2. Academic Validation
  3. Identification of GPR83 as the receptor for the neuroendocrine peptide PEN

Identification of GPR83 as the receptor for the neuroendocrine peptide PEN

  • Sci Signal. 2016 Apr 26;9(425):ra43. doi: 10.1126/scisignal.aad0694.
Ivone Gomes 1,  Erin N Bobeck 1,  Elyssa B Margolis 2,  Achla Gupta 1,  Salvador Sierra 1,  Amanda K Fakira 1,  Wakako Fujita 1,  Timo D Müller 3,  Anne Müller 4,  Matthias H Tschöp 3,  Gunnar Kleinau 4,  Lloyd D Fricker 5,  Lakshmi A Devi 6
Affiliations

Affiliations

  • 1 Department of Pharmacology and Systems Therapeutics, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.
  • 2 Department of Neurology, University of California, San Francisco, San Francisco, CA 94158, USA.
  • 3 Institute for Diabetes and Obesity, Helmholtz Diabetes Center, Helmholtz Zentrum München, German Research Center for Environmental Health (GmbH), 85764 Neuherberg, Germany. Division of Metabolic Diseases, Department of Medicine, Technische Universität München, 80333 Munich, Germany.
  • 4 Institut für Experimentelle Pädiatrische Endokrinologie, Charité-Universitätsmedizin, 13125 Berlin, Germany.
  • 5 Department of Molecular Pharmacology, Albert Einstein College of Medicine, Bronx, NY 10461, USA.
  • 6 Department of Pharmacology and Systems Therapeutics, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA. Friedman Brain Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA. lakshmi.devi@mssm.edu.
PMID: 27117253 DOI: 10.1126/scisignal.aad0694
Abstract

PEN is an abundant peptide in the brain that has been implicated in the regulation of feeding. We identified a receptor for PEN in mouse hypothalamus and Neuro2A cells. PEN bound to and activated GPR83, a G protein (heterotrimeric guanine nucleotide)-binding protein)-coupled receptor (GPCR). Reduction of GPR83 expression in mouse brain and Neuro2A cells reduced PEN binding and signaling, consistent with GPR83 functioning as the major receptor for PEN. In some brain regions, GPR83 colocalized with GPR171, a GPCR that binds the neuropeptide bigLEN, another neuropeptide that is involved in feeding and is generated from the same precursor protein as is PEN. Coexpression of these two receptors in cell lines altered the signaling properties of each receptor, suggesting a functional interaction. Our data established PEN as a neuropeptide that binds GPR83 and suggested that these two ligand-receptor systems-PEN-GPR83 and bigLEN-GPR171-may be functionally coupled in the regulation of feeding.

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