Structure-Guided Strategies of Targeted Therapies for Patients with EGFR-Mutant Non-Small Cell Lung Cancer

被引：3

作者：

Du, Zhenfang ^{[1
]}

Sun, Jinghan ^{[2
]}

Zhang, Yunkai ^{[3
]}

Hesilaiti, Nigaerayi ^{[1
]}

Xia, Qi ^{[1
]}

Cui, Heqing ^{[4
]}

Fan, Na ^{[5
]}

Xu, Xiaofang ^{[6
]}

机构：

[1] Southeast Univ, Sch Med, Dept Genet & Dev Biol, Nanjing 210003, Peoples R China

[2] Southeast Univ, Sch Life Sci & Technol, Nanjing 210018, Peoples R China

[3] BioSpatula LLC, Telford, PA 18969 USA

[4] Nanjing Med Univ, Nanjing Chest Hosp, Dept Radiotherapy, Affiliated Brain Hosp, Nanjing 210029, Peoples R China

[5] Xi An Jiao Tong Univ, Dept Resp Med & Crit Care Med, Affiliated Hosp 2, Xian 710004, Peoples R China

[6] Chinese Acad Sci, Zhejiang Canc Hosp, Inst Basic Med & Canc IBMC, Dept Thorac Surg,Canc Hosp Univ Chinese Acad Sci, Hangzhou 310022, Peoples R China

来源：

BIOMOLECULES | 2023年 / 13卷 / 02期

关键词：

non-small cell lung cancer; EGFR; structure; targeted therapy; FACTOR-RECEPTOR MUTATIONS; TYROSINE KINASE INHIBITORS; 20 INSERTION MUTATIONS; EXON; 18; MUTATIONS; CLINICOPATHOLOGICAL CHARACTERISTICS; DOMAIN DUPLICATION; CLINICAL ACTIVITY; 1ST-LINE TREATMENT; PRIMARY RESISTANCE; AFATINIB TREATMENT;

D O I：

10.3390/biom13020210

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Oncogenic mutations within the EGFR kinase domain are well-established driver mutations in non-small cell lung cancer (NSCLC). Small-molecule tyrosine kinase inhibitors (TKIs) specifically targeting these mutations have improved treatment outcomes for patients with this subtype of NSCLC. The selectivity of these targeted agents is based on the location of the mutations within the exons of the EGFR gene, and grouping mutations based on structural similarities has proved a useful tool for conceptualizing the heterogeneity of TKI response. Structure-based analysis of EGFR mutations has influenced TKI development, and improved structural understanding will inform continued therapeutic development and further improve patient outcomes. In this review, we summarize recent progress on targeted therapy strategies for patients with EGFR-mutant NSCLC based on structure and function analysis.

引用

页数：16

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