Kisspeptin, encoded by the Kiss1 gene, is required for reproduction. Humans and mice lacking kisspeptin or its receptor, Kiss1r, have impairments in reproductive physiology and fertility. In addition to being located in the hypothalamus in the anteroventral periventricular and arcuate nuclei, kisspeptin neurons are also present in several extra-hypothalamic regions, such as the medial amygdala ...

Invasion into deep myometrium and/or lymphovascular space is a well-known risk factor for endometrial cancer metastasis, resulting in poor prognosis. It is therefore clinically important to identify novel molecules that suppress tumor invasion. Reduced expression of the metastasis suppressor, kisspeptin (KISS1), and its endogenous receptor, GPR54, has been reported in several cancers, but the s...

The dogmatic adherence to “what is good for the goose is good for the gander” appears to pervade avian endocrinology research when it comes to vertebrate evolution of hormones and their physiological roles in birds. There appears to be a general acceptance that specific hormones, their cognate receptors, and their regulatory functions identified in other vertebrates should be present and serve ...

The gonadotropic axis is centrally controlled by a complex regulatory network of excitatory and inhibitory signals that is activated at puberty. Recently, loss of function mutations of the gene encoding G protein-coupled receptor 54 (GPR54), the putative receptor for the KiSS-1-derived peptide metastin, have been associated with lack of puberty onset and hypogonadotropic hypogonadism. Yet the p...

Kisspeptin has recently emerged as a key regulator of the mammalian reproductive axis. It is known that kisspeptin, acting centrally via the kisspeptin receptor, stimulates secretion of gonadotrophin releasing hormone (GnRH). Loss of kisspeptin signaling causes hypogonadotrophic hypogonadism in humans and other mammals. Kisspeptin interacts with other neuropeptides such as neurokinin B and dyno...

G protein-coupled receptor 54 (GPR54) is a G(q/11)-coupled 7 transmembrane-spanning receptor (7TMR). Activation of GPR54 by kisspeptin (Kp) stimulates PIP(2) hydrolysis, Ca(2+) mobilization and ERK1/2 MAPK phosphorylation. Kp and GPR54 are established regulators of the hypothalamic-pituitary-gonadal (HPG) axis and loss-of-function mutations in GPR54 are associated with an absence of puberty and...

Kisspeptins are peptide products of the KiSS-1 metastasis-suppressor (KISS1) gene and the natural ligands of the G-protein– coupled receptor GPR54. KISS1 was initially investigated as an antimetastasis gene. More recent studies have demonstrated that the kisspeptins are potent stimulators of the hypothalamo-pituitarygonadal axis. Mice and humans with defective kisspeptin signaling show hypogona...

BACKGROUND Kisspeptin-GPR54 system stimulates the hypothalamus-pituitary-gonadal (HPG) axis; dysfunction of the gene encoding the GPR54 receptor causes hypogonadism and infertility. Opioid peptides inhibit the reproductive axis. Peptide 234 is a GPR54 receptor antagonist and blocks the stimulatory effects of kisspeptin on HPG axis. OBJECTIVES Interactions of morphine, kisspeptin and peptide 2...