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GPR120: Mechanism of action, role and potential for medical applications.
Postępy Higieny i Medycyny Doświadczalnej Pub Date : 2017-11-28 , DOI: 10.5604/01.3001.0010.5809
Hanna Karakuła-Juchnowicz 1 , Joanna Róg 2 , Dariusz Juchnowicz 3 , Justyna Morylowska-Topolska 4
Affiliation  

G protein-coupled receptors (GPCRs) constitute a family of transmembrane proteins that mediate many cellular processes. GPR120/FFAR4, a receptor from this family that is activated by fatty acids, has received considerable attention recently. This paper presents a literature review concerning the role of GPR120 and its mechanism of action in animal and human studies as well as the potential use of GPR120 for the treatment of chronic diseases. Two electronic databases - Medline and Google Scholar - were searched for available studies addressing the review topic that were written in English and published from 2000 to June 2017. The following key terms were used in the search: GPR120, FFA4, GPR120 agonist, PUFAs, EPA, DHA, adipocyte, obesity, hyperlipidemia, inflammation, cancer, diabetes, insulin resistance, taste, atherogenesis, hepatis, central nervous system. In humans, GPR120 expression is expressed in macrophages, eosinophils, and adipose tissue, in cells of the tongue, liver, lungs, small and large intestine, gastric mucosa, and pancreas, in the central nervous system and placental microvilli. Medium- and long-chain fatty acids act as ligands for the receptor. Through the internalization of beta-arrestin-2 complex and the inhibition of NF-κB, GPR120 mediates the activation of the cell's anti-inflammatory mechanisms. The receptor is also involved in the maturation of adipocytes, the modulation of insulin signalling pathways, the regulation of glucose metabolism, and the secretion of intestinal hormones. GPR120 is a promising target for the treatment of numerous diseases, whose pathophysiology is associated with low-grade inflammation. As a result of intensive searches, a likely group of synthetic agonists of the receptor was determined with potential therapeutic applications in conditions such as obesity, impaired carbohydrate metabolism, inflammatory bowel diseases, cancer, mental disorders.

中文翻译:

GPR120:作用机制,作用和在医疗领域的潜力。

G蛋白偶联受体(GPCR)构成了介导许多细胞过程的跨膜蛋白家族。GPR120 / FFAR4是该家族的一种被脂肪酸激活的受体,最近受到了极大的关注。本文介绍了有关GPR120在动物和人类研究中的作用及其作用机理的文献综述,以及GPR120在治疗慢性疾病中的潜在用途。搜索了两个电子数据库-Medline和Google Scholar,以查找针对该评论主题的可用研究,这些研究以英文撰写并于2000年至2017年6月发布。搜索中使用了以下关键术语:GPR120,FFA4,GPR120激动剂,PUFA, EPA,DHA,脂肪细胞,肥胖症,高脂血症,炎症,癌症,糖尿病,胰岛素抵抗,味道,动脉粥样硬化,肝炎,中枢神经系统。在人类中,GPR120表达在巨噬细胞,嗜酸性粒细胞和脂肪组织,舌,肝,肺,小肠和大肠,胃粘膜和胰腺的细胞,中枢神经系统和胎盘微绒毛中表达。中链和长链脂肪酸充当受体的配体。通过β-arrestin-2复合物的内在化和对NF-κB的抑制,GPR120介导了细胞抗炎机制的激活。该受体还参与脂肪细胞的成熟,胰岛素信号通路的调节,葡萄糖代谢的调节以及肠激素的分泌。GPR120是治疗多种疾病的有希望的靶标,其病理生理学与低度炎症相关。经过大量搜索,
更新日期:2019-11-01
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