Wang Jue, Xiao RuiPing
Institute of Molecular Medicine, Peking University, Beijing, 100871, China,
Sci China Life Sci. 2014 Jul;57(7):672-80. doi: 10.1007/s11427-014-4694-2. Epub 2014 Jun 26.
G-protein coupled receptors (GPCRs) compromise the largest membrane protein superfamily which play vital roles in physiological and pathophysiological processes including energy homeostasis. Moreover, they also represent the up-to-date most successful drug target. The gut hormone GPCRs, such as glucagon receptor and GLP-1 receptor, have been intensively studied for their roles in metabolism and respective drugs have developed for the treatment of metabolic diseases such as type 2 diabetes (T2D). Along with the advances of biomedical research, more GPCRs have been found to play important roles in the regulation of energy homeostasis from nutrient sensing, appetite control to glucose and fatty acid metabolism with various mechanisms. The investigation of their biological functions will not only improve our understanding of how our body keeps the balance of energy intake and expenditure, but also highlight the possible drug targets for the treatment of metabolic diseases. The present review summarizes GPCRs involved in the energy control with special emphasis on their pathophysiological roles in metabolic diseases and hopefully triggers more intensive and systematic investigations in the field so that a comprehensive network control of energy homeostasis will be revealed, and better drugs will be developed in the foreseeable future.
G蛋白偶联受体（GPCRs）构成了最大的膜蛋白超家族，在包括能量稳态在内的生理和病理生理过程中发挥着至关重要的作用。此外，它们也是目前最成功的药物靶点。肠道激素GPCRs，如胰高血糖素受体和GLP-1受体，因其在代谢中的作用而受到深入研究，并且已经开发出相应药物用于治疗2型糖尿病（T2D）等代谢性疾病。随着生物医学研究的进展，人们发现更多的GPCRs在能量稳态调节中发挥重要作用，其机制涵盖从营养感知、食欲控制到葡萄糖和脂肪酸代谢等多个方面。对它们生物学功能的研究不仅将增进我们对身体如何维持能量摄入与消耗平衡的理解，还将凸显出治疗代谢性疾病的潜在药物靶点。本综述总结了参与能量控制的GPCRs，特别强调它们在代谢性疾病中的病理生理作用，希望能引发该领域更深入、系统的研究，从而揭示能量稳态的全面网络调控机制，并在可预见的未来开发出更好的药物。
