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

*この研究の対応する著者

    研究成果: Review article査読

    21 被引用数 (Scopus)

    抄録

    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.

    本文言語English
    ページ(範囲)3573-3607
    ページ数35
    ジャーナルBritish Journal of Pharmacology
    174
    20
    DOI
    出版ステータスPublished - 2017

    ASJC Scopus subject areas

    • 薬理学

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