Recent advances in small molecules targeting the METTL3
文献类型：期刊论文
| 作者 | Wu, Feifei3,4; Yu, Lei2; Xu, Shilin1,3,4 |
| 刊名 | FUTURE MEDICINAL CHEMISTRY
 |
| 出版日期 | 2025-08-03 |
| 卷号 | 17期号:15页码:1933-1944 |
| 关键词 | |
| ISSN号 | 1756-8919 |
| DOI | 10.1080/17568919.2025.2546781 |
| 通讯作者 | Xu, Shilin(slxu@simm.ac.cn) |
| 英文摘要 | N6-methyladenosine (m6A) is the most prevalent internal modification of eukaryotic mRNA, playing a crucial role in the regulation of gene expression. Methyltransferase-like 3 (METTL3), a key catalytic component of the m6A methyltransferase complex, is primarily responsible for the deposition of m6A on target RNA. Recent studies have revealed that METTL3 contributes to diverse pathological processes, particularly tumorigenesis, through both m6A-dependent and independent mechanisms. As a result, METTL3 has attracted increasing interest as a potential therapeutic target across various cancer types. This review summarizes recent advances in the discovery of small molecules targeting METTL3, including substrate-competitive inhibitors, allosteric inhibitors, and proteolysis-targeting chimeras (PROTACs). It also discusses the strategies in their discovery, the associated structural features, and the remaining challenges and future directions in this field. Overall, these efforts provide valuable insights into the design and discovery of METTL3-targeted therapeutics with potential clinical applications. |
| WOS关键词 | M(6)A METHYLATION ; MYELOID-LEUKEMIA ; RNA ; TRANSLATION |
| 资助项目 | National Key Research and Development Program of China[2023YFA1800804] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001554935900001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/321297]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Xu, Shilin |
| 作者单位 | 1.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou, Peoples R China 2.Tongji Univ, Shanghai Peoples Hosp 10, Canc Ctr, Sch Med, Shanghai, Peoples R China 3.Univ Chinese Acad Sci, Shanghai Inst Materia Med, Dept Med Chem, Beijing, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Materia Med, Dept Med Chem, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wu, Feifei,Yu, Lei,Xu, Shilin. Recent advances in small molecules targeting the METTL3[J]. FUTURE MEDICINAL CHEMISTRY,2025,17(15):1933-1944. |
| APA | Wu, Feifei,Yu, Lei,&Xu, Shilin.(2025).Recent advances in small molecules targeting the METTL3.FUTURE MEDICINAL CHEMISTRY,17(15),1933-1944. |
| MLA | Wu, Feifei,et al."Recent advances in small molecules targeting the METTL3".FUTURE MEDICINAL CHEMISTRY 17.15(2025):1933-1944. |
入库方式： OAI收割
来源：上海药物研究所
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