The Neuropeptide 26RFa (QRFP) and Its Role in the Regulation of Energy Homeostasis: A Mini-Review

Chartrel, Nicolas; Picot, Marie Christine; Medhi, Mouna El; Arabo, Arnaud; Berrahmoune, Hind; Dionne‐Laporte, Alexandre; Maucotel, Julie; Anouar, Youssef; Prévost, Gaëtan

doi:10.3389/fnins.2016.00549

Cited by 37 publications

(33 citation statements)

References 42 publications

(94 reference statements)

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“…GPR103 mRNA is also detected in a number of hypothalamic and extrahypothalamic regions (Takayasu et al, ; Bruzzone et al, ). Consistent with the widespread distribution of the receptor, 26RFa and QRFP have been found to regulate many physiological functions including energy homeostasis (Chartrel et al, ), bone formation (Baribault et al, ), hypothalamo‐pituitary‐gonadal activity (Navarro et al, ; Patel et al, ), insulin secretion (Egido et al, ; Granata et al, ; Prévost et al, ), locomotor activity (Do Rego et al, ) and analgesia (Yamamoto et al, ). The potential implication of these neuropeptides in various pathologies has prompted medicinal chemists to study the structure–activity relationships (SAR) of 26RFa in order to design selective agonists and antagonists (Le Marec et al, ; Neveu et al, , ; Georgsson et al, , ; Nordqvist et al, ).…”

Section: Introductionmentioning

confidence: 81%

“…26RFa/QRFP and its receptor have been shown to play a role in energy balance and glucose metabolism, the majority of studies indicating that central administration of 26RFa increases energy intake (Chartrel et al, ; Do Rego et al, ; Moriya et al, ; Takayasu et al, ; Primeaux et al, ; Lectez et al, ; Mulumba et al, ; Primeaux, ; Primeaux et al, ; Chartrel et al, ; Schreiber et al, ). In mice and rats, i.c.v.…”

Section: Biological and Pharmacological Effects Of Qfrp Peptidesmentioning

confidence: 99%

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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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Section: Introductionmentioning

confidence: 81%

Section: Biological and Pharmacological Effects Of Qfrp 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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“…Accumulated data obtained during the last decade have promoted the evidence that the neuropeptide 26RFa plays a key role in the control of feeding behaviour (10, 13, 14) and the regulation of glucose homeostasis (24, 25, 27, 28). Supporting this notion, it has been recently shown that acute administration of a GPR103 (the 26RFa receptor) antagonist decreases food intake (30) and reduces the global glucose-induced incretin effect as well as the insulin sensitivity (28).…”

Section: Discussionmentioning

confidence: 99%

“…26RFa (also referred to as QRFP) is a hypothalamic neuropeptide discovered concurrently by us and others (10-12). 26RFa has been characterized in all vertebrate phyla including human (13, 14), and identified as the cognate ligand of the human orphan G protein-coupled receptor, GPR103 (11-13,15, 16). Neuroanatomical observations revealed that 26RFa- and GPR103-expressing neurons are primarily localized in hypothalamic nuclei involved in the control of feeding behaviour (10,11,15,17,18).…”

Section: Introductionmentioning

confidence: 99%

Glucose homeostasis is impaired in mice deficient for the neuropeptide 26RFa (QRFP)

Mehdi

Takhlidjt

Khiar

et al. 2019

Preprint

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1 Introduction: 26RFa (QRFP) is a biologically active peptide that has been found to control 2 feeding behaviour by stimulating food intake, and to regulate glucose homeostasis by acting as 3 an incretin. The aim of the present study was thus to investigate the impact of 26RFa gene 4 knockout on the regulation of energy and glucose metabolism. 5Research design and methods: 26RFa mutant mice were generated by homologous 6 recombination, in which the entire coding region of prepro-26RFa was replaced by the iCre 7 sequence. Energy and glucose metabolism was evaluated through measurement of 8 complementary parameters. Morphological and physiological alterations of the pancreatic islets 9 were also investigated. 10Results: Our data do not reveal significant alteration of energy metabolism in the 26RFa-11 deficient mice except the occurrence of an increased basal metabolic rate. By contrast, 26RFa 12 mutant mice exhibit an altered glycemic phenotype with an increased hyperglycemia after a 13 glucose challenge associated with an impaired insulin production, and an elevated hepatic 14 glucose production. 2D and 3D immunohistochemical experiments indicate that the insulin 15 content of pancreatic β cells is much lower in the 26RFa -/mice as compared to the wild-type 16 littermates. 17Conclusion: Disruption of the 26RFa gene induces substantial alteration in the regulation of 18 glucose homeostasis with, in particular, a deficit in insulin production by the pancreatic islets. 19These findings further support the notion that 26RFa is an important regulator of glucose 20 homeostasis. 21 22

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“…It is striking that many bilaterian neuropeptide GPCRs closely related to Clytia MIHR are known for roles in regulating feeding and nutritional balance. In mammals these include GPR83/PEN [50] as well as QRFP receptors and Neuropeptide Y receptors, which provide important links between metabolic state and reproductive regulation [51][52][53], in conjunction with GnIH signalling [54]. Related hormone receptor families from protostomes are also known for regulating feeding, including those for Drosophila Leucokinin [55] and Luqins in arthropods (RYamides) and nematodes [49,56].…”

Section: An Ancient Regulatory System Linking Reproduction and Nutritmentioning

confidence: 99%

A G-protein-coupled receptor mediates neuropeptide-induced oocyte maturation in the jellyfish Clytia

Artigas

Lapébie

Leclère

et al. 2019

Preprint

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The reproductive hormones that trigger oocyte meiotic maturation and release from the ovary vary greatly between animal species. Identification of receptors for these Maturation Inducing Hormones (MIHs), and understanding how they initiate the largely conserved maturation process, remain important challenges. In hydrozoan cnidarians including the jellyfish Clytia hemisphaerica, MIH comprises neuropeptides released from somatic cells of the gonad. We identified the receptor (MIHR) for these MIH neuropeptides in Clytia using cell culture-based "deorphanization" of candidate oocyte-expressed GPCRs. MIHR mutant jellyfish generated using CRISPR-Cas9 had severe defects in gamete development or in spawning both in males and females. Female gonads, or oocytes isolated from MIHR mutants, failed to respond to synthetic MIH. Treatment with the cAMP analogue 5'Br-cAMP to mimic cAMP rise at maturation onset rescued meiotic maturation and spawning. Injection of inhibitory antibodies to Gα S into wild type oocytes phenocopied the MIHR mutants. These results provide the molecular links between MIH stimulation and meiosis initiation in hydrozoan oocytes. Molecular phylogeny grouped Clytia MIHR with a subset of bilaterian neuropeptide receptors including Neuropeptide Y, Gonadotropin Inhibitory Hormone, pyroglutamylated RFamide and Luqin, all upstream regulators of sexual reproduction. This identification and functional characterisation of a cnidarian peptide GPCR advances our understanding of oocyte maturation initiation and sheds light on the evolution of neuropeptidehormone systems. Non-standard Abbreviations: MIH -Maturation Inducing Hormone; GVBD -Germinal VesicleBreakdown.

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The Neuropeptide 26RFa (QRFP) and Its Role in the Regulation of Energy Homeostasis: A Mini-Review

Cited by 37 publications

References 42 publications

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

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

Glucose homeostasis is impaired in mice deficient for the neuropeptide 26RFa (QRFP)

A G-protein-coupled receptor mediates neuropeptide-induced oocyte maturation in the jellyfish Clytia

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