FGFR-TKI resistance in cancer: current status and perspectives

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作者信息关键词期刊信息基础信息归属信息摘要

成果类型：

期刊论文

作者：

Yue, Sitong;Li, Yukun;Chen, Xiaojuan;Wang, Juan;Li, Meixiang;...

通讯作者：

Chen, Yongheng;Wu, Daichao

作者机构：

[Chen, Xiaojuan; Chen, Yongheng; Wu, Daichao; Yue, Sitong] Cent South Univ, Xiangya Hosp, Dept Oncol, Lab Struct Biol,NHC Key Lab Canc Prote,State Loca, Changsha 410008, Hunan, Peoples R China.

[Li, Yukun; Li, Meixiang; Wu, Daichao; Wang, Juan] Univ South China, Clin Anat & Reprod Med Applicat Inst, Dept Histol & Embryol, Hunan Prov Key Lab Canc Cellular & Mol Pathol, Hengyang 421001, Peoples R China.

[Chen, Yongheng; Wu, Daichao] Cent South Univ, Xiangya Hosp, Natl Clin Res Ctr Geriatr Disorders, Changsha 410008, Hunan, Peoples R China.

[Wu, Daichao] Univ Maryland, WM Keck Lab Struct Biol, Inst Biosci & Biotechnol Res, Rockville, MD 20850 USA.

通讯机构：

[Chen, YH; Wu, DC] C

[Wu, Daichao] U

Cent South Univ, Xiangya Hosp, Dept Oncol, Lab Struct Biol,NHC Key Lab Canc Prote,State Loca, Changsha 410008, Hunan, Peoples R China.

Univ South China, Clin Anat & Reprod Med Applicat Inst, Dept Histol & Embryol, Hunan Prov Key Lab Canc Cellular & Mol Pathol, Hengyang 421001, Peoples R China.

Cent South Univ, Xiangya Hosp, Natl Clin Res Ctr Geriatr Disorders, Changsha 410008, Hunan, Peoples R China.

语种：

英文

关键词：

FGFR;Tyrosine kinase inhibitor;Drug resistance;Gatekeeper mutation;Lysosome sequestration

期刊：

Journal of Hematology & Oncology

ISSN：

1756-8722

年：

2021

卷：

期：

页码：

1-14

DOI：

10.1186/s13045-021-01040-2

基金类别：

This work was supported by grants from the National Natural Science Foundation of China (81974074 and 81570537), Outstanding Youth Project of Hunan Education Department (19B475), Open Project of State Local Joint Engineering Laboratory for Anticancer Drugs (KAYW-FK-20-01), Scientific Research Foundation of the University of South China (190XQD016).

机构署名：

本校为通讯机构

院系归属：

医学院

摘要：

Fibroblast growth factor receptors (FGFRs) play key roles in promoting the proliferation, differentiation, and migration of cancer cell. Inactivation of FGFRs by tyrosine kinase inhibitors (TKI) has achieved great success in tumor-targeted therapy. However, resistance to FGFR-TKI has become a concern. Here, we review the mechanisms of FGFR-TKI resistance in cancer, including gatekeeper mutations, alternative signaling pathway activation, lysosome-mediated TKI sequestration, and gene fusion. In addition, we summarize strategies to overcome resistance, including developing covalent inhibitors, d...

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