that in turn signal the gonads to make testosterone and estrogen. This chain of signals is called the hypothalamic–pituitary–gonadal (HPG) axis, and kisspeptin signaling sits at its upstream control point. All kisspeptin isoforms that share the C-terminal GLRF motif — including Kp-13 — are active at KISS1R, with the C-terminal sequence being the primary receptor-engagement pharmacophore (Kirby and colleagues 2010). Beyond reproductive control, the broader kisspeptin system also appears to integrate metabolic signals: circulating kisspeptin levels correlate with measures of glucose handling, and experimental kisspeptin administration affects insulin secretion in human volunteers (Izzi-Engbeaya and colleagues, Seminars in Reproductive Medicine 2019). A behavioral dimension has also been described: kisspeptin neurons are distributed in limbic brain regions beyond the hypothalamus, and kisspeptin signaling appears to modulate emotional and sexual behavioral processing (Mills and colleagues, Seminars in Reproductive Medicine 2019).

Evidence

  • Human: Clinical evidence for the broader kisspeptin system in humans is moderate-to-strong. Jayasena and colleagues (Journal of Clinical Endocrinology & Metabolism 2011) demonstrated that kisspeptin-10 acutely stimulates LH and FSH release in both men and women, with sexually dimorphic response patterns — providing the clearest human proof-of-concept for the receptor pharmacology that Kp-13 shares. Jayasena and colleagues (Clinical Pharmacology & Therapeutics 2010) showed that twice-weekly administration of Kp-54 for 8 weeks sustained gonadotropin stimulation in women with hypothalamic amenorrhea, though earlier work from the same group found that chronic subcutaneous Kp-54 causes tachyphylaxis (Jayasena and colleagues, Journal of Clinical Endocrinology & Metabolism 2009). Kp-13 itself has not been the primary intervention in published human trials; the human evidence base belongs predominantly to Kp-10 and Kp-54.
  • Animal: Strong. Intrahypothalamic administration of Kp-54 potently increased plasma LH and testosterone in adult male rats (Patterson and colleagues, Journal of Neuroendocrinology 2006), establishing the HPG-axis mechanism in rodents. Evolutionary conservation of the C-terminal kisspeptin sequence — including the Kp-13 region — across vertebrates from fish to mammals is documented in Akazome and colleagues (Journal of Fish Biology 2010) and Pasquier and colleagues (Frontiers in Endocrinology 2012).
  • In vitro / mechanistic: KISS1R excitation of GnRH neurons and downstream Ca²⁺ mobilization by kisspeptin are well characterized at the cellular level; the signaling pharmacology of the receptor is reviewed in Rønnekleiv and colleagues (Advances in Experimental Medicine and Biology 2013) and in the IUPHAR nomenclature review (Kirby and colleagues 2010).

Known effects

  • GnRH pulse stimulation — Mechanistic; well established across species. The primary and defining action of KISS1R agonism.
  • LH and FSH release (acute) — Human, RCT-level evidence for Kp-10 and Kp-54 (Jayasena and colleagues 2011). Shared mechanism with Kp-13 via KISS1R.
  • Gonadal steroid production — Downstream consequence of HPG axis activation; documented in animal models (Patterson and colleagues 2006) and inferred from human LH/FSH responses.
  • Behavioral and limbic modulation — Preclinical and mechanistic; kisspeptin neurons in limbic regions appear to modulate sexual and emotional processing (Mills and colleagues 2019).
  • Glucose homeostasis signaling — Emerging; associations between circulating kisspeptin and insulin secretion reported in human studies (Izzi-Engbeaya and colleagues 2019).
  • Reproductive diagnostics (pre-ovulation marker) — Circulating kisspeptin rises at the preovulatory phase; its utility as a biomarker for ovulation prediction has been investigated (Zhai and colleagues, Gynecological Endocrinology 2017).

