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doi: 10.1038/nrc.2017.8.

Advances and challenges in targeting FGFR signalling in cancer

Irina S Babina 1 Nicholas C Turner 1 
  • PMID: 28303906
  •     157 citations


Fibroblast growth factors (FGFs) and their receptors (FGFRs) regulate numerous cellular processes. Deregulation of FGFR signalling is observed in a subset of many cancers, making activated FGFRs a highly promising potential therapeutic target supported by multiple preclinical studies. However, early-phase clinical trials have produced mixed results with FGFR-targeted cancer therapies, revealing substantial complexity to targeting aberrant FGFR signalling. In this Review, we discuss the increasing understanding of the differences between diverse mechanisms of oncogenic activation of FGFR, and the factors that determine response and resistance to FGFR targeting.

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Precision Medicine to Treat Advanced Gastroesophageal Adenocarcinoma: A Work in Progress.
Valentina Gambardella, Tania Fleitas, +6 authors, Andrés Cervantes.
J Clin Med, 2020 Sep 26; 9(9). PMID: 32971757    Free PMC article.
Hormonal Receptor Status Determines Prognostic Significance of FGFR2 in Invasive Breast Carcinoma.
Marcin Braun, Dominika Piasecka, +8 authors, Hanna M Romanska.
Cancers (Basel), 2020 Sep 26; 12(9). PMID: 32971804    Free PMC article.
An updated meta-analysis of the association between fibroblast growth factor receptor 4 polymorphisms and susceptibility to cancer.
Abdolkarim Moazeni-Roodi, Sahel Sarabandi, +2 authors, Saeid Ghavami.
Biosci Rep, 2020 Oct 06; 40(10). PMID: 33017009    Free PMC article.
FGF2-Derived PeptibodyF2-MMAE Conjugate for Targeted Delivery of Cytotoxic Drugs into Cancer Cells Overexpressing FGFR1.
Karolina Jendryczko, Julia Chudzian, +5 authors, Anna Szlachcic.
Cancers (Basel), 2020 Oct 21; 12(10). PMID: 33076489    Free PMC article.
The FGF/FGFR System in Breast Cancer: Oncogenic Features and Therapeutic Perspectives.
Maria Francesca Santolla, Marcello Maggiolini.
Cancers (Basel), 2020 Oct 22; 12(10). PMID: 33081025    Free PMC article.
FGF18-FGFR2 signaling triggers the activation of c-Jun-YAP1 axis to promote carcinogenesis in a subgroup of gastric cancer patients and indicates translational potential.
Jinglin Zhang, Chi Chun Wong, +16 authors, Wei Kang.
Oncogene, 2020 Sep 17; 39(43). PMID: 32934314    Free PMC article.
Fibroblast Growth Factor Receptor (FGFR) Inhibitors in Urothelial Cancer.
Rohan Garje, Josiah An, +3 authors, Yousef Zakharia.
Oncologist, 2020 Aug 14; 25(11). PMID: 32790011    Free PMC article.
Fibroblast growth factor receptor signaling as therapeutic targets in female reproductive system cancers.
Dong-Li Zhu, Xiao-Mei Tuo, +2 authors, Yan Guo.
J Cancer, 2020 Nov 17; 11(24). PMID: 33193890    Free PMC article.
Unique genomic features and prognostic value of COSMIC mutational signature 4 in lung adenocarcinoma and lung squamous cell carcinoma.
Xiuyu Cai, Zhenghe Chen, +6 authors, Chun Luo.
Ann Transl Med, 2020 Nov 27; 8(18). PMID: 33241025    Free PMC article.
Tyrosine Kinase Receptors in Oncology.
Jorge Esteban-Villarrubia, Juan José Soto-Castillo, +6 authors, Javier Molina-Cerrillo.
Int J Mol Sci, 2020 Nov 18; 21(22). PMID: 33198314    Free PMC article.
FGFR1β is a driver isoform of FGFR1 alternative splicing in breast cancer cells.
Ming Zhao, Ming-Lei Zhuo, +2 authors, Funda Meric-Bernstam.
Oncotarget, 2019 Feb 05; 10(1). PMID: 30713601    Free PMC article.
FGFs/FGFRs-dependent signalling in regulation of steroid hormone receptors - implications for therapy of luminal breast cancer.
Dominika Piasecka, Marcin Braun, +4 authors, Hanna Romanska.
J Exp Clin Cancer Res, 2019 May 31; 38(1). PMID: 31142340    Free PMC article.
Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1/2/3 and CSF-1R, in FGFR-dependent and macrophage-dominant cancer models.
Xia Peng, Pengcong Hou, +13 authors, Jing Ai.
J Exp Clin Cancer Res, 2019 Aug 24; 38(1). PMID: 31438996    Free PMC article.
The Role of Glypicans in Cancer Progression and Therapy.
Nan Li, Madeline R Spetz, Mitchell Ho.
J Histochem Cytochem, 2020 Jul 07; 68(12). PMID: 32623934    Free PMC article.
High throughput profiling of undifferentiated pleomorphic sarcomas identifies two main subgroups with distinct immune profile, clinical outcome and sensitivity to targeted therapies.
Maud Toulmonde, Carlo Lucchesi, +16 authors, Antoine Italiano.
EBioMedicine, 2020 Dec 01; 62. PMID: 33254023    Free PMC article.
Phase I/IIa, open-label, multicentre study to evaluate the optimal dosing and safety of ODM-203 in patients with advanced or metastatic solid tumours.
Petri Bono, Christophe Massard, +11 authors, Jordi A Rodon.
ESMO Open, 2020 Dec 03; 5(6). PMID: 33262202    Free PMC article.
A 'Real-Life' Experience on Automated Digital Image Analysis of FGFR2 Immunohistochemistry in Breast Cancer.
Marcin Braun, Dominika Piasecka, +3 authors, Hanna M Romanska.
Diagnostics (Basel), 2020 Dec 11; 10(12). PMID: 33297384    Free PMC article.

