Metastin is an antimetastatic peptide encoded by the KiSS-1 gene in cancer cells. Recent studies found that metastin is a ligand for the orphan G-protein-coupled receptor GPR54, which is highly expressed in specific brain regions such as the hypothalamus and parts of the hippocampus. This study shows that activation of GPR54 by submicromolar concentrations of metastin reversibly enhances excita...

TheKiSS-1 gene has been reported to be ametastasis suppressor gene in humanmelanoma. Thegene product was isolated from human placenta as the ligand of GPR54, a G protein–coupled receptor, and the C-terminally amidated peptide of 54 amino acids is called metastin. The binding of metastin to GPR54 has been shown to inhibit tumormetastasis in some tumor cells; however, its function remains unclear...

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...

Objective The inhibitory effects of Morphine and the stimulatory influence of kisspeptin signaling have been demonstrated on GnRH/LH release. Hypothalamic kisspeptin is involved in relaying the environmental and metabolic information to reproductive axis. In the present study the role of kisspeptin/GPR54 signaling system was investigated on relaying the inhibitory effects of morphine on LH horm...

Reproduction is integrated by interaction of neural and hormonal signals converging on hypothalamic neurons for controlling gonadotropin-releasing hormone (GnRH). Kisspeptin, the peptide product of the kiss1 gene and the endogenous agonist for the GRP54 receptor, plays a key role in the regulation of GnRH secretion. In the present study, we investigated the interaction between kisspeptin, estro...

KiSS1 is a putative metastasis suppressor gene in melanoma and breast cancer-encoding kisspeptins, which are also described as neuroendocrine regulators of the gonadotropic axis. Negative as well as positive regulation of KiSS1 gene expression by estradiol (E(2)) has been reported in the hypothalamus. Estrogen receptor alpha (ERalpha level is recognized as a marker of breast cancer, raising the...

Neurons that produce gonadotropin-releasing hormone (GnRH) drive the reproductive axis, but the molecular and cellular mechanisms by which hormonal and environmental signals regulate GnRH secretion remain poorly understood. Kisspeptins are products of the Kiss1 gene, and the interaction of kisspeptin and its receptor GPR54 plays a crucial role in governing the onset of puberty and adult reprodu...

BACKGROUND Kisspeptin-10 (KP-10), a potent vasoconstrictor and inhibitor of angiogenesis, and its receptor, GPR54, have currently received much attention in relation to pre-eclampsia. However, it still remains unknown whether KP-10 could affect atherogenesis. METHODS AND RESULTS We evaluated the effects of KP-10 on human umbilical vein endothelial cells, human monocyte-derived macrophages, hu...

Kisspeptins are products of the KiSS-1 gene, which bind to a G protein-coupled receptor known as GPR54. Mutations or targeted disruptions in the GPR54 gene cause hypogonadotropic hypogonadism in humans and mice, suggesting that kisspeptin signaling may be important for the regulation of gonadotropin secretion. To examine the effects of kisspeptin-54 (metastin) and kisspeptin-10 (the biologicall...