Department of Pharmacology, Max Planck Institute for Heart and Lung Research, Ludwigstrasse 43, 61231 Bad Nauheim, Germany.
Nat Rev Drug Discov. 2012 Aug;11(8):603-19. doi: 10.1038/nrd3777. Epub 2012 Jul 13.
Several G protein-coupled receptors (GPCRs) that are activated by intermediates of energy metabolism - such as fatty acids, saccharides, lactate and ketone bodies - have recently been discovered. These receptors are able to sense metabolic activity or levels of energy substrates and use this information to control the secretion of metabolic hormones or to regulate the metabolic activity of particular cells. Moreover, most of these receptors appear to be involved in the pathophysiology of metabolic diseases such as diabetes, dyslipidaemia and obesity. This Review summarizes the functions of these metabolite-sensing GPCRs in physiology and disease, and discusses the emerging pharmacological agents that are being developed to target these GPCRs for the treatment of metabolic disorders.
近年来发现了一些可被能量代谢中间产物激活的 G 蛋白偶联受体（GPCR），如脂肪酸、糖、乳酸和酮体。这些受体能够感知代谢活性或能量底物水平，并利用这些信息来控制代谢激素的分泌或调节特定细胞的代谢活性。此外，这些受体中的大多数似乎都与代谢性疾病（如糖尿病、血脂异常和肥胖症）的病理生理学有关。本综述总结了这些代谢物感应 GPCR 在生理学和疾病中的功能，并讨论了正在开发的新兴药物，这些药物被设计用来靶向这些 GPCR 以治疗代谢紊乱。
