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Small-Molecule Neuromedin U Receptor 2 Agonists Suppress Food Intake and Decrease Visceral Fat in Animal Models.

Pharmacol Res Perspect. 2018-10; 
SampsonCatherine M,KasperJames M,FelsingDaniel E,RavalSweta R,YeNa,WangPingyuan,PatrikeevIgor,RyttingErik,ZhouJia,AllenJohn A,HommelJonath
Products/Services Used Details Operation
… verified using HPLC analysis. 2.3 Cell culture. Human Embryonic Kidney 293 (HEK293) cells and HEK293 stably expressing the human NMUR2 receptor (C11 cells) were obtained from GenScript (cat no. M00244 Piscataway, NJ …

摘要

Obesity is a growing public health concern, with 37.5% of the adult population in need of therapeutics that are more efficacious with a better side effect profile. An innovative target in this regard is neuromedin U, a neuropeptide shown to suppress food intake and attenuate weight gain in animal models. These effects of neuromedin U on feeding behavior are thought to be related to agonism at the centrally expressed neuromedin U receptor 2 (NMUR2). As peptides present unique challenges that limit their therapeutic potential, the discovery of small-molecule NMUR2 agonists is needed to validate the targets therapeutic value, but to date, none have been evaluated in any animal model of disease. We theref... More

关键词

Neuromedin U receptor 2,calcium,cyclic AMP,feeding,high‐fat diet,obesity,small‐molecule ago