Kimura Ikuo, Inoue Daisuke, Hirano Kanako, Tsujimoto Gozoh
Department of Applied Biological Science, Graduate School of Agriculture, Tokyo University of Agriculture and Technology , Tokyo , Japan ; Department of Pharmacogenomics, Kyoto University Graduate School of Pharmaceutical Science , Kyoto , Japan.
Department of Pharmacogenomics, Kyoto University Graduate School of Pharmaceutical Science , Kyoto , Japan.
Front Endocrinol (Lausanne). 2014 Jun 5;5:85. doi: 10.3389/fendo.2014.00085. eCollection 2014.
Free fatty acids (FFAs) are essential nutrients and act as signaling molecules in various cellular processes via binding with FFA receptors. Of these receptors, GPR43 is activated by short-chain fatty acids (SCFAs; e.g., acetate, propionate, and butyrate). During feeding, SCFAs are produced by microbial fermentation of dietary fiber in the gut, and these SCFAs become important energy sources for the host. The gut microbiota affects nutrient acquisition and energy regulation of the host and can influence the development of obesity, insulin resistance, and diabetes. Recently, GPR43 has been reported to regulate host energy homeostasis in the gastrointestinal tract and adipose tissues. Hence, GPR43 is also thought to be a potential drug target for metabolic disorders, such as obesity and diabetes. In this review, we summarize the identification, structure, and activities of GPR43, with a focus on host energy regulation, and present an essential overview of our current understanding of its physiological roles in host energy regulation that is mediated by gut microbiota. We also discuss the potential for GPR43 as a therapeutic target.
游离脂肪酸（FFAs）是必需营养素，并通过与游离脂肪酸受体结合在各种细胞过程中充当信号分子。在这些受体中，GPR43被短链脂肪酸（SCFAs；例如乙酸盐、丙酸盐和丁酸盐）激活。在进食期间，SCFAs由肠道中膳食纤维的微生物发酵产生，这些SCFAs成为宿主的重要能量来源。肠道微生物群影响宿主的营养获取和能量调节，并可影响肥胖、胰岛素抵抗和糖尿病的发展。最近，有报道称GPR43可调节胃肠道和脂肪组织中的宿主能量稳态。因此，GPR43也被认为是肥胖和糖尿病等代谢紊乱的潜在药物靶点。在这篇综述中，我们总结了GPR43的鉴定、结构和活性，重点关注宿主能量调节，并对我们目前对其在肠道微生物群介导的宿主能量调节中的生理作用的理解进行了必要概述。我们还讨论了GPR43作为治疗靶点的潜力。
