Mechanism of action of the bile acid receptor TGR5 in obesity

被引:10
|
作者
Lun, Weijun [1 ,2 ]
Yan, Qihao [1 ,2 ]
Guo, Xinghua [1 ,2 ]
Zhou, Minchuan [1 ,2 ]
Bai, Yan [3 ]
He, Jincan [3 ]
Cao, Hua [4 ]
Che, Qishi [5 ]
Guo, Jiao [2 ]
Su, Zhengquan [1 ,2 ]
机构
[1] Guangdong Prov Univ Engn Technol Res Ctr Nat Prod, Guangdong Prov Univ, Guangdong Engn Res Ctr Nat Prod & New Drugs, Engn Technol Res Ctr Nat Prod & Drugs, Guangzhou 510006, Peoples R China
[2] Guangdong Pharmaceut Univ, Guangdong Metab Dis Res Ctr Integrated Chinese & W, Key Lab Glucolipid Metab Disorder, Guangdong TCM Key Lab Metab Dis,Minist Educ China, Guangzhou 510006, Peoples R China
[3] Guangdong Pharmaceut Univ, Sch Publ Hlth, Guangzhou 510310, Peoples R China
[4] Guangdong Pharmaceut Univ, Sch Chem & Chem Engn, Zhongshan 528458, Peoples R China
[5] Guangzhou Rainhome Pharm & Tech Co Ltd, Guangzhou 510663, Peoples R China
关键词
Obesity; TGR5; Bile acids; Ligand; Appetite; Metabolism; GLP-1; Inflammation; BROWN ADIPOSE-TISSUE; DIET-INDUCED OBESITY; THYROID-HORMONE; FATTY LIVER; INSULIN-RESISTANCE; THERAPEUTIC TARGET; NATURAL-PRODUCTS; INTESTINAL MACROPHAGES; CHENODEOXYCHOLIC ACID; BIOLOGICAL EVALUATION;
D O I
10.1016/j.apsb.2023.11.011
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
G protein-coupled receptors (GPCRs) are a large family of membrane protein receptors, and Takeda G protein-coupled receptor 5 (TGR5) is a member of this family. As a membrane receptor, TGR5 is widely distributed in different parts of the human body and plays a vital role in regulating metabolism, including the processes of energy consumption, weight loss and blood glucose homeostasis. Recent studies have shown that TGR5 plays an important role in glucose and lipid metabolism disorders such as fatty liver, obesity and diabetes. With the global obesity situation becoming more and more serious, a comprehensive explanation of the mechanism of TGR5 and filling the gaps in knowledge concerning clinical ligand drugs are urgently needed. In this review, we mainly explain the anti-obesity mechanism of TGR5 to promote the further study of this target, and show the electron microscope structure of TGR5 and review recent studies on TGR5 ligands to illustrate the specific binding between TGR5 receptor binding sites and ligands, which can effectively provide new ideas for ligand research and promote drug research.
引用
收藏
页码:468 / 491
页数:24
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