ShanghaiTech University Knowledge Management System
| Routes to molecular glue degrader discovery | |
| 2025-02-01 | |
| 发表期刊 | TRENDS IN BIOCHEMICAL SCIENCES (IF:11.6[JCR-2023],12.5[5-Year]) |
| ISSN | 0968-0004 |
| EISSN | 1362-4326 |
| 卷号 | 50期号:2 |
| DOI | 10.1016/j.tibs.2024.12.006 |
| 摘要 | Molecular glue degraders (MGDs) represent a unique class of targeted protein degradation (TPD) modalities. By facilitating protein-protein interactions between E3 ubiquitin ligases and neo-substrates, MGDs offer a novel approach to target previously undruggable or insufficiently drugged disease-causing proteins. Here, we present an overview of recently reported MGDs, highlighting their di-verse mechanisms, and we discuss mechanism-based strategies to discover new MGDs and neo-substrates. These strategies include repurposing existing E3 ubiquitin ligase-targeting ligands, screening for novel binders to proteins of in-terest, and leveraging functional genomics and quantitative proteomics to probe the MGD mechanism of action. Despite their historically serendipitous discovery, MGDs are on their way to being rationally designed to deplete undesired proteins by purposely altering the evolutionarily conserved ligase:substrate interactions. |
| URL | 查看原文 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS研究方向 | Biochemistry & Molecular Biology |
| WOS类目 | Biochemistry & Molecular Biology |
| WOS记录号 | WOS:001453248400001 |
| 出版者 | CELL PRESS |
| 文献类型 | 期刊论文 |
| 条目标识符 | https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/452361 |
| 专题 | 生命科学与技术学院 生命科学与技术学院_PI研究组_刘艳芬组 生命科学与技术学院_PI研究组_仓勇组 生命科学与技术学院_博士生 |
| 通讯作者 | Liu, Yanfen; Cang, Yong |
| 作者单位 | ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China |
| 第一作者单位 | 生命科学与技术学院 |
| 通讯作者单位 | 生命科学与技术学院 |
| 第一作者的第一单位 | 生命科学与技术学院 |
| 推荐引用方式 GB/T 7714 | Liu, Yanfen,Bai, Jieyun,Li, Dong,et al. Routes to molecular glue degrader discovery[J]. TRENDS IN BIOCHEMICAL SCIENCES,2025,50(2). |
| APA | Liu, Yanfen,Bai, Jieyun,Li, Dong,&Cang, Yong.(2025).Routes to molecular glue degrader discovery.TRENDS IN BIOCHEMICAL SCIENCES,50(2). |
| MLA | Liu, Yanfen,et al."Routes to molecular glue degrader discovery".TRENDS IN BIOCHEMICAL SCIENCES 50.2(2025). |
| 条目包含的文件 | ||||||
| 条目无相关文件。 | ||||||
修改评论
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。