An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy
文献类型：期刊论文
| 作者 | Li, Huiwen2,3; Cai, Xinhui1; Yang, Xiaoyu1; Zhang, Xuan1,2,3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2024-06-05 |
| 卷号 | 272页码:8 |
| 关键词 | MDM2 PROTAC p53 MDMX Targeted protein degradation |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2024.116506 |
| 通讯作者 | Zhang, Xuan(zhangxuan@simm.ac.cn) |
| 英文摘要 | MDM2 genes amplification or altered expression is commonly observed in various cancers bearing wild-type TP53. . Directly targeting the p53-binding pocket of MDM2 to activate the p53 pathway represents a promising therapeutic approach. Despite the development of numerous potent MDM2 inhibitors that have advanced into clinical trials, their utility is frequently hampered by drug resistance and hematologic toxicity such as neutropenia and thrombocytopenia. The emergence of PROTAC technology has revolutionized drug discovery and development, with applications in both preclinical and clinical research. Harnessing the power of PROTAC molecules to achieve MDM2 targeted degradation and p53 reactivation holds significant promise for cancer therapy. In this review, we summarize representative MDM2 PROTAC degraders and provide insights for researchers investigating MDM2 proteins and the p53 pathway. |
| WOS关键词 | P53-RELATED PROTEIN ; P53 ; GROWTH ; INHIBITORS ; LETHALITY ; DEGRADER ; REVEALS ; COMPLEX ; POTENT ; GSPT1 |
| 资助项目 | National Natural Sci-ence Foundation of China[22277131] ; Pioneer Hundred Talents Program of the Chinese Academy of Sciences |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001293736300001 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/312812]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhang, Xuan |
| 作者单位 | 1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Dev Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Huiwen,Cai, Xinhui,Yang, Xiaoyu,et al. An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2024,272:8. |
| APA | Li, Huiwen,Cai, Xinhui,Yang, Xiaoyu,&Zhang, Xuan.(2024).An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,272,8. |
| MLA | Li, Huiwen,et al."An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 272(2024):8. |
入库方式： OAI收割
来源：上海药物研究所
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