Research ArticlePharmacology

Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake

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Science Signaling  31 May 2016:
Vol. 9, Issue 430, pp. ra55
DOI: 10.1126/scisignal.aac8035

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, selectively bound to GPR171 and required GPR171 to stimulate a response in cultured cells and in mice. This drug, when delivered by injection into the periphery, stimulated food intake and increased body weight in a manner dependent on GPR171. Thus, not only is this drug useful in exploring the functions of GPR171, but this study demonstrates the utility of virtual screening to identify small molecules that regulate appetite.

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