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New Gatekeepers of Reproduction: GPR54 and Its Cognate Ligand, KiSS-1

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This article is published in Endocrinology.The article was published on 2005-04-01 and is currently open access. It has received 60 citations till now.

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Activation of Gonadotropin-Releasing Hormone Neurons by Kisspeptin as a Neuroendocrine Switch for the Onset of Puberty

TL;DR: It is demonstrated that kisspeptin exerts a potent depolarizing effect on the excitability of almost all adult GnRH neurons and that the responsiveness of Gn RH neurons tokisspeptin increases over postnatal development.
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Evidence for two distinct KiSS genes in non-placental vertebrates that encode kisspeptins with different gonadotropin-releasing activities in fish and mammals

TL;DR: The data are the first to provide conclusive evidence for the existence of a second KiSS gene, KiSS-2, in non-placental vertebrates, whose product is likely to play a dominant stimulatory role in the regulation of the gonadotropic axis at least in teleosts.
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Ontogeny and mechanisms of action for the stimulatory effect of kisspeptin on gonadotropin-releasing hormone system of the rat.

TL;DR: The present data document the ontogeny, sensitivity and intracellular signals for the stimulatory action of kisspeptin on the GnRH/LH axis in the rat and stress the essential role ofkisspeptin in normal, and eventually pathological, timing of puberty.
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Glucagon regulates hepatic kisspeptin to impair insulin secretion.

TL;DR: It is shown that glucagon stimulates via cAMP-PKA-CREB signaling hepatic production of the neuropeptide kisspeptin1, which acts on β cells to suppress GSIS, and this indicates a hormonal circuit between the liver and the endocrine pancreas in glycemia regulation and suggests in T2DM a sequential link between hyperglucagonemia via hepatic kisspe leptin1 to impaired insulin secretion.
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Hypothalamic Expression of KiSS-1 System and Gonadotropin-Releasing Effects of Kisspeptin in Different Reproductive States of the Female Rat

TL;DR: This work evaluated maximal LH and FSH secretory responses to kisspeptin-10, as well as changes in sensitivity and hypothalamic expression of KiSS-1 and GPR54 genes, in different physiological and experimental models in the adult female rat to document for the first time the changes in leptin expression and the gonadotropic effects in different functional states of the female reproductive axis.
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The KiSS-1 receptor GPR54 is essential for the development of the murine reproductive system

TL;DR: The analysis of the GPR54 mutant mice revealed developmental abnormalities of both male and female genitalia and histopathological changes in tissues which normally contain sexually dimorphic features, suggesting a role for GPR 54/KiSS-1 in normal sexual development.
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Peripheral administration of metastin induces marked gonadotropin release and ovulation in the rat

TL;DR: It is shown that subcutaneous administration of metastin increased the plasma levels of gonadotropins and induced ovulation in prepubertal female rats that had been pretreated with pregnant mare serum gonadotropic hormone to induce follicle maturation and that s.c. administered metastin induces the release of Gonadotropin via activation of the hypothalamic GnRH neurons.
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Central and peripheral administration of kisspeptin-10 stimulates the hypothalamic-pituitary-gonadal axis.

TL;DR: Kisspeptin therefore potently stimulates the hypothalamic‐pituitary‐gonadal axis and is likely to be mediated via the hypothalamate LHRH system.
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Characterization of the potent luteinizing hormone-releasing activity of KiSS-1 peptide, the natural ligand of GPR54.

TL;DR: Results provide solid evidence for a potent stimulatory effect of KiSS-1 on LH release, acting at central levels (likely the hypothalamus) and eventually at the pituitary, and further document a novel role of the Ki SS1/GPR54 system as a relevant downstream element in the neuroendocrine network governing LH secretion.
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Advanced vaginal opening and precocious activation of the reproductive axis by KiSS-1 peptide, the endogenous ligand of GPR54

TL;DR: It is reported that chronic central administration of KiSS‐1 peptide to immature female rats induced the precocious activation of the gonadotrophic axis, as estimated by advanced vaginal opening, elevated uterus weight, and increased serum levels of luteinizing hormone (LH) and oestrogen.
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