KiSS1-derived peptide receptor

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

Function
Kisspeptin is involved in the regulation of endocrine function and the onset of is_associated_with::puberty, with activation of the kisspeptin receptor triggering release of is_associated_with::gonadotropin-releasing hormone (GnRH), and release of kisspeptin itself being inhibited by is_associated_with::oestradiol but enhanced by GnRH. 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 is_associated_with::luteinizing hormone.

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

 * is_associated_with::Kisspeptin
 * Kisspeptin-10 (112-121 C-terminal fragment)

Antagonists

 * Kisspeptin-10 analogues modified with amino substitutions