Update on the development of TGR5 agonists for human diseases
文献类型：期刊论文
| 作者 | Jin, Wangrui2,5,6; Zheng, Mingyue1 ; Chen, Yihua2,3,4; Xiong, Hai5,6
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2024-05-05 |
| 卷号 | 271页码:20 |
| 关键词 | Bile acids TGR5 T2DM Gut-targeted TGR5 agonists |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2024.116462 |
| 通讯作者 | Chen, Yihua(chenyihua@kmmu.edu.cn) ; Xiong, Hai(hai.xiong@szu.edu.cn) |
| 英文摘要 | The G protein-coupled bile acid receptor 1 (GPBAR1) or TGR5 is widely distributed across organs, including the small intestine, stomach, liver, spleen, and gallbladder. Many studies have established strong correlations between TGR5 and glucose homeostasis, energy metabolism, immune-inflammatory responses, and gastrointestinal functions. These results indicate that TGR5 has a significant impact on the progression of tumor development and metabolic disorders such as diabetes mellitus and obesity. Targeting TGR5 represents an encouraging therapeutic approach for treating associated human ailments. Notably, the GLP-1 receptor has shown exceptional efficacy in clinical settings for diabetes management and weight loss promotion. Currently, numerous TGR5 agonists have been identified through natural product-based approaches and virtual screening methods, with some successfully progressing to clinical trials. This review summarizes the intricate relationships between TGR5 and various diseases emphasizing recent advancements in research on TGR5 agonists, including their structural characteristics, design tactics, and biological activities. We anticipate that this meticulous review could facilitate the expedited discovery and optimization of novel TGR5 agonists. |
| WOS关键词 | BILE-ACID RECEPTOR ; FATTY LIVER-DISEASE ; IN-VIVO ; CHENODEOXYCHOLIC ACID ; POTENT AGONISTS ; 1 GPBAR1 ; DISCOVERY ; DERIVATIVES ; ACTIVATION ; DESIGN |
| 资助项目 | National Key Research and Development Program of China[2023YFA1800403] ; Science and Technology Innovation Commission of Shenzhen, China[20231121191245001] ; Special Project of Key Fields of Universities in Guangdong Province, China[2021ZDZX2047] ; Key Research and Development Program of Ningxia[2023BEG02010] ; ECNU Construction Fund of Innovation and Entrepreneurship Laboratory[44400-20201-532300/021] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001236650800001 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/311803]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Chen, Yihua; Xiong, Hai |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.East China Normal Univ, Inst Biomed Sci, Sch Life Sci, Shanghai Key Lab Regulatory Biol, Shanghai 200241, Peoples R China 3.Kunming Med Univ, Yunnan Key Lab Pharmacol Nat Prod, Kunming 650500, Yunnan, Peoples R China 4.Kunming Med Univ, Sch Pharmaceut Sci, Kunming 650500, Yunnan, Peoples R China 5.Shenzhen Univ, Coll Phys & Optoelect Engn, Shenzhen 518060, Peoples R China 6.Shenzhen Univ, Inst Adv Study, Shenzhen 518060, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jin, Wangrui,Zheng, Mingyue,Chen, Yihua,et al. Update on the development of TGR5 agonists for human diseases[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2024,271:20. |
| APA | Jin, Wangrui,Zheng, Mingyue,Chen, Yihua,&Xiong, Hai.(2024).Update on the development of TGR5 agonists for human diseases.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,271,20. |
| MLA | Jin, Wangrui,et al."Update on the development of TGR5 agonists for human diseases".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 271(2024):20. |
入库方式： OAI收割
来源：上海药物研究所
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