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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Autores principales: Lingfeng Chen, Yanmei Zhang, Lina Yin, Binhao Cai, Ping Huang, Xiaokun Li, Guang Liang
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Lenguaje:EN
Publicado: BMC 2021
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Acceso en línea:https://doaj.org/article/63d4b06e8e2b4f1aa64ee4415063ed6c
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spelling 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)
institution DOAJ
collection DOAJ
language EN
topic Fibroblast growth factor receptors
Fusion proteins
Chromosomal translocation
Cancer
Inhibitors
Neoplasms. Tumors. Oncology. Including cancer and carcinogens
RC254-282
spellingShingle 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
description 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 AT lingfengchen fibroblastgrowthfactorreceptorfusionsincanceropportunitiesandchallenges
AT yanmeizhang fibroblastgrowthfactorreceptorfusionsincanceropportunitiesandchallenges
AT linayin fibroblastgrowthfactorreceptorfusionsincanceropportunitiesandchallenges
AT binhaocai fibroblastgrowthfactorreceptorfusionsincanceropportunitiesandchallenges
AT pinghuang fibroblastgrowthfactorreceptorfusionsincanceropportunitiesandchallenges
AT xiaokunli fibroblastgrowthfactorreceptorfusionsincanceropportunitiesandchallenges
AT guangliang fibroblastgrowthfactorreceptorfusionsincanceropportunitiesandchallenges
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