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Compound Profiles

Kisspeptin: How a Metastasis-Suppressor Gene Led to a New Peptide Hormone

In 2001 researchers showed that the KiSS-1 gene encodes peptides that activate the orphan receptor GPR54. The discovery reshaped research on neuroendocrine signalling.

Kisspeptins are peptides derived from the product of the KISS1 gene (originally written KiSS-1). Kisspeptin-10, the shortest active form, consists of ten amino acids.

The 2001 discovery

Ohtaki and colleagues reported in Nature in 2001, in Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor, that peptides derived from the KiSS-1 gene product are the endogenous ligands of the orphan receptor GPR54 (now often called KISS1R). They named the 54-amino-acid peptide metastin, reflecting the gene's earlier identification in metastasis-suppression research, and showed its activity at the receptor.

Why it mattered

Identifying a ligand for an orphan receptor gives researchers the tools to study the receptor's function. Subsequent research established the kisspeptin–KISS1R system as an important subject in neuroendocrinology.

Different lengths, shared activity

Kisspeptins of different lengths share a common C-terminal sequence, and the C-terminal decapeptide (kisspeptin-10) retains activity at the receptor in experimental systems. This makes the short form convenient for laboratory studies.

Analytical considerations

Kisspeptin-10 has an amidated C-terminus. Identity data should confirm the amide rather than the free acid, since the two differ by about one mass unit and the free acid is a potential related impurity.

Kisspeptin-10 supplied by ICU RESEARCH is for laboratory research use only.

Scientific references

Primary source: Ohtaki T, Shintani Y, Honda S, et al. Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor. Nature. 2001;411:613–617. — Source published 31 May 2001

For laboratory research information only. Not medical advice; no product is intended for human or veterinary use.