成纤维细胞生长因子受体4(FGFR4)通过启动STAT3、MAPK和PI3K/AKT等信号级联,调节细胞的增殖、分化和转移。其基因突变、过表达或其配体分子过表达等异常信号转导在某些肿瘤的发生发展中发挥着重要的作用,表明FGFR4是此类肿瘤潜在的治疗靶标。靶向FGFR4的抗肿瘤药物或方法主要包括小分子抑制剂、单克隆抗体、配体捕获蛋白、短链RNA寡核苷酸适配体(shRNA)。本文回顾FGFR4异常的肿瘤及靶向FGFR4抗肿瘤药物的研究进展。
Activated fibroblast growth factor receptor 4(FGFR4) initiates STAT3, MAPK and PI3K/AKT signaling cascades, regulates the proliferation, differentiation and migration of cells. The FGFR4 signaling aberrations, such as mutation, overexpression or ligand overexpression, play crucial roles in the genesis and development of various tumor cells. It indicates that FGFR4 is a potential therapy target. Blocking FGFR4 signaling pathway is an effective method for treating tumors with FGFR4 signaling aberrations, which containing small molecule kinase inhibitor, monoclonal antibody, ligand capture protein and short RNA oligonucleotide adapter(shRNA). In this paper, we reviewed the abnormal signaling of FGFR4 in tumor and the research progress of anti-tumor drug.