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Br J Pharmacol. 2017 Oct;174(20):3573-3607. doi: 10.1111/bph.13907. Epub 2017 Sep 8.

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

Author information

1
INSERM U1239, Laboratory of Neuronal and Neuroendocrine Differentiation and Communication, Normandy University, Rouen, France.
2
CNS Drug Discovery, Arena Pharmaceuticals Inc., San Diego, CA, USA.
3
Normandy Centre for Studies and Research on Medicines (CERMN), Normandy University, Caen, France.
4
International Institute for Integrative Sleep Medicine (WPI-IIIS), University of Tsukuba, Tsukuba, Ibaraki, Japan.
5
Laboratory of Molecular and Cellular Endocrinology, Division of Endocrinology, Diabetes and Metabolism, Department of Medical Sciences, University of Torino, Torino, Italy.
6
Department of Food and Nutrition, Faculty of Human Life Science, Senri Kinran University, Suita-City, Osaka, Japan.
7
Department of Neuroscience, Unit of Pharmacology, Uppsala University, Uppsala, Sweden.
8
Department of Physiology, Joint Diabetes, Endocrinology & Metabolism Center, Louisiana State University Health Sciences Center, New Orleans, LA, USA.
9
Laboratory of Integrative Brain Sciences, Department of Biology, Waseda University, Center for Medical Life Science, Tokyo, Japan.
10
Section of Behavioral Sciences, Graduate School of Integrated Arts and Sciences, Hiroshima University, Higashi-Hiroshima, Japan.

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.

PMID:
28613414
PMCID:
PMC5610166
DOI:
10.1111/bph.13907
[Indexed for MEDLINE]
Free PMC Article

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