RF-amide neuropeptides and their receptors in Mammals: Pharmacological properties, drug development and main physiological functions

Quillet, Raphaëlle; Ayachi, Safia; Bihel, Frédéric; Elhabazi, Khadija; Ilien, Brigitte; Simonin, Frédéric

doi:10.1016/j.pharmthera.2016.02.005

Cited by 51 publications

(53 citation statements)

References 609 publications

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“…This may be because, at some moment during the reactivation, the effect of RFRP‐3 will switch from stimulatory to inhibitory as a result of RFRP‐3 being inhibitory in sexually active male Djungarian hamsters. This complex functional pattern might be related to the pharmacology and expression pattern of the 2 GPCR receptors binding RFRP, NPFF1 and NPFF2 . Understanding how photoperiodic variation in RFRP‐3 participates in the photoperiodic regulation of the gonadotrophic axis will now have to concentrate on how and where these differential responses to this peptide are generated, particularly whether they involve various RFRP‐3 receptor(s) present on kisspeptin or GnRH neurones.…”

Section: Discussionmentioning

confidence: 99%

Differential response patterns of kisspeptin and RFamide‐related peptide to photoperiod and sex steroid feedback in the Djungarian hamster (Phodopus sungorus)

Rasri-Klosen

Simonneaux

Klosen

2017

J Neuroendocrinology

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Many animals synchronise their reproductive activity with the seasons to optimise the survival of their offspring. This synchronisation involves switching on and off their gonadotrophic axis. Ever since their discovery as key regulators of gonadotrophin-releasing hormone (GnRH) neurones, the hypothalamic RF-amide peptides kisspeptin and RFamide-related peptide (RFRP) have been a major focus of research on the seasonal regulation of the gonadotrophic axis. In the present study, we investigated the regulation of both neuropeptides in the Djungarian hamster, a major animal model for the study of seasonal reproduction. During the long-day breeding period, kisspeptin neurones in the anteroventral periventricular area are solely controlled by a positive sex steroid feedback and, in the arcuate nucleus, they are subject to a very strong negative sex steroid feedback associated with a minor photoperiodic effect. During short-day sexual quiescence, the disappearance of this hormonal feedback leads to high levels of kisspeptin in arcuate neurones. Notably, chronic central administration of kisspeptin is able to over-ride the photoperiodic inhibition of the gonadotrophic axis and reactivate the reproductive function. Therefore, our data suggest that kisspeptin secretion by arcuate neurones during sexual quiescence is inhibited by mechanisms upstream of kisspeptin neurones. RFRP expression is solely controlled by photoperiod, being strongly reduced in short days independently of the sex steroid feedback. Thus, kisspeptin and RFRP display contrasting patterns of expression and regulation. Upstream mechanisms controlling these neurones should be the focus of further studies on the roles of these RFamide neuropeptides in the seasonal control of reproduction.

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Section: Discussionmentioning

confidence: 99%

Differential response patterns of kisspeptin and RFamide‐related peptide to photoperiod and sex steroid feedback in the Djungarian hamster (Phodopus sungorus)

Rasri-Klosen

Simonneaux

Klosen

2017

J Neuroendocrinology

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“…In vertebrates, the RFamide peptide family consists of PRL-releasing peptides (PrRP), PQRFamide peptides (neuropeptide FF, NPFF), pyroglutamylated RFamide peptide (QRFP)/26RFamides, LPXRFamide peptides (gonadotropin-inhibitory hormone, GnIH, in lower vertebrates, RFamide-related peptide-3, RFRP-3, in mammals) and kisspeptins (Tsutsui and Ubuka, 2013; Osugi et al, 2016). RFamides have been shown to regulate several physiological functions in vertebrates, including feeding (Bechtold and Luckman, 2007; Quillet et al, 2016). A number of RFamides have been identified in fish, although most have been examined for their role in reproduction and are not yet well characterized with regards to their potential role as feeding regulators.…”