Safety signals

Safety data for kisspeptin in humans derives almost entirely from studies of Kp-54 and Kp-10, not from Kp-13 specifically. In the clinical trials reviewed across the Jayasena group's work, acute kisspeptin administration was generally well tolerated, with injection-site reactions being the most commonly reported event. The tachyphylaxis signal — receptor desensitization with continuous or high-frequency dosing — is mechanistically important: Jayasena and colleagues (2009) observed that chronic subcutaneous Kp-54 produced diminishing gonadotropin responses, establishing a practical ceiling on repeated-dosing protocols. Loss-of-function mutations in KISS1R cause hypogonadotropic hypogonadism in humans, as reviewed in Bonomi and colleagues (Asian Journal of Andrology 2012), illustrating that this signaling axis is not redundant for reproductive function. The long-term safety of repeated exogenous kisspeptin administration beyond the duration of published trials (typically single doses or courses of weeks) remains uncharacterized.

Regulatory status

  • US: Not FDA-approved for any indication. No kisspeptin isoform holds marketing authorization in the United States. Clinical research continues.
  • EU/UK: Not EMA- or MHRA-approved. The UK has hosted the majority of published human clinical trials of kisspeptin through Imperial College London, but no marketing authorization has been granted.
  • WADA: Not explicitly named, but falls under S2 (peptide hormones and releasing factors) by mechanism — any peptide that acutely stimulates LH and testosterone release is prohibited in competitive sport under catch-all language covering GnRH and its analogs.
  • Compounding / research use: Not on FDA's 503A compounding bulk substances list. All human use is in the context of clinical trials or specialist medical settings.

Related peptides

The kisspeptin isoforms share the KISS1R pharmacophore but differ in length and pharmacokinetics. The full-length 54-residue form (Kisspeptin-54), which has the most extensive clinical evidence base covering IVF triggering, hypothalamic amenorrhea, and hypoactive sexual desire disorder, is catalogued separately on this platform. The shorter Kp-10 decapeptide, used in human sexual-dimorphism studies and mechanistic work (Jayasena and colleagues 2011), is likewise a distinct card in this family. For the broader GnRH-axis context, GnRH itself and its clinical analogs (leuprolide, triptorelin) act one step downstream of kisspeptin signaling.

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 the middle portion of kisspeptin-13 make the fertility signal last longer inside the cell?

Kisspeptin is a natural hormone that tells the brain to release reproductive hormones. If this hypothesis holds, a specific stretch of kisspeptin-13 could keep the signal switched on longer, which might allow doctors to better tune fertility treatments for conditions like irregular ovulation, potentially improving outcomes without increasing the dose.

The hypothesis
The NYNWNS segment (positions 3-8) in Kp-13 acts as an allosteric modulator of the GLRF pharmacophore-KISS1R interaction, slowing the rate of Gq/11 uncoupling after initial receptor activation and thereby prolonging the duration of intracellular calcium transients beyond what the GLRF motif alone (as in Kp-10) produces.
Why it’s plausible
The KISS1R-kisspeptin structural pharmacology literature shows that the C-terminal GLRF motif is the primary pharmacophore, but that all isoforms have equivalent in vitro affinity while longer forms show superior in vivo effect. This discrepancy implies the upstream sequence affects post-binding dynamics rather than initial binding kinetics. NYNWNS contains two aromatic residues (W at position 6, Y at position 4) that could engage extracellular loop residues of KISS1R through pi-stacking or hydrophobic contacts, establishing a secondary binding interface that slows receptor-ligand complex rearrangement. The high iptm of 0.91 suggests the predicted complex captures a stable pose that may include contacts beyond the GLRF terminus.
Why it matters
If NYNWNS acts as an allosteric modifier of KISS1R signaling duration, it defines a new pharmacological handle in kisspeptin design: the duration of the calcium transient, not just its amplitude, could be tuned by N-terminal engineering. This is directly relevant to GnRH pulse frequency programming, where signal duration affects the differential release of LH versus FSH from the pituitary.
Plausibility.50
Novelty.62
Impact.63
Basis · grounding1 paper · 2 computed/notes
[1]
structureiptm 0.91 indicates a confident, stable complex pose with KISS1R; the high interface confidence suggests contacts beyond the minimal GLRF pharmacophore may be captured.
[2]
paper
Kisspeptin-induced inward currents involve TRPC-like cationic channels and multiple ion channel blockers differentially inhibit the response, indicating a complex downstream signaling cascade whose duration could be modulated allosterically.
doi: 10.1007/978-1-4614-6199-9_6
[3]
sequenceNYNWNS segment (positions 3-8) contains aromatic residues Y4 and W6 capable of pi-stacking with receptor extracellular loop residues, providing a potential secondary contact surface.
openupdated 2026-06-05

