KiSS1-derived peptide receptor

KiSS1-derived peptide receptor

KISS1 receptor
Identifiers
KISS1R Gene
Orthologs
SpeciesHumanMouse

The KiSS1-derived peptide receptor (also known as GPR54 or the Kisspeptin receptor) is a G protein-coupled receptor[1] which binds the peptide hormone kisspeptin (metastin).[2][3][4] Kisspeptin is encoded by the metastasis suppressor gene KISS1, which is expressed in a variety of endocrine and gonadal tissues.[5] Activation of the kisspeptin receptor is linked to the phospholipase C and inositol trisphosphate second messenger cascades inside the cell.[6]

Function

Kisspeptin is involved in the regulation of endocrine function and the onset of puberty, with activation of the kisspeptin receptor triggering release of gonadotropin-releasing hormone (GnRH),[7][8] and release of kisspeptin itself being inhibited by oestradiol but enhanced by GnRH.[9] Reductions in kisspeptin levels with age may conversely be one of the reasons behind age-related declines in levels of other endocrine hormones such as luteinizing hormone.[10]

Ligands

No non-peptide ligands for this receptor have yet been discovered, but as of 2009 both selective agonist and antagonist peptides are known.

Agonists

Antagonists

  • Kisspeptin-10 analogues modified with amino substitutions[12]

References

Further reading

External links

  • Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.