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Role of Fibroblast Growth Factors Receptors (FGFRs) in Brain Tumors, Focus on Astrocytoma and Glioblastoma.
Alessio Ardizzone, Sarah A Scuderi, +6 authors, Irene Paterniti.
Cancers (Basel), 2020 Dec 24; 12(12). PMID: 33352931    Free PMC article.
The Expression and Prognostic Value of FGF2, FGFR3, and FGFBP1 in Esophageal Squamous Cell Carcinoma.
Wenjing Zhang, Yaxing Zhou, +5 authors, Hui Wang.
Anal Cell Pathol (Amst), 2021 Jan 01; 2020. PMID: 33381388    Free PMC article.
Detection of ESR1 Mutations Based on Liquid Biopsy in Estrogen Receptor-Positive Metastatic Breast Cancer: Clinical Impacts and Prospects.
Hao Liao, Wenfa Huang, Wendi Pei, Huiping Li.
Front Oncol, 2021 Jan 02; 10. PMID: 33384956    Free PMC article.
Integration of whole-exome and anchored PCR-based next generation sequencing significantly increases detection of actionable alterations in precision oncology.
Shaham Beg, Rohan Bareja, +19 authors, Juan Miguel Mosquera.
Transl Oncol, 2020 Nov 16; 14(1). PMID: 33190043    Free PMC article.
The Role of Anti-angiogenesis in the Treatment Landscape of Non-small Cell Lung Cancer - New Combinational Approaches and Strategies of Neovessel Inhibition.
Sophia Daum, Hannes Hagen, +2 authors, Andreas Pircher.
Front Cell Dev Biol, 2021 Jan 21; 8. PMID: 33469537    Free PMC article.
Use of Antiangiogenic Therapies in Pediatric Solid Tumors.
Claudia Ollauri-Ibáñez, Itziar Astigarraga.
Cancers (Basel), 2021 Jan 16; 13(2). PMID: 33445470    Free PMC article.
Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.
Ryan A Brawn, Andrew Cook, +17 authors, Stephanos Ioannidis.
ACS Med Chem Lett, 2021 Jan 26; 12(1). PMID: 33488969    Free PMC article.
Metabolic Effects of Recurrent Genetic Aberrations in Multiple Myeloma.
Timon A Bloedjes, Guus de Wilde, Jeroen E J Guikema.
Cancers (Basel), 2021 Jan 27; 13(3). PMID: 33494394    Free PMC article.
FGFR-TKI resistance in cancer: current status and perspectives.
Sitong Yue, Yukun Li, +4 authors, Daichao Wu.
J Hematol Oncol, 2021 Feb 12; 14(1). PMID: 33568192    Free PMC article.
Regulation of aromatase in cancer.
Deborah Molehin, Fahmida Rasha, Rakhshanda Layeequr Rahman, Kevin Pruitt.
Mol Cell Biochem, 2021 Feb 19; 476(6). PMID: 33599895
Deletion of FGF9 in GABAergic neurons causes epilepsy.
Moran Guo, Can Cui, +14 authors, Chunyan Li.
Cell Death Dis, 2021 Feb 21; 12(2). PMID: 33608505    Free PMC article.
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HNO, 2020 Jun 11; 69(3). PMID: 32519203    Free PMC article.
FGFR4 promotes nuclear localization of GABP to inhibit cell apoptosis in uterine leiomyosarcoma.
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Cell Tissue Res, 2020 Nov 06; 383(2). PMID: 33151453
Fibroblast growth factor receptors in cancer: genetic alterations, diagnostics, therapeutic targets and mechanisms of resistance.
Melanie A Krook, Julie W Reeser, +5 authors, Sameek Roychowdhury.
Br J Cancer, 2020 Dec 04; 124(5). PMID: 33268819    Free PMC article.
Avian Reovirus P17 Suppresses Angiogenesis by Promoting DPP4 Secretion.
Ekta Manocha, Antonella Bugatti, +5 authors, Arnaldo Caruso.
Cells, 2021 Feb 03; 10(2). PMID: 33525607    Free PMC article.
Protein Arginine Methyltransferase 5 (PRMT5) and the ERK1/2 & PI3K Pathways: A Case for PRMT5 Inhibition and Combination Therapies in Cancer.