Could reshaping kisspeptin-13 into a closed loop stop the body from breaking it down too quickly?

Natural kisspeptin fragments are destroyed in the bloodstream within minutes, which makes them impractical as a drug. If this chemical modification works, it could yield a small, stable version that lasts long enough for patients to inject at home, potentially opening up treatment options for people with hormonal infertility who currently have few convenient choices.

The hypothesis
Cyclization of Kp-13 via a lactam bridge between the N-terminal amine (L1) and a glutamate introduced at position 8 (replacing S8) would confer proteolytic resistance exceeding that of linear Kp-13 while preserving KISS1R agonism, because the lactam would lock the LP-NYNWN segment into a constrained loop that shields the trypsin-labile RF terminus from exopeptidase approach.
Why it’s plausible
Linear kisspeptin fragments have short plasma half-lives (approximately 4 minutes for Kp-10). The GLRF terminus is susceptible to carboxypeptidase and the LP N-terminus to aminopeptidase. A head-to-sidechain lactam using the natural LP N-terminus as the bridge donor and a strategically placed Glu sidechain at position 8 (currently S8, a small polar residue tolerant of substitution) would create a constrained ring over the non-pharmacophore N-terminal portion, physically protecting both termini without altering the GLRF receptor-binding tail that protrudes from the ring. S8 is distant from the pharmacophore GLRF (positions 10-13) based on sequence and predicted structure.
Why it matters
A stable cyclic Kp-13 analog could achieve the in vivo duration of Kp-54 in a 13-residue scaffold, dramatically reducing synthesis cost and immunogenicity while enabling subcutaneous self-administration for hypothalamic amenorrhea or male hypogonadotropic hypogonadism, indications where the tachyphylaxis and short half-life of current kisspeptin fragments are the main barriers to clinical use.
Plausibility.52
Novelty.52
Impact.62
Basis · grounding1 paper · 2 computed/notes
[1]
paper
Plasma half-life of Kp-10 is approximately 4 minutes in human volunteers, establishing the short half-life benchmark that cyclization aims to overcome.
doi: 10.1210/jc.2011-1408
[2]
sourceAxis-hit on proteolytic stability noting that certain peptide modifications confer complete resistance to trypsin, chymotrypsin, pepsin, and papain.
[3]
sequenceS at position 8 of LPNYNWNSFGLRF is a small polar residue outside the pharmacophore GLRF (positions 10-13); substitution with Glu to enable lactam cyclization is structurally feasible without disrupting the receptor-binding motif.
openupdated 2026-06-05

Could kisspeptin-13 stimulate the fertility signal while causing less of the receptor shutdown that makes repeated doses less effective?

A recurring problem with kisspeptin therapy is that the receptor it targets can become desensitized, making the drug less effective with repeated use. If kisspeptin-13 turns out to favor one signaling pathway over the one that triggers desensitization, it could be better suited for ongoing fertility treatment, for example in people with hypothalamic amenorrhea who need repeated stimulation.

