Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors
文献类型：期刊论文
| 作者 | Wang, Qiangfeng5; Zhu, Yumeng3,4; Pei, Junping1,2 |
| 刊名 | FUTURE MEDICINAL CHEMISTRY
 |
| 出版日期 | 2024-08-27 |
| 页码 | 22 |
| 关键词 | cancer degrader EGFR lysosome-based degradation PROTAC resistance |
| ISSN号 | 1756-8919 |
| DOI | 10.1080/17568919.2024.2389764 |
| 通讯作者 | Pei, Junping(jppei@baridd.ac.cn) |
| 英文摘要 | Abnormal activation of EGFR is often associated with various malignant tumors, making it an important target for antitumor therapy. However, traditional targeted inhibitors have several limitations, such as drug resistance and side effects. Many studies have focused on the development of EGFR degraders to overcome this resistance and enhance the therapeutic effect on tumors. Proteolysis targeting chimeras (PROTAC) and Lysosome-based degradation techniques have made significant progress in degrading EGFR. This review provides a summary of the structural and function of EGFR, the resistance, particularly the research progress and activity of EGFR degraders via the proteasome and lysosome. Furthermore, this review aims to provide insights for the development of the novel EGFR degraders. |
| WOS关键词 | EPIDERMAL-GROWTH-FACTOR ; CELL LUNG-CANCER ; FACTOR RECEPTOR EGFR ; TYROSINE KINASE INHIBITORS ; BIM DELETION POLYMORPHISM ; E3 UBIQUITIN LIGASE ; PROTEIN-DEGRADATION ; 1ST-LINE TREATMENT ; OPEN-LABEL ; BIOLOGICAL EVALUATION |
| 资助项目 | National Natural Science Foundation of China[81902720] ; Shandong Provincial Natural Science Foundation[ZR2023QH355] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001303551600001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/313071]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Pei, Junping |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China 3.Sichuan Univ, West China Hosp, Canc Ctr, Collaborat Innovat Ctr Biotherapy, Chengdu 610041, Peoples R China 4.Sichuan Univ, West China Hosp, Collaborat Innovat Ctr Biotherapy, State Key Lab Biotherapy, Chengdu 610041, Peoples R China 5.Zhejiang Univ, Affiliated Hosp 1, Dept Med Oncol, Sch Med, Hangzhou 310003, Zhejiang, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Qiangfeng,Zhu, Yumeng,Pei, Junping. Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors[J]. FUTURE MEDICINAL CHEMISTRY,2024:22. |
| APA | Wang, Qiangfeng,Zhu, Yumeng,&Pei, Junping.(2024).Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors.FUTURE MEDICINAL CHEMISTRY,22. |
| MLA | Wang, Qiangfeng,et al."Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors".FUTURE MEDICINAL CHEMISTRY (2024):22. |
入库方式： OAI收割
来源：上海药物研究所
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