机构：[1]Department of Pharmacy, Chengdu Fifth People’s Hospital, Chengdu 611130, Sichuan, China[2]Department of Respiratory & Critical Care Medicine, Targeted Tracer Research & Development Laboratory, Institute of Respiratory Health, Precision Medicine Research Center, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China四川大学华西医院[3]Laboratory Medicine Center, Sichuan Provincial Maternity & Child Health Care Hospital, Affiliated Women’s & Children’s Hospital of Chengdu Medical College, Chengdu Medical College, Chengdu 610041, China[4]Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN 38163, USA[5]State Key Laboratory of Biotherapy & Cancer Center, Department of Respiratory & Critical Care Medicine, Core Facilities of West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China
The FGF receptors (FGFRs) belong to a family of receptor tyrosine kinases. Abundant evidence shows that FGFRs are closely related to tumor cell invasion and angiogenesis. Hence, targeted modulation of FGFRs has become an effective strategy for cancer treatment. Recently, the development of small-molecule inhibitors targeting FGFRs has been extensively studied, and three inhibitors have been approved for marketing. Based on the clinical problems with the current inhibitors, there is a need to develop novel inhibitors and technologies to address the pitfalls. This review summarizes recent advances in small-molecule inhibitors targeting FGFRs, focusing on structure-activity relationships. Moreover, recent progress of novel technologies are summarized to provide a reference for promoting the application of drugs targeting FGFRs in tumor therapy.
基金：
Health Commission of Sichuan Province (21PJ149), National Natural Science Foundation of China
(81903502), Natural Science Foundation of Sichuan Province (2022NSDSC1187, 2022NSFSC1365) and the Xingling Foundation
of Chengdu University of Traditional Chinese Medicine (TCM) (YYZX2021043).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2022]版：
大类|3 区医学
小类|4 区药物化学
最新[2023]版：
大类|4 区医学
小类|4 区药物化学
第一作者：
第一作者机构：[1]Department of Pharmacy, Chengdu Fifth People’s Hospital, Chengdu 611130, Sichuan, China[2]Department of Respiratory & Critical Care Medicine, Targeted Tracer Research & Development Laboratory, Institute of Respiratory Health, Precision Medicine Research Center, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China[5]State Key Laboratory of Biotherapy & Cancer Center, Department of Respiratory & Critical Care Medicine, Core Facilities of West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China
共同第一作者：
通讯作者：
通讯机构：[1]Department of Pharmacy, Chengdu Fifth People’s Hospital, Chengdu 611130, Sichuan, China[2]Department of Respiratory & Critical Care Medicine, Targeted Tracer Research & Development Laboratory, Institute of Respiratory Health, Precision Medicine Research Center, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China
推荐引用方式(GB/T 7714)：
Dong Yunzhou,Ren Changyu,Zhu Mengli,et al.Targeting FGFRs for tumor therapy: current status and novel strategies[J].Future medicinal chemistry.2022,doi:10.4155/fmc-2022-0194.
APA：
Dong Yunzhou,Ren Changyu,Zhu Mengli,Zhang Dan,Wang Ting...&Long Fangyi.(2022).Targeting FGFRs for tumor therapy: current status and novel strategies.Future medicinal chemistry,,
MLA：
Dong Yunzhou,et al."Targeting FGFRs for tumor therapy: current status and novel strategies".Future medicinal chemistry .(2022)