Tzuriel Sapir, David Shifteh, +2 authors, Radhashree Maitra.
Mol Cancer Res, 2020 Dec 09; 19(3). PMID: 33288733    Free PMC article.
A Detailed Protocol for Large-scale Recombinant Expression and Validation of Human FGFR2 with Its Transmembrane and Extracellular Domains in Escherichia coli.
Adam Bajinting, Ho Leung Ng.
Bio Protoc, 2019 Jun 05; 9(11). PMID: 33654782    Free PMC article.
Effects of FGFR inhibitors TKI258, BGJ398 and AZD4547 on breast cancer cells in 2D, 3D and tissue explant cultures.
T E Kähkönen, M Toriseva, +10 authors, P L Härkönen.
Cell Oncol (Dordr), 2020 Oct 30; 44(1). PMID: 33119860    Free PMC article.
DDX41 regulates the expression and alternative splicing of genes involved in tumorigenesis and immune response.
Kai Qin, Danni Jian, +7 authors, Xianglin Yuan.
Oncol Rep, 2021 Mar 03; 45(3). PMID: 33650667    Free PMC article.
Circulating Tumor DNA Markers for Early Progression on Fulvestrant With or Without Palbociclib in ER+ Advanced Breast Cancer.
Ben O'Leary, Rosalind J Cutts, +9 authors, Nicholas C Turner.
J Natl Cancer Inst, 2020 Sep 18; 113(3). PMID: 32940689    Free PMC article.
Co-dependency for MET and FGFR1 in basal triple-negative breast cancers.
Vanessa Y C Sung, Jennifer F Knight, +7 authors, Morag Park.
NPJ Breast Cancer, 2021 Mar 28; 7(1). PMID: 33772015    Free PMC article.
Inhibition of FGF-FGFR and VEGF-VEGFR signalling in cancer treatment.
Guihong Liu, Tao Chen, +3 authors, Xiawei Wei.
Cell Prolif, 2021 Mar 04; 54(4). PMID: 33655556    Free PMC article.
MET-Pyk2 Axis Mediates Acquired Resistance to FGFR Inhibition in Cancer Cells.
Kamila Kitowska, Monika Gorska-Arcisz, +8 authors, Rafal Sadej.
Front Oncol, 2021 Apr 27; 11. PMID: 33898310    Free PMC article.
Developing Precision Medicine for Bladder Cancer.
Brendan J Guercio, Gopa Iyer, Jonathan E Rosenberg.
Hematol Oncol Clin North Am, 2021 May 08; 35(3). PMID: 33958155    Free PMC article.
Novel Regulatory Factors and Small-Molecule Inhibitors of FGFR4 in Cancer.
Yanan Liu, Canwei Wang, +3 authors, Huanhai Xu.
Front Pharmacol, 2021 May 14; 12. PMID: 33981224    Free PMC article.
Emerging agents for the treatment of metastatic urothelial cancer.
Whi An Kwon, Ho Kyung Seo.
Investig Clin Urol, 2021 May 05; 62(3). PMID: 33943047    Free PMC article.
S100A4 Is Involved in Stimulatory Effects Elicited by the FGF2/FGFR1 Signaling Pathway in Triple-Negative Breast Cancer (TNBC) Cells.
Maria Francesca Santolla, Marianna Talia, Marcello Maggiolini.
Int J Mol Sci, 2021 May 06; 22(9). PMID: 33946884    Free PMC article.
2b or Not 2b: How Opposing FGF Receptor Splice Variants Are Blocking Progress in Precision Oncology.
Richard J Epstein, Li Jun Tian, Yan Fei Gu.
J Oncol, 2021 May 20; 2021. PMID: 34007277    Free PMC article.
Adamantinomatous craniopharyngioma as a model to understand paracrine and senescence-induced tumourigenesis.
Jose Mario Gonzalez-Meljem, Juan Pedro Martinez-Barbera.
Cell Mol Life Sci, 2021 May 22; 78(10). PMID: 34019103
Targeting fibroblast growth factor receptors to combat aggressive ependymoma.
Daniela Lötsch, Dominik Kirchhofer, +34 authors, Johannes Gojo.
Acta Neuropathol, 2021 May 29;. PMID: 34046693
Targeting the Fibroblast Growth Factor Receptor (FGFR) Family in Lung Cancer.
Laura Pacini, Andrew D Jenks, Nadia Carvalho Lima, Paul H Huang.
Cells, 2021 Jun 03; 10(5). PMID: 34068816    Free PMC article.