Abstract
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.
Keywords: fifbroblast growth factor receptor (FGFR), non-small-cell lung cancer (NSCLC), amplification, tumorigenic role, prognostic role, targeted inhibitors.
Anti-Cancer Agents in Medicinal Chemistry
Title:Fibroblast Growth Factor Receptor (FGFR): A New Target for Non-small Cell Lung Cancer Therapy
Volume: 16 Issue: 9
Author(s): Federica Biello, Giovanni Burrafato, Erika Rijavec, Carlo Genova, Giulia Barletta, Anna Truini, Simona Coco, Maria Giovanna Dal Bello, Angela Alama, Francesco Boccardo and Francesco Grossi
Affiliation:
Keywords: fifbroblast growth factor receptor (FGFR), non-small-cell lung cancer (NSCLC), amplification, tumorigenic role, prognostic role, targeted inhibitors.
Abstract: 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.
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Biello Federica, Burrafato Giovanni, Rijavec Erika, Genova Carlo, Barletta Giulia, Truini Anna, Coco Simona, Bello Giovanna Dal Maria, Alama Angela, Boccardo Francesco and Grossi Francesco, Fibroblast Growth Factor Receptor (FGFR): A New Target for Non-small Cell Lung Cancer Therapy, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (9) . https://dx.doi.org/10.2174/1871520616666160204112347
DOI https://dx.doi.org/10.2174/1871520616666160204112347 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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