The KiSS1-derived peptide receptor (also known as GPR54 or the Kisspeptin receptor) is a
G protein-coupled receptor which binds the peptide hormone
kisspeptin (metastin).
Kisspeptin is encoded by the
metastasis suppressor gene
KISS1
Kisspeptins (including kisspeptin-54 (KP-54), formerly known as metastin) are proteins encoded by the ''KISS1'' gene in humans. Kisspeptins are ligands of the G-protein coupled receptor, GPR54. ''Kiss1'' was originally identified as a human meta ...
, which is expressed in a variety of endocrine and gonadal tissues.
Activation of the kisspeptin receptor is linked to the
phospholipase C
Phospholipase C (PLC) is a class of membrane-associated enzymes that cleave phospholipids just before the phosphate group (see figure). It is most commonly taken to be synonymous with the human forms of this enzyme, which play an important role ...
and
inositol trisphosphate second messenger cascades inside the cell.
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),
and release of kisspeptin itself being inhibited by
oestradiol
Estradiol (E2), also spelled oestradiol, is an estrogen steroid hormone and the major female sex hormone. It is involved in the regulation of the estrous and menstrual female reproductive cycles. Estradiol is responsible for the development of f ...
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
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
*
Kisspeptin (kisspeptin-54, metastin)
* Kisspeptin-10 (112-121 C-terminal fragment)
*
KISS1-305
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MVT-602
MVT-602 (other developmental code names RVT-602, TAK-448) is a kisspeptin receptor agonist which is under development for the treatment of female infertility and hypogonadism. It has been found to increase luteinizing hormone levels in premeno ...
(RVT-602, TAK-448)
*
TAK-683
Antagonists
* Kisspeptin-10 analogues modified with amino substitutions
*
Kisspeptin-234
References
Further reading
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External links
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{{G protein-coupled receptors
G protein-coupled receptors