The hypothesis
Kp-13, owing to its intermediate chain length, displays a differential bias toward Gq/11-mediated calcium mobilization over beta-arrestin-mediated receptor internalization relative to both Kp-10 and Kp-54 at equimolar receptor occupancy.
Why it’s plausible
KISS1R signals through Gq/11-PLC and is subject to beta-arrestin-mediated desensitization. Chain length affects receptor contact surface; longer peptides (Kp-54) produce greater tachyphylaxis in vivo (Jayasena 2009), suggesting they drive more beta-arrestin recruitment. The LP extension in Kp-13 adds two residues versus Kp-10 but 41 fewer than Kp-54. If the N-terminal tail allosterically contacts an extracellular loop of KISS1R, biased agonism could emerge at this intermediate length. The selectivity axis literature notes that ligands in the kisspeptin family are frequently treated as interchangeable when their discrete physiological roles may actually differ.
Why it matters
A Kp-13 variant with favorable Gq/11 bias would be more resistant to tachyphylaxis than Kp-54 while retaining the superior half-life advantage over Kp-10. This would resolve the clinical dilemma where the longest active isoform drives desensitization, making Kp-13 a lead for repeat-dosing fertility indications such as hypothalamic amenorrhea.
Plausibility.38
Novelty.58
Impact.63
Basis · grounding3 papers
[1]
paper
Chronic subcutaneous Kp-54 produced diminishing gonadotropin responses (tachyphylaxis), establishing a practical ceiling for continuous dosing.
doi: 10.1210/jc.2009-0406
[2]
paper
Kisspeptin ligands are frequently considered interchangeable in the literature despite potentially discrete physiological roles.
doi: 10.1055/s-0039-3400242
[3]
paper
KISS1R activation is via Gq/11 and PLC pathway; receptor internalization pathways are established components of KISS1R pharmacology.
doi: 10.1124/pr.110.002774
openupdated 2026-06-05

Do the two extra building blocks at the start of kisspeptin-13 help it stay attached to the receptor for longer?

Kisspeptin-10 is active but very brief in its action. If the LP addition in kisspeptin-13 slows how quickly the peptide lets go of its receptor, it could provide a longer hormonal pulse without overstimulating the system. That would matter in IVF protocols, where timing and duration of the fertility signal directly affect success rates.

The hypothesis
The LP dipeptide at positions 1-2 of Kp-13 (absent in Kp-10) forms a transient beta-turn or proline-constrained kink that slows the rate of receptor dissociation from KISS1R, giving Kp-13 a longer receptor-occupied dwell time than Kp-10 without altering maximal efficacy.
Why it’s plausible
All kisspeptin isoforms share equivalent in vitro KISS1R affinity, yet in vivo potency scales with chain length. Kp-13 adds LP to the Kp-10 N-terminus. Proline is a helix and turn breaker; an LP motif at a free N-terminus commonly adopts a type-II beta-turn-like geometry that could occlude protease access to the adjoining NYNWNS segment and sterically retard receptor unbinding. The boltz-2 prediction gives an iptm of 0.91, indicating a confident complex pose, yet avg_plddt is only 70.3, consistent with partial disorder in the N-terminal LP region that could adopt multiple low-energy conformations upon receptor contact.
Why it matters
If LP prolongs receptor dwell without changing Gq/11 coupling, Kp-13 would be pharmacokinetically superior to Kp-10 for pulsatile GnRH stimulation, which requires sustained but not continuous receptor activation. This would distinguish Kp-13 as the isoform of choice for IVF triggering protocols where receptor desensitization (tachyphylaxis) is a clinical constraint.
Plausibility.38
Novelty.57
Impact.53
Basis · grounding1 paper · 2 computed/notes
[1]
paper
All kisspeptin isoforms reported to have similar affinity and efficacy in vitro at GPR54; Kp-54 is most effective in vivo, implying length-dependent pharmacokinetic, not pharmacodynamic, advantage.
doi: 10.1124/pr.110.002774
[2]
structureiptm 0.91 indicates confident KISS1R interface; avg_plddt 70.3 is consistent with partially disordered N-terminal extension in the unbound state.
[3]
sequenceKp-13 sequence LPNYNWNSFGLRF begins with LP, which is absent from Kp-10 (YNWNSFGLRF); proline at position 2 constrains backbone phi/psi angles.
openupdated 2026-06-05

Did the upper portion of kisspeptin-13 evolve specifically to match the human fertility receptor rather than the equivalent receptor in fish?

