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Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy

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WOS体系：
Pubmed体系：

收录情况： ◇ SCIE

作者：
Zheng Sixiang[1] ; Chen Ruixian[2] ; Zhang Lele[3] ; Tan Lun[3] ; Li Lintao[4] ; Long Fangyi[5] ; Wang Ting[1] ;
机构： [1]Department of Clinical Research, Sichuan Clinical Research Center for Cancer, Sichuan Cancer Hospital & Institute, Sichuan Cancer Center, Affiliated Cancer Hospital of University of Electronic Science and Technology of China, Chengdu, 610041, China [2]Department of Breast Center, West China Hospital, Sichuan University, Chengdu, 610041, China [3]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, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [4]Department of Radiotherapy, Radiation Oncology Key Laboratory of Sichuan Province, Sichuan Clinical Research Center for Cancer, Sichuan Cancer Hospital & Institute, Sichuan Cancer Center, Affiliated Cancer Hospital of University of Electronic Science and Technology of China, Chengdu, 610041, China [5]Laboratory Medicine Center, Sichuan Provincial Maternity and Child Health Care Hospital, Affiliated Women’s and Children’s Hospital of Chengdu Medical College, Chengdu Medical College, Chengdu, 610032, China
出处：
DOI： 10.1016/j.ejmech.2024.116702
ISSN：

关键词： HER2 Cancer treatment Tyrosine kinase inhibitors Drug design Drug resistance Structure-activity relationship

摘要：
Human epidermal growth factor receptor 2 (HER2) is a transmembrane receptor-like protein with tyrosine kinase activity that plays a vital role in processes such as cell proliferation, differentiation, and angiogenesis. The degree of malignancy of different cancers, notably breast cancer, is strongly associated with HER2 amplification, overexpression, and mutation. Currently, widely used clinical HER2 tyrosine kinase inhibitors (TKIs), such as lapatinib and neratinib, have several drawbacks, including susceptibility to drug resistance caused by HER2 mutations and adverse effects from insufficient HER2 selectivity. To address these issues, it is essential to create innovative HER2 TKIs with enhanced safety, effectiveness against mutations, and high selectivity. Typically, SPH5030 has advanced to phase I clinical trials for its strong suppression of four HER2 mutations. This review discusses the latest research progress in HER2 TKIs, with a focus on the structural optimization process and structure-activity relationship analysis. In particular, this study highlights promising design strategies to address these challenges, providing insightful information and inspiration for future development in this field.Copyright © 2024 Elsevier Masson SAS. All rights reserved.

基金：
National Natural Science Foundation of China (82274142, 82374088) and the Sichuan Science and Technology Program (2022ZYD0092, 2023NSFSC0681, 2024YFHZ0164).
语种：
外文
WOS：
PubmedID：
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 Clinical Research, Sichuan Clinical Research Center for Cancer, Sichuan Cancer Hospital & Institute, Sichuan Cancer Center, Affiliated Cancer Hospital of University of Electronic Science and Technology of China, Chengdu, 610041, China
共同第一作者：
通讯作者：
推荐引用方式(GB/T 7714)：
Zheng Sixiang,Chen Ruixian,Zhang Lele,et al.Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy[J].European Journal Of Medicinal Chemistry.2024,276:116702.doi:10.1016/j.ejmech.2024.116702.
APA：
Zheng Sixiang,Chen Ruixian,Zhang Lele,Tan Lun,Li Lintao...&Wang Ting.(2024).Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy.European Journal Of Medicinal Chemistry,276,
MLA：
Zheng Sixiang,et al."Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy".European Journal Of Medicinal Chemistry 276.(2024):116702

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