論文

2017年

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

British Journal of Pharmacology
  • 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

174
20
開始ページ
3573
終了ページ
3607
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1111/bph.13907
出版者・発行元
John Wiley and Sons Inc.

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.

リンク情報
DOI
https://doi.org/10.1111/bph.13907
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/28613414
ID情報
  • DOI : 10.1111/bph.13907
  • ISSN : 1476-5381
  • ISSN : 0007-1188
  • PubMed ID : 28613414
  • SCOPUS ID : 85029049149

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