Mechanism of action of the bile acid receptor TGR5 in obesity.
10.1016/j.apsb.2023.11.011
- Author:
Weijun LUN
1
;
Qihao YAN
1
;
Xinghua GUO
1
;
Minchuan ZHOU
1
;
Yan BAI
2
;
Jincan HE
2
;
Hua CAO
3
;
Qishi CHE
4
;
Jiao GUO
5
;
Zhengquan SU
1
Author Information
1. Guangdong Engineering Research Center of Natural Products and New Drugs, Guangdong Provincial University Engineering Technology Research Center of Natural Products and Drugs, Guangdong Pharmaceutical University, Guangzhou 510006, China.
2. School of Public Health, Guangdong Pharmaceutical University, Guangzhou 510310, China.
3. School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Zhongshan 528458, China.
4. Guangzhou Rainhome Pharm & Tech Co., Ltd., Science City, Guangzhou 510663, China.
5. Guangdong Metabolic Disease Research Center of Integrated Chinese and Western Medicine, Key Laboratory of Glucolipid Metabolic Disorder, Ministry of Education of China, Guangdong TCM Key Laboratory for Metabolic Diseases, Guangdong Pharmaceutical University, Guangzhou 510006, China.
- Publication Type:Review
- Keywords:
Appetite;
Bile acids;
GLP-1;
Inflammation;
Ligand;
Metabolism;
Obesity;
TGR5
- From:
Acta Pharmaceutica Sinica B
2024;14(2):468-491
- CountryChina
- Language:English
-
Abstract:
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.
