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Recent discovery and development of AXL inhibitors as antitumor agents

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收录情况： ◇ SCIE

作者：
Liu Zihang[1,2] ; Chen Li[1,3] ; Zhang Jifa[1] ; Yang Jun[1] ; Xiao Xue[4] ; Shan Lianhai[2] ; Mao Wuyu[1] ;
机构： [1]Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-Related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Center, State Key Laboratory of Respiratory Health and Multimorbidity, Laboratory of Neuro-system and Multimorbidity, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [2]School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, Sichuan, China [3]Department of Pharmacy, Sichuan Academy of Medical Sciences & Sichuan Provincial People’s Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, Sichuan, China [4]Department of Obstetrics & Gynecology, Key Laboratory of Birth Defects and Related Diseases of Women and Children, Ministry of Education, West China Second University Hospital, Sichuan University, Chengdu, 610041, Sichuan, China
出处：
DOI： 10.1016/j.ejmech.2024.116475
ISSN：

关键词： Cancer AXL Drug discovery Structure-activity relationship Inhibitors

摘要：
AXL, a receptor tyrosine kinase (RTK), plays a pivotal role in various cellular functions. It is primarily involved in processes such as epithelial-mesenchymal transition (EMT) in tumor cells, angiogenesis, apoptosis, immune regulation, and chemotherapy resistance mechanisms. Therefore, targeting AXL is a promising therapeutic approach for the treatment of cancer. AXL inhibitors that have entered clinical trials, such as BGB324(1), have shown promising efficacy in the treatment of melanoma and non-small cell lung cancer. Additionally, novel AXL-targeted drugs, such as AXL degraders, offer a potential solution to overcome the limitations of traditional small-molecule AXL inhibitors targeting single pathways. We provide an overview of the structure and biological functions of AXL, discusses its correlation with various cancers, and critically analyzes the structure-activity relationship of AXL small-molecule inhibitors in cellular contexts. Additionally, we summarize multiple research and development strategies, offering insights for the future development of innovative AXL inhibitors.Copyright © 2024. Published by Elsevier Masson SAS.

基金：
This review was supported by National Natural Science Foundation of China (22277083), and Natural Science Foundation of Sichuan Province (2022NSFSC1187).
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外文
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中科院(CAS)分区：
出版当年[2023]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
最新[2023]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
JCR分区：
出版当年[2023]版：
Q1 CHEMISTRY, MEDICINAL
最新[2023]版：
Q1 CHEMISTRY, MEDICINAL

影响因子： 最新[2023版] 最新五年平均 出版当年[2023版] 出版当年五年平均 出版前一年[2023版]

第一作者：
第一作者机构： [1]Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-Related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Center, State Key Laboratory of Respiratory Health and Multimorbidity, Laboratory of Neuro-system and Multimorbidity, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [2]School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, Sichuan, China
共同第一作者：
通讯作者：
推荐引用方式(GB/T 7714)：
Liu Zihang,Chen Li,Zhang Jifa,et al.Recent discovery and development of AXL inhibitors as antitumor agents[J].European Journal Of Medicinal Chemistry.2024,272:116475.doi:10.1016/j.ejmech.2024.116475.
APA：
Liu Zihang,Chen Li,Zhang Jifa,Yang Jun,Xiao Xue...&Mao Wuyu.(2024).Recent discovery and development of AXL inhibitors as antitumor agents.European Journal Of Medicinal Chemistry,272,
MLA：
Liu Zihang,et al."Recent discovery and development of AXL inhibitors as antitumor agents".European Journal Of Medicinal Chemistry 272.(2024):116475

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