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Research Overview

Kisspeptin-10 (Research Overview)

Kisspeptins are a family of RF-amide peptides encoded by the KiSS-1 gene, which was first described as a metastasis suppressor gene in melanoma cells. Kisspeptin-10 (Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2, molecular weight about 1302 Da) is the C-terminal decapeptide of the family and carries the shared RF-amide motif.

Mechanism of Action

In 2001, two groups reported that the products of the KiSS-1 gene are the natural ligands of the orphan G protein-coupled receptor GPR54 (now designated KISS1R). The peptides, which have a common RF-amide C terminus, bound the receptor with low nanomolar affinity in transfected cells and stimulated phosphoinositide hydrolysis, calcium mobilization and MAP kinase phosphorylation.

Cryo-EM structures of KISS1R bound to kisspeptin-10 and to a synthetic analogue have since shown how the peptide ligands engage the receptor's extracellular loops, and that the receptor couples to Gq through a distinctive intracellular conformation. Reviews describe the structure, synthesis and phylogeny of kisspeptins and their receptors across vertebrates.

Research Areas

Receptor pharmacology and structure: kisspeptin-10 is used as the reference agonist in KISS1R binding, signalling and structural studies.

Neuroendocrine research: reviews describe kisspeptins as neuropeptides produced in discrete hypothalamic nuclei that act upstream of gonadotropin-releasing hormone (GnRH) neurons, and they summarize the regulatory mechanisms examined in animal models.

Comparative biology: the kisspeptin and KISS1R systems have been compared across vertebrate species, including the additional kisspeptin and receptor subtypes found in non-mammalian species.

Findings from published studies do not establish safety or efficacy for any indication and should not be interpreted as medical claims.

Specification summary

Molecular Weight1302.4 Da
Molecular FormulaC63H83N17O14
CAS Number374675-21-5
SequenceTyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2
Compound TypeRF-amide neuropeptide
Related research compound at Sealed Peptides

Kisspeptin-10 10mg

Stated purity ≥99%. For laboratory research use only.

View Kisspeptin-10

Related materials

References

  1. Kotani M, Detheux M, Vandenbogaerde A, Communi D, Vanderwinden JM, Le Poul E, et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J Biol Chem. 2001;276(37):34631-6. PMID 11457843 · DOI
  2. Ohtaki T, Shintani Y, Honda S, Matsumoto H, Hori A, Kanehashi K, et al. Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor. Nature. 2001;411(6837):613-7. PMID 11385580 · DOI
  3. Pinilla L, Aguilar E, Dieguez C, Millar RP, Tena-Sempere M. Kisspeptins and reproduction: physiological roles and regulatory mechanisms. Physiol Rev. 2012;92(3):1235-316. PMID 22811428 · DOI
  4. Kanda S, Oka Y. Structure, synthesis, and phylogeny of kisspeptin and its receptor. Adv Exp Med Biol. 2013;784:9-26. PMID 23550000 · DOI
  5. Shen S, Wang D, Liu H, He X, Cao Y, Chen J, et al. Structural basis for hormone recognition and distinctive Gq protein coupling by the kisspeptin receptor. Cell Rep. 2024;43(7):114389. PMID 38935498 · DOI

Cited literature is provided for scientific context only and does not describe or endorse any use of these products.

For laboratory research use only. Not for human or veterinary use. Not intended to diagnose, treat, cure, or prevent any disease.