A neuropeptide ligand of the G protein-coupled receptor GPR103 regulates feeding, behavioral arousal, and blood pressure in mice.

Proceedings of the National Academy of Sciences of the United States of America
Shinobu TakayasuJuro Sakai

Abstract

Here, we report the isolation and characterization of an endogenous peptide ligand of GPR103 from rat brains. The purified peptide was found to be the 43-residue RF-amide peptide QRFP. We also describe two mouse homologues of human GPR103, termed mouse GPR103A and GPR103B. QRFP binds and activates the human GPR103, as well as mouse GPR103A and GPR103B, with nanomolar affinities in transfected cells. Systematic in situ hybridization analysis in mouse brains showed that QRFP is expressed exclusively in the periventricular and lateral hypothalamus, whereas the two receptor mRNAs are distinctly localized in various brain areas without an overlap to each other. When administered centrally in mice, QRFP induced feeding behavior, accompanied by increased general locomotor activity and metabolic rate. QRFP-induced food intake was abolished by preadministration of BIBP3226, a specific antagonist for the Y1 neuropeptide Y receptor. Hypothalamic prepro-QRFP mRNA expression was up-regulated upon fasting and in genetically obese ob/ob and db/db mice. Central QRFP administration also evoked highly sustained elevation of blood pressure and heart rate. Our findings suggest that QRFP and GPR103A/B may regulate diverse neuroendocrine and behavio...Continue Reading

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Citations

Jun 1, 2011·Journal of Medicinal Chemistry·Olivier Le MarecJérôme Leprince
Mar 25, 2014·Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology·Qihai XiaoRongping Zhang
Feb 18, 2014·Journal of Molecular Endocrinology·Kazuyoshi UkenaKazuyoshi Tsutsui
Aug 8, 2014·Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology·Hu ShuHaifa Zhang
Dec 3, 2014·General and Comparative Endocrinology·Bo XuDan Larhammar
Apr 11, 2015·Diabetes·Gaëtan PrévostNicolas Chartrel
Jun 12, 2012·Progress in Neurobiology·Ishwar ParharTakashi Kitahashi
Mar 1, 2011·Pharmacology, Biochemistry, and Behavior·Yu OhmuraEdward F Domino
Sep 20, 2015·Brain Research Bulletin·Olga ZagoráczLászló Lénárd
Sep 5, 2012·Molecular Nutrition & Food Research·Tomomi KagebayashiKousaku Ohinata
Oct 12, 2013·Journal of Cellular Physiology·Anna Eisenstein, Katya Ravid
Jun 14, 2012·Brain Research Bulletin·Anita KovácsLászló Lénárd
Aug 7, 2012·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·Jessy AlonzeauNicolas Chartrel
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Jul 23, 2016·Frontiers in Neuroscience·Philip GorwoodJacques Epelbaum

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