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BIOMARKER:

FGFR overexpression

i
Other names: FGFR, Fibroblast Growth Factor Receptor
23d
Radiolabelled FGF-2 for Imaging Activated Fibroblasts in the Tumor Micro-Environment. (PubMed, Biomolecules)
we labeled FGF-2 with 99mTc and showed nanomolar Kd in vitro with human keratinocytes expressing FGF-2 receptors. In mice, 99mTc-FGF-2 rapidly and efficiently accumulated in tumors expressing FGF-2 receptors. This new radiopharmaceutical could be used in humans to image TAFs.
Journal
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FGF2 (Fibroblast Growth Factor 2)
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FGFR2 overexpression • FGFR overexpression
6ms
FGFR3 and FGFR4 overexpression in juvenile nasopharyngeal angiofibroma: impact of smoking history and implications for personalized management. (PubMed, J Appl Genet)
Furthermore, medical reports indicated higher rates of recurrence and bleeding intensity among smokers. These findings emphasize the potential role of FGFR3 as a key molecular factor in JNA, particularly in the context of smoking.
Journal
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FGFR3 (Fibroblast growth factor receptor 3) • FGFR4 (Fibroblast growth factor receptor 4)
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FGFR3 overexpression • FGFR overexpression • FGFR4 overexpression • FGFR3 expression • FGF3 overexpression
1year
FGFR1 is an important prognostic factor in oral leukoplakia and tongue squamous cell carcinoma. (PubMed, J Oral Pathol Med)
Fibroblast growth factor receptor 1 protein expression is an important prognostic factor in oral leukoplakia and tongue squamous cell carcinoma.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 amplification • FGFR1 overexpression • FGFR overexpression • FGFR1 expression
over1year
Generation of multicellular tumor spheroids with micro-well array for anticancer drