Biello Federica, Burrafato Giovanni, Rijavec Erika, Genova Carlo, Barletta Giulia, Truini Anna, Coco Simona, Bello Maria Giovanna Dal, Alama Angela, Boccardo Francesco, Grossi Francesco
UOS Tumori Polmonari, IRCCS AOU San Martino IST- Istituto Nazionale per la Ricerca sul Cancro, Largo Rosanna Benzi n°10, 16132 Genova, Italy.
Anticancer Agents Med Chem. 2016;16(9):1142-54. doi: 10.2174/1871520616666160204112347.
Lung cancer is still the leading cause of cancer related death worldwide. Fibroblast growth factor receptor (FGFR) is a tirosine-kinase receptor that is seen to be amplified or mutated in non-small cell lung cancer (NSCLC) and it plays a crucial role in tumour development and maintenance. The authors analyzed the state of the art of FGFR by reviewing the current literature. Fibroblast growth factor (FGF)-FGFR pathway and their aberrations are described, with the evaluation of their possible prognostic role in NSCLC and in particular in squamous cell carcinomas, in which FGFR is more often amplified. New therapeutic agents targeting FGFR signaling have been developed and are now in clinical evaluation. Dysregulation of FGF signaling in tumour cells is related to FGFR gene amplification or mutation, although it is still uncertain which of these aberrations represents a real predictor of response to specific inhibitors. However, recent evidence has questioned whether FGFR is a real target in squamous cell histology. The effectiveness of FGFR inhibitors is also still unclear since there are no clinical data on selected patients. Moreover, the management of specific side effects related to inhibition of the physiological role of FGF should be more thorough.
肺癌仍是全球癌症相关死亡的主要原因。成纤维细胞生长因子受体（FGFR）是一种酪氨酸激酶受体，在非小细胞肺癌（NSCLC）中可见扩增或突变，它在肿瘤的发生和维持中起着关键作用。作者通过回顾当前文献分析了FGFR的研究现状。描述了成纤维细胞生长因子（FGF）-FGFR通路及其异常情况，并评估了它们在NSCLC尤其是鳞状细胞癌中的可能预后作用，在鳞状细胞癌中FGFR更常发生扩增。针对FGFR信号传导的新型治疗药物已被开发出来，目前正处于临床评估阶段。肿瘤细胞中FGF信号传导的失调与FGFR基因扩增或突变有关，尽管仍不确定这些异常情况中哪一种是对特定抑制剂反应的真正预测指标。然而，最近的证据对FGFR在鳞状细胞组织学中是否为真正靶点提出了质疑。由于缺乏针对特定患者的临床数据，FGFR抑制剂的有效性也仍不明确。此外，对于与抑制FGF生理作用相关的特定副作用的管理应更加全面。
