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

Jérôme Leprince, Didier Bagnol, Ronan Bureau, Shoji Fukusumi, Riccarda Granata, Shuji Hinuma, Dan Larhammar, Stefany Primeaux, Jana Sopkova-de Oliveiras Santos, Kazuyoshi Tsutsui, Kazuyoshi Ukena, Hubert Vaudry

    Research output: Contribution to journalReview article

    11 Citations (Scopus)

    Abstract

    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.

    Original languageEnglish
    Pages (from-to)3573-3607
    Number of pages35
    JournalBritish Journal of Pharmacology
    Volume174
    Issue number20
    DOIs
    Publication statusPublished - 2017

    Fingerprint

    Peptide Receptors
    Glutamine
    Amides
    Rana clamitans
    Ligands
    Endocrine Glands
    Messenger RNA
    Peptides
    Nociception
    Brain
    Neuropeptides
    Osteogenesis
    Testis
    Pancreas
    Mammals
    Rodentia
    Protein Isoforms
    Homeostasis
    Binding Sites
    Kidney

    ASJC Scopus subject areas

    • Pharmacology

    Cite this

    Leprince, J., Bagnol, D., Bureau, R., Fukusumi, S., Granata, R., Hinuma, S., ... Vaudry, H. (2017). The Arg–Phe-amide peptide 26RFa/glutamine RF-amide peptide and its receptor: IUPHAR Review 24. British Journal of Pharmacology, 174(20), 3573-3607. https://doi.org/10.1111/bph.13907

    The Arg–Phe-amide peptide 26RFa/glutamine RF-amide peptide and its receptor : IUPHAR Review 24. / Leprince, Jérôme; Bagnol, Didier; Bureau, Ronan; Fukusumi, Shoji; Granata, Riccarda; Hinuma, Shuji; Larhammar, Dan; Primeaux, Stefany; Sopkova-de Oliveiras Santos, Jana; Tsutsui, Kazuyoshi; Ukena, Kazuyoshi; Vaudry, Hubert.

    In: British Journal of Pharmacology, Vol. 174, No. 20, 2017, p. 3573-3607.

    Research output: Contribution to journalReview article

    Leprince, J, Bagnol, D, Bureau, R, Fukusumi, S, Granata, R, Hinuma, S, Larhammar, D, Primeaux, S, Sopkova-de Oliveiras Santos, J, Tsutsui, K, Ukena, K & Vaudry, H 2017, 'The Arg–Phe-amide peptide 26RFa/glutamine RF-amide peptide and its receptor: IUPHAR Review 24', British Journal of Pharmacology, vol. 174, no. 20, pp. 3573-3607. https://doi.org/10.1111/bph.13907
    Leprince, Jérôme ; Bagnol, Didier ; Bureau, Ronan ; Fukusumi, Shoji ; Granata, Riccarda ; Hinuma, Shuji ; Larhammar, Dan ; Primeaux, Stefany ; Sopkova-de Oliveiras Santos, Jana ; Tsutsui, Kazuyoshi ; Ukena, Kazuyoshi ; Vaudry, Hubert. / The Arg–Phe-amide peptide 26RFa/glutamine RF-amide peptide and its receptor : IUPHAR Review 24. In: British Journal of Pharmacology. 2017 ; Vol. 174, No. 20. pp. 3573-3607.
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    AU - Bureau, Ronan

    AU - Fukusumi, Shoji

    AU - Granata, Riccarda

    AU - Hinuma, Shuji

    AU - Larhammar, Dan

    AU - Primeaux, Stefany

    AU - Sopkova-de Oliveiras Santos, Jana

    AU - Tsutsui, Kazuyoshi

    AU - Ukena, Kazuyoshi

    AU - Vaudry, Hubert

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