Fibroblast growth factor receptor fusions in cancer: opportunities and challenges
Abstract Fibroblast growth factors (FGFs) and their receptors (FGFRs) play critical roles in many biological processes and developmental functions. Chromosomal translocation of FGFRs result in the formation of chimeric FGFR fusion proteins, which often cause aberrant signaling leading to the develop...
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2021
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oai:doaj.org-article:63d4b06e8e2b4f1aa64ee4415063ed6c2021-11-08T10:44:42ZFibroblast growth factor receptor fusions in cancer: opportunities and challenges10.1186/s13046-021-02156-61756-9966https://doaj.org/article/63d4b06e8e2b4f1aa64ee4415063ed6c2021-11-01T00:00:00Zhttps://doi.org/10.1186/s13046-021-02156-6https://doaj.org/toc/1756-9966Abstract Fibroblast growth factors (FGFs) and their receptors (FGFRs) play critical roles in many biological processes and developmental functions. Chromosomal translocation of FGFRs result in the formation of chimeric FGFR fusion proteins, which often cause aberrant signaling leading to the development and progression of human cancer. Due to the high recurrence rate and carcinogenicity, oncogenic FGFR gene fusions have been identified as promising therapeutic targets. Erdafitinib and pemigatinib, two FGFR selective inhibitors targeting FGFR fusions, have been approved by the U.S. Food and Drug Administration (FDA) to treat patients with urothelial cancer and cholangiocarcinoma, respectively. Futibatinib, a third-generation FGFR inhibitor, is under phase III clinical trials in patients with FGFR gene rearrangements. Herein, we review the current understanding of the FGF/FGFRs system and the oncogenic effect of FGFR fusions, summarize promising inhibitors under clinical development for patients with FGFR fusions, and highlight the challenges in this field.Lingfeng ChenYanmei ZhangLina YinBinhao CaiPing HuangXiaokun LiGuang LiangBMCarticleFibroblast growth factor receptorsFusion proteinsChromosomal translocationCancerInhibitorsNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENJournal of Experimental & Clinical Cancer Research, Vol 40, Iss 1, Pp 1-15 (2021) |
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Fibroblast growth factor receptors Fusion proteins Chromosomal translocation Cancer Inhibitors Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 |
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Fibroblast growth factor receptors Fusion proteins Chromosomal translocation Cancer Inhibitors Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Lingfeng Chen Yanmei Zhang Lina Yin Binhao Cai Ping Huang Xiaokun Li Guang Liang Fibroblast growth factor receptor fusions in cancer: opportunities and challenges |
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Abstract Fibroblast growth factors (FGFs) and their receptors (FGFRs) play critical roles in many biological processes and developmental functions. Chromosomal translocation of FGFRs result in the formation of chimeric FGFR fusion proteins, which often cause aberrant signaling leading to the development and progression of human cancer. Due to the high recurrence rate and carcinogenicity, oncogenic FGFR gene fusions have been identified as promising therapeutic targets. Erdafitinib and pemigatinib, two FGFR selective inhibitors targeting FGFR fusions, have been approved by the U.S. Food and Drug Administration (FDA) to treat patients with urothelial cancer and cholangiocarcinoma, respectively. Futibatinib, a third-generation FGFR inhibitor, is under phase III clinical trials in patients with FGFR gene rearrangements. Herein, we review the current understanding of the FGF/FGFRs system and the oncogenic effect of FGFR fusions, summarize promising inhibitors under clinical development for patients with FGFR fusions, and highlight the challenges in this field. |
format |
article |
author |
Lingfeng Chen Yanmei Zhang Lina Yin Binhao Cai Ping Huang Xiaokun Li Guang Liang |
author_facet |
Lingfeng Chen Yanmei Zhang Lina Yin Binhao Cai Ping Huang Xiaokun Li Guang Liang |
author_sort |
Lingfeng Chen |
title |
Fibroblast growth factor receptor fusions in cancer: opportunities and challenges |
title_short |
Fibroblast growth factor receptor fusions in cancer: opportunities and challenges |
title_full |
Fibroblast growth factor receptor fusions in cancer: opportunities and challenges |
title_fullStr |
Fibroblast growth factor receptor fusions in cancer: opportunities and challenges |
title_full_unstemmed |
Fibroblast growth factor receptor fusions in cancer: opportunities and challenges |
title_sort |
fibroblast growth factor receptor fusions in cancer: opportunities and challenges |
publisher |
BMC |
publishDate |
2021 |
url |
https://doaj.org/article/63d4b06e8e2b4f1aa64ee4415063ed6c |
work_keys_str_mv |
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_version_ |
1718442621613899776 |