Zheng Jia, Zhang Wei, Li Linfeng, He Yi, Wei Yue, Dang Yongjun, Nie Shenyou, Guo Zufeng
Center for Novel Target and Therapeutic Intervention, Institute of Life Sciences, Chongqing Medical University, Chongqing, China.
Front Chem. 2022 Apr 14;10:860985. doi: 10.3389/fchem.2022.860985. eCollection 2022.
Targeted therapy is a groundbreaking innovation for cancer treatment. Among the receptor tyrosine kinases, the fibroblast growth factor receptors (FGFRs) garnered substantial attention as promising therapeutic targets due to their fundamental biological functions and frequently observed abnormality in tumors. In the past 2 decades, several generations of FGFR kinase inhibitors have been developed. This review starts by introducing the biological basis of FGF/FGFR signaling. It then gives a detailed description of different types of small-molecule FGFR inhibitors according to modes of action, followed by a systematic overview of small-molecule-based therapies of different modalities. It ends with our perspectives for the development of novel FGFR inhibitors.
靶向治疗是癌症治疗领域的一项突破性创新。在受体酪氨酸激酶中，成纤维细胞生长因子受体（FGFRs）因其基本生物学功能以及在肿瘤中经常出现的异常情况，作为有前景的治疗靶点而备受关注。在过去20年里，已经开发了几代FGFR激酶抑制剂。本综述首先介绍FGF/FGFR信号传导的生物学基础。然后根据作用方式详细描述不同类型的小分子FGFR抑制剂，接着对不同模式的小分子疗法进行系统概述。最后阐述我们对新型FGFR抑制剂开发的展望。
