Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake
@article{Wardman2016IdentificationOA, title={Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake}, author={J. Wardman and I. Gomes and E. Bobeck and Jennifer A. Stockert and Abhijeet Kapoor and P. Bisignano and A. Gupta and M. Mezei and S. Kumar and M. Filizola and L. Devi}, journal={Science Signaling}, year={2016}, volume={9}, pages={ra55 - ra55} }
Stimulation of the receptor GPR171 with a small-molecule ligand results in hyperphagia and weight gain in mice. Discovering chemicals that control appetite Understanding the signals that control hunger and food intake is important given the global increase in metabolic disease. The neuropeptide b-LEN and its receptor GPR171 regulate food intake in mice. Wardman et al. used structural modeling and virtual molecule docking to identify candidate chemical ligands for GPR171. One of these, MS0015203… Expand
Topics from this paper
15 Citations
Orphan neuropeptides and receptors: Novel therapeutic targets.
- Biology, Medicine
- Pharmacology & therapeutics
- 2018
- 8
The BigLEN-GPR171 Peptide Receptor System Within the Basolateral Amygdala Regulates Anxiety-Like Behavior and Contextual Fear Conditioning
- Psychology, Medicine
- Neuropsychopharmacology
- 2017
- 10
- PDF
Carboxypeptidase E and the Identification of Novel Neuropeptides as Potential Therapeutic Targets.
- Chemistry, Medicine
- Advances in pharmacology
- 2018
- 5
Opioid-Induced Signaling and Antinociception Are Modulated by the Recently Deorphanized Receptor, GPR171
- Medicine
- The Journal of Pharmacology and Experimental Therapeutics
- 2019
- 2
- PDF
Quantitative Mass Spectrometry Reveals Food Intake-Induced Neuropeptide Level Changes in Rat Brain: Functional Assessment of Selected Neuropeptides as Feeding Regulators*
- Biology, Medicine
- Molecular & Cellular Proteomics
- 2017
- 7
Neuro-psychopharmacological perspective of Orphan receptors of Rhodopsin (class A) family of G protein-coupled receptors
- Biology, Medicine
- Psychopharmacology
- 2017
- 18
- Highly Influenced
Advances in therapeutic peptides targeting G protein-coupled receptors
- Biology, Medicine
- Nature Reviews Drug Discovery
- 2020
- 18
- PDF
GPR171 Activation Modulates Nociceptor Functions, Alleviating Pathologic Pain
- Medicine
- Biomedicines
- 2021
- 1
- PDF
Discovery of new GPCR ligands to illuminate new biology.
- Biology, Medicine
- Nature chemical biology
- 2017
- 42
- PDF
The G protein‐coupled receptors deorphanization landscape
- Medicine, Chemistry
- Biochemical pharmacology
- 2018
- 29
References
SHOWING 1-10 OF 68 REFERENCES
GPR171 is a hypothalamic G protein-coupled receptor for BigLEN, a neuropeptide involved in feeding
- Biology, Medicine
- Proceedings of the National Academy of Sciences
- 2013
- 39
- PDF
Identification of GPR83 as the receptor for the neuroendocrine peptide PEN
- Biology, Medicine
- Science Signaling
- 2016
- 34
- PDF
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65
- Biology, Computer Science
- Nature
- 2015
- 122
Melanocortin-4 receptor agonists for the treatment of obesity.
- Biology, Medicine
- Current topics in medicinal chemistry
- 2007
- 38
- PDF
Therapeutic potential of neuropeptide Y (NPY) receptor ligands
- Biology, Medicine
- EMBO molecular medicine
- 2010
- 165
- PDF
The fate of P2Y-related orphan receptors: GPR80/99 and GPR91 are receptors of dicarboxylic acids
- Biology, Medicine
- Purinergic Signalling
- 2004
- 19
- PDF
Gpr171, a putative P2Y-like receptor, negatively regulates myeloid differentiation in murine hematopoietic progenitors.
- Biology, Medicine
- Experimental hematology
- 2013
- 13
Structure of the human P2Y12 receptor in complex with an antithrombotic drug
- Chemistry, Medicine
- Nature
- 2014
- 265
- PDF
Rapid, reversible activation of AgRP neurons drives feeding behavior in mice.
- Biology, Medicine
- The Journal of clinical investigation
- 2011
- 836
- PDF