If the distinctive part of kisspeptin-13 fits the human receptor but not the fish version, researchers could use that difference in two ways: designing peptides that control spawning in farmed fish without affecting other biology, and building sharper drug candidates for human reproductive conditions by understanding exactly which molecular features matter for selectivity.

The hypothesis
Kp-13 binds the single mammalian KISS1R with higher apparent affinity than the fish-lineage Kiss2r ortholog, and this selectivity gap narrows for Kp-10, because the LP-N segment in positions 1-8 co-evolved with mammalian KISS1R extracellular loop 2 residues that are absent or divergent in teleost Kiss2r.
Why it’s plausible
Teleost fish possess two kisspeptin receptors (Kiss1r and Kiss2r); mammals retain only one (KISS1R, orthologous to fish Kiss1r). The fish Kp-13 equivalent region shows the most sequence variation at the N-terminal end while preserving the C-terminal GLRF pharmacophore. Cross-species conservation data in Akazome et al. (2010) and Pasquier et al. (2012) show the Kp-10 core is conserved, but upstream residues vary. If fish Kiss2r-selective peptides differ primarily in N-terminal composition, then the LP extension in Kp-13 is a mammal-specific elaboration that disfavors Kiss2r engagement.
Why it matters
Understanding which structural features of Kp-13 confer mammalian KISS1R versus fish Kiss2r selectivity would allow rational design of isoform-selective kisspeptin analogs for aquaculture reproductive management, a commercially significant application for controlling spawning in farmed species, as well as informing KISS1R pharmacophore models for human drug design.
Plausibility.42
Novelty.57
Impact.40
Basis · grounding2 papers · 1 computed/note
[1]
paper
Comparative table shows N-terminal sequence variation in the Kp-10 region across fish and mammals; GLRF C-terminus is conserved; fish have two Kissr paralogs.
doi: 10.1111/j.1095-8649.2009.02496.x
[2]
paper
Comparative evolutionary analysis of kisspeptin receptors across vertebrates showing both parallel and divergent features.
doi: 10.3389/fendo.2012.00173
[3]
sequenceKp-13 LP dipeptide at positions 1-2 is not shared by fish Kiss1 orthologs (table in 10.1111/j.1095-8649.2009.02496.x shows F/Y at position equivalent to Kp-13 position 4 varies across species).
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.9129645824432373 boltz-2
ranking score 0.7452750205993652 boltz-2
3-letter notation
Leu-Pro-Asn-Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-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). Kisspeptin-13: natural fragment that triggers the reproductive hormone system (pep-10619, v1). PeptideModel. https://peptidemodel.com/card/pep-10619
@peptide{pep10619,
  sequence = {LPNYNWNSFGLRF},
  target   = {kiss1r},
  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 14 papers
[3]
The Effects of Kisspeptin-10 on Reproductive Hormone Release Show Sexual Dimorphism in Humans
Jayasena, C. et al. The Journal of Clinical Endocrinology & Metabolism 2011
supporting
[4]
Kisspeptin Excitation of GnRH Neurons
Rønnekleiv, O. et al. Advances in Experimental Medicine and Biology 2013
supporting
[6]
Kisspeptin as a Behavioral Hormone
Mills, E. et al. Seminars in Reproductive Medicine 2019
supporting
[9]
Kisspeptin and Glucose Homeostasis
Izzi-Engbeaya, C. et al. Seminars in Reproductive Medicine 2019
supporting
[13] supporting
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