Section: Hormones Involved In Food Intakementioning

confidence: 99%

The Neuroendocrine Regulation of Food Intake in Fish: A Review of Current Knowledge

2016

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Fish are the most diversified group of vertebrates and, although progress has been made in the past years, only relatively few fish species have been examined to date, with regards to the endocrine regulation of feeding in fish. In fish, as in mammals, feeding behavior is ultimately regulated by central effectors within feeding centers of the brain, which receive and process information from endocrine signals from both brain and peripheral tissues. Although basic endocrine mechanisms regulating feeding appear to be conserved among vertebrates, major physiological differences between fish and mammals and the diversity of fish, in particular in regard to feeding habits, digestive tract anatomy and physiology, suggest the existence of fish- and species-specific regulating mechanisms. This review provides an overview of hormones known to regulate food intake in fish, emphasizing on major hormones and the main fish groups studied to date.

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“…The number of FLPs characterized in vertebrates is much lower than in invertebrates (Orchard and Lange, ). In mammals, five distinct genes, designated farp‐1 to farp‐5 (Dockray, ), encoding seven FLPs have been identified so far (Quillet et al, ).…”

Section: Rfa/qrfp Peptidesmentioning

confidence: 99%

The Arg–Phe‐amide peptide 26RFa/glutamine RF‐amide peptide and its receptor: IUPHAR Review 24

Leprince

Bagnol

Bureau

et al. 2017

British J Pharmacology

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This article, contributed by members of the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR) subcommittee for the QRFP receptor, confirms the existing nomenclature for this receptor, and reviews our current understanding of its structure, pharmacology and functions, and likely physiological roles in health and disease. More information on this receptor can be found in the Concise Guide to PHARMACOLOGY The RFamide neuropeptide 26RFa was first isolated from the brain of the European green frog on the basis of cross-reactivity with antibodies raised against bovine neuropeptide FF (NPFF). 26RFa and its N-terminally extended form glutamine RF-amide peptide (QRFP) have been identified as cognate ligands of the former orphan receptor GPR103, now renamed glutamine RF-amide peptide receptor (QRFP receptor). The 26RFa/QRFP precursor has been characterized in various mammalian and non-mammalian species. In the brain of mammals, including humans, 26RFa/QRFP mRNA is almost exclusively expressed in hypothalamic nuclei. The 26RFa/QRFP transcript is also present in various organs especially in endocrine glands. While humans express only one QRFP receptor, two isoforms are present in rodents. The QRFP receptor genes are widely expressed in the CNS and in peripheral tissues, notably in bone, heart, kidney, pancreas and testis. Structure-activity relationship studies have led to the identification of low MW peptidergic agonists and antagonists of QRFP receptor. Concurrently, several selective non-peptidic antagonists have been designed from high-throughput screening hit optimization. Consistent with the widespread distribution of QRFP receptor mRNA and 26RFa binding sites, 26RFa/QRFP exerts a large range of biological activities, notably in the control of energy homeostasis, bone formation and nociception that are mediated by QRFP receptor or NPFF2. The present report reviews the current knowledge concerning the 26RFa/QRFP-QRFP receptor system and discusses the potential use of selective QRFP receptor ligands for therapeutic applications.

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RF-amide neuropeptides and their receptors in Mammals: Pharmacological properties, drug development and main physiological functions

Cited by 51 publications

References 609 publications

Differential response patterns of kisspeptin and RFamide‐related peptide to photoperiod and sex steroid feedback in the Djungarian hamster (Phodopus sungorus)

Differential response patterns of kisspeptin and RFamide‐related peptide to photoperiod and sex steroid feedback in the Djungarian hamster (Phodopus sungorus)

The Neuroendocrine Regulation of Food Intake in Fish: A Review of Current Knowledge

The Arg–Phe‐amide peptide 26RFa/glutamine RF‐amide peptide and its receptor: IUPHAR Review 24

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