机构：[1]Department of Medical Oncology, The First Affiliated Hospital, Zhejiang University School of Medicine, 310003, Hangzhou, Zhejiang, China浙江大学医学院附属第一医院[2]State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu, 610041, China四川大学华西医院[3]Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong, 264117, China[4]Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China
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.
基金：
National Natural Science Foundation of China [81902720]; Shandong Provincial Natural Science Foundation [ZR2023QH355]
第一作者机构：[1]Department of Medical Oncology, The First Affiliated Hospital, Zhejiang University School of Medicine, 310003, Hangzhou, Zhejiang, China
通讯作者：
通讯机构：[3]Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong, 264117, China[4]Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, 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.2024,16(18):1923-1944.doi:10.1080/17568919.2024.2389764.
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,16,(18)
MLA：
Wang, Qiangfeng,et al."Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors".FUTURE MEDICINAL CHEMISTRY 16..18(2024):1923-1944
