The roles of G-protein-coupled receptors (GPCRs) in the control of food intake and energy expenditure are being increasingly recognized, and new drug candidates targeting these receptors are making their entry into the clinic. GPCRs exert their action along the various sites of regulation of energy homeostasis control including the central nervous system, the pancreas, the gut and fat cells. Exciting new data about GPCRs recognizing and mediating the effects of lipid mediators and concerning receptors for which no endogenous ligands have been identified yet open new exciting avenues for the validation of additional drug targets. In addition, recently developed paradigms around the concepts of cross-talk regulation and functional selectivity should lead to the development of drugs with improved therapeutic efficacy and reduced undesirable effects. Some of these promising discoveries are discussed in the present article and accompanying papers.

G 蛋白偶联受体 (GPCRs) 在控制食物摄入和能量消耗中的作用正日益得到认可，针对这些受体的新候选药物正在进入临床。GPCR 沿着能量稳态控制的各个调节位点发挥作用，包括中枢神经系统、胰腺、肠道和脂肪细胞。关于 GPCR 识别和介导脂质介质作用的激动人心的新数据，以及关于尚未鉴定出内源性配体的受体的新数据，为验证其他药物靶点开辟了新的激动人心的途径。此外，最近围绕串扰调节和功能选择性概念开发的范例应导致开发具有改善治疗效果和减少不良反应的药物。