Structural pharmacology and mechanisms of GLP-1R signaling
文献类型：期刊论文
| 作者 | Zhou, Qingtong5,6; Zhao, Fenghui4; Zhang, Yao3; Yang, Dehua5; Wang, Ming-Wei1,2,3,5,6
|
| 刊名 | TRENDS IN PHARMACOLOGICAL SCIENCES
 |
| 出版日期 | 2025-05-01 |
| 卷号 | 46期号:5页码:422-436 |
| ISSN号 | 0165-6147 |
| DOI | 10.1016/j.tips.2025.03.003 |
| 通讯作者 | Wang, Ming-Wei(mwwang@simm.ac.cn) |
| 英文摘要 | Glucagon-like peptide-1 receptor (GLP-1R), a class B1 G protein-coupled receptor, plays critical roles in glucose homeostasis. Recent structural pharmacology studies using cryogenic electron microscopy, X-ray crystallography, mass spectrometry, and functional analyses, have provided valuable insights into its activation by endogenous hormones and mono-or dual agonists like semaglutide and tirzepatide, highly effective in treating type 2 diabetes and obesity. They highlight significant conformational changes in the extracellular and transmembrane domains of GLP-1R that drive receptor activation and downstream signal transduction. Additionally, allosteric modulators, supported by emerging structural information, show great promises as an alternative strategy. Future research investigating unexplored effector interactions, biased signaling, weight rebound mechanisms, and personalized therapy strategies will be critical for developing better therapeutic agents targeting GLP-1R. |
| WOS关键词 | CRYO-EM STRUCTURE ; RECEPTOR ; ACTIVATION ; AGONIST ; COMPLEX ; GLUCOSE ; PEPTIDE ; TRIAL |
| 资助项目 | Ruijin Hospital, Shanghai Jiao Tong University School of Medicine |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001485212400004 |
| 出版者 | CELL PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/317878]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Wang, Ming-Wei |
| 作者单位 | 1.Univ Tokyo, Sch Sci, Dept Chem, Tokyo 1130033, Japan 2.Hainan Med Univ, Engn Res Ctr Trop Med Innovat & Transformat, Sch Pharm, Minist Educ, Haikou 570228, Peoples R China 3.Fudan Univ, Sch Basic Med Sci, Dept Pharmacol, Shanghai 200032, Peoples R China 4.Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 5.Res Ctr Deepsea Bioresources, Sanya 572025, Hainan, Peoples R China 6.Shanghai Jiao Tong Univ, Res Ctr Med Struct Biol, Natl Res Ctr Translat Med Shanghai, State Key Lab Med Genom,Ruijin Hosp,Sch Med, Shanghai 200025, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Qingtong,Zhao, Fenghui,Zhang, Yao,et al. Structural pharmacology and mechanisms of GLP-1R signaling[J]. TRENDS IN PHARMACOLOGICAL SCIENCES,2025,46(5):422-436. |
| APA | Zhou, Qingtong,Zhao, Fenghui,Zhang, Yao,Yang, Dehua,&Wang, Ming-Wei.(2025).Structural pharmacology and mechanisms of GLP-1R signaling.TRENDS IN PHARMACOLOGICAL SCIENCES,46(5),422-436. |
| MLA | Zhou, Qingtong,et al."Structural pharmacology and mechanisms of GLP-1R signaling".TRENDS IN PHARMACOLOGICAL SCIENCES 46.5(2025):422-436. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。