G protein-coupled receptors in energy homeostasis

Abstract

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-protein coupled receptor, energy homeostasis, metabolism

Bifidobacterium animalis subsp. lactis A6 Enhances Fatty Acid β-Oxidation of Adipose Tissue to Ameliorate the Development of Obesity in Mice

“…G protein-coupled receptors (GPRs) play pivotal roles in cell signaling to maintain energy homeostasis [21,22]. They are known to regulate various adipocyte functions, including FAO and thermogenesis [23].…”

Inhibition of GPR39 restores defects in endothelial cell–mediated neovascularization under the duress of chronic hyperglycemia: Evidence for regulatory roles of the sonic hedgehog signaling axis

“…However, increasing evidence has suggested that GPR39 also displays ligand-independent constitutive activities. In population studies, associations have been found between polymorphic variants of GPR39 and the onset of pathologies, including cancer, cardiovascular diseases, nutrition, and energy homeostasis ( 13 – 16 ). In animal studies, GPR39 has been reported to participate in adipocyte metabolism ( 17 ) and regulate pancreatic islet function ( 18 ).…”