Biological Significance and Targeting of the FGFR Axis in Cancer

The pleiotropic effects of fibroblast growth factors (FGFs), the widespread expression of all seven signalling FGF receptors (FGFRs) throughout the body, and the dramatic phenotypes shown by many FGF/R knockout mice, highlight the diversity, complexity and functional importance of FGFR signalling. T...

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Autores principales:	Athina-Myrto Chioni, Richard P. Grose
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	fibroblast growth factor cancer FGFR inhibitors FGFR mutations FGFR signalling targeting FGFR Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/7be05bd5fe354fef9ddfc59c7b2f4b73
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spelling	oai:doaj.org-article:7be05bd5fe354fef9ddfc59c7b2f4b732021-11-25T17:02:36ZBiological Significance and Targeting of the FGFR Axis in Cancer10.3390/cancers132256812072-6694https://doaj.org/article/7be05bd5fe354fef9ddfc59c7b2f4b732021-11-01T00:00:00Zhttps://www.mdpi.com/2072-6694/13/22/5681https://doaj.org/toc/2072-6694The pleiotropic effects of fibroblast growth factors (FGFs), the widespread expression of all seven signalling FGF receptors (FGFRs) throughout the body, and the dramatic phenotypes shown by many FGF/R knockout mice, highlight the diversity, complexity and functional importance of FGFR signalling. The FGF/R axis is critical during normal tissue development, homeostasis and repair. Therefore, it is not surprising that substantial evidence also pinpoints the involvement of aberrant FGFR signalling in disease, including tumourigenesis. FGFR aberrations in cancer include mutations, gene fusions, and amplifications as well as corrupted autocrine/paracrine loops. Indeed, many clinical trials on cancer are focusing on targeting the FGF/FGFR axis, using selective FGFR inhibitors, nonselective FGFR tyrosine kinase inhibitors, ligand traps, and monoclonal antibodies and some have already been approved for the treatment of cancer patients. The heterogeneous tumour microenvironment and complexity of FGFR signalling may be some of the factors responsible for the resistance or poor response to therapy with FGFR axis-directed therapeutic agents. In the present review we will focus on the structure and function of FGF(R)s, their common irregularities in cancer and the therapeutic value of targeting their function in cancer.Athina-Myrto ChioniRichard P. GroseMDPI AGarticlefibroblast growth factorcancerFGFR inhibitorsFGFR mutationsFGFR signallingtargeting FGFRNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENCancers, Vol 13, Iss 5681, p 5681 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	fibroblast growth factor cancer FGFR inhibitors FGFR mutations FGFR signalling targeting FGFR Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	fibroblast growth factor cancer FGFR inhibitors FGFR mutations FGFR signalling targeting FGFR Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Athina-Myrto Chioni Richard P. Grose Biological Significance and Targeting of the FGFR Axis in Cancer
description	The pleiotropic effects of fibroblast growth factors (FGFs), the widespread expression of all seven signalling FGF receptors (FGFRs) throughout the body, and the dramatic phenotypes shown by many FGF/R knockout mice, highlight the diversity, complexity and functional importance of FGFR signalling. The FGF/R axis is critical during normal tissue development, homeostasis and repair. Therefore, it is not surprising that substantial evidence also pinpoints the involvement of aberrant FGFR signalling in disease, including tumourigenesis. FGFR aberrations in cancer include mutations, gene fusions, and amplifications as well as corrupted autocrine/paracrine loops. Indeed, many clinical trials on cancer are focusing on targeting the FGF/FGFR axis, using selective FGFR inhibitors, nonselective FGFR tyrosine kinase inhibitors, ligand traps, and monoclonal antibodies and some have already been approved for the treatment of cancer patients. The heterogeneous tumour microenvironment and complexity of FGFR signalling may be some of the factors responsible for the resistance or poor response to therapy with FGFR axis-directed therapeutic agents. In the present review we will focus on the structure and function of FGF(R)s, their common irregularities in cancer and the therapeutic value of targeting their function in cancer.
format	article
author	Athina-Myrto Chioni Richard P. Grose
author_facet	Athina-Myrto Chioni Richard P. Grose
author_sort	Athina-Myrto Chioni
title	Biological Significance and Targeting of the FGFR Axis in Cancer
title_short	Biological Significance and Targeting of the FGFR Axis in Cancer
title_full	Biological Significance and Targeting of the FGFR Axis in Cancer
title_fullStr	Biological Significance and Targeting of the FGFR Axis in Cancer
title_full_unstemmed	Biological Significance and Targeting of the FGFR Axis in Cancer
title_sort	biological significance and targeting of the fgfr axis in cancer
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/7be05bd5fe354fef9ddfc59c7b2f4b73
work_keys_str_mv	AT athinamyrtochioni biologicalsignificanceandtargetingofthefgfraxisincancer AT richardpgrose biologicalsignificanceandtargetingofthefgfraxisincancer
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Biological Significance and Targeting of the FGFR Axis in Cancer

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