In a study published recently in Nature,Sass,Ma,and colleagues describe the neurokinin 2 receptor(NK2R),a G protein-coupled receptor(GPCR),as a novel regulator of food intake as well as energy expenditure,and develop ...In a study published recently in Nature,Sass,Ma,and colleagues describe the neurokinin 2 receptor(NK2R),a G protein-coupled receptor(GPCR),as a novel regulator of food intake as well as energy expenditure,and develop and characterize selective agonists that effectively activate NK2R to promote weight loss.Most interestingly,the authors bridge the gap between rodents and primates,raising hopes for novel treatment options.1 Although obesity cases are continuously rising,thereby contributing to major health problems,long-term effective treatment options are still limited.However,it is well established that GPCRs and their pathways are involved in the regulation of different processes controlling appetite,food intake,or energy homeostasis.Thus,several receptors expressed in neurons governing food intake have been proposed to be promising targets for body weight reduction.However,currently the only GPCR agonists approved for obesity treatment are targeting incretin receptors(receptors for glucagon-like peptide-1(GLP1R),glucose-dependent insulinotropic peptide(GIP),glucagon(GCGR))(Fig.1).展开更多
基金supported by the German Diabetes Association(DDG)(D.T.)the German Research Foundation(DFG)in CRC1423/2(project number 421152132,C04(S.P.)).
文摘In a study published recently in Nature,Sass,Ma,and colleagues describe the neurokinin 2 receptor(NK2R),a G protein-coupled receptor(GPCR),as a novel regulator of food intake as well as energy expenditure,and develop and characterize selective agonists that effectively activate NK2R to promote weight loss.Most interestingly,the authors bridge the gap between rodents and primates,raising hopes for novel treatment options.1 Although obesity cases are continuously rising,thereby contributing to major health problems,long-term effective treatment options are still limited.However,it is well established that GPCRs and their pathways are involved in the regulation of different processes controlling appetite,food intake,or energy homeostasis.Thus,several receptors expressed in neurons governing food intake have been proposed to be promising targets for body weight reduction.However,currently the only GPCR agonists approved for obesity treatment are targeting incretin receptors(receptors for glucagon-like peptide-1(GLP1R),glucose-dependent insulinotropic peptide(GIP),glucagon(GCGR))(Fig.1).