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Metabolic Functions of G Protein-Coupled Receptors in Hepatocytes—Potential Applications for Diabetes and NAFLD
Biomolecules ( IF 5.5 ) Pub Date : 2020-10-15 , DOI: 10.3390/biom10101445
Takefumi Kimura 1, 2 , Sai P Pydi 1 , Jonathan Pham 1 , Naoki Tanaka 3, 4
Affiliation  

G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of extracellular ligands. Understanding how GPCRs work at the molecular level has important therapeutic implications, as 30–40% of the drugs currently in clinical use mediate therapeutic effects by acting on GPCRs. Like many other cell types, liver function is regulated by GPCRs. More than 50 different GPCRs are predicted to be expressed in the mouse liver. However, knowledge of how GPCRs regulate liver metabolism is limited. A better understanding of the metabolic role of GPCRs in hepatocytes, the dominant constituent cells of the liver, could lead to the development of novel drugs that are clinically useful for the treatment of various metabolic diseases, including type 2 diabetes, nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH). In this review, we describe the functions of multiple GPCRs expressed in hepatocytes and their role in metabolic processes.

中文翻译:

G蛋白偶联受体在肝细胞中的代谢功能—糖尿病和NAFLD的潜在应用

G蛋白偶联受体(GPCR)是介导细胞外配体功能的细胞表面受体。了解GPCR在分子水平上的作用具有重要的治疗意义,因为目前临床使用的药物中有30-40%通过作用于GPCR来介导治疗作用。像许多其他细胞类型一样,肝功能受GPCR调节。预计将在小鼠肝脏中表达50多种不同的GPCR。然而,关于GPCR如何调节肝脏代谢的知识是有限的。更好地了解GPCR在肝细胞(肝脏的主要组成细胞)中的代谢作用,可能会导致开发出在临床上可用于治疗各种代谢性疾病(包括2型糖尿病)的新型药物,非酒精性脂肪肝疾病(NAFLD)和非酒精性脂肪性肝炎(NASH)。在这篇综述中,我们描述了肝细胞中表达的多个GPCR的功能及其在代谢过程中的作用。
更新日期:2020-10-15
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