Laboratory of Molecular Design and Drug Discovery, School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing, Jiangsu, 211198, China.
National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing, Jiangsu, 210023, China.
Eur J Med Chem. 2020 Jan 15;186:111884. doi: 10.1016/j.ejmech.2019.111884. Epub 2019 Nov 16.
Mutation or abnormal expression of protein tyrosine kinases (PTKs) is one of the main causes of cancer. Fibroblast growth factor receptors (FGFRs) are a subfamily of tyrosine kinase receptors, which have four subtypes including FGFR1, FGFR2, FGFR3 and FGFR4. Their abnormal expression in cells is considered to be the main cause of tumorigenesis, so inhibiting FGFRs is thought to be important targets for cancer treatment. This article mainly summarizes the recent development of FGFR inhibitors in the past 5 years, and hopes to guide the future research on the design and synthesis of FGFR inhibitors.
蛋白酪氨酸激酶（PTKs）的突变或异常表达是癌症的主要原因之一。成纤维细胞生长因子受体（FGFRs）是酪氨酸激酶受体的一个亚家族，包括 FGFR1、FGFR2、FGFR3 和 FGFR4 四种亚型。它们在细胞中的异常表达被认为是肿瘤发生的主要原因，因此抑制 FGFRs 被认为是癌症治疗的重要靶点。本文主要总结了过去 5 年 FGFR 抑制剂的最新研究进展，以期为 FGFR 抑制剂的设计和合成提供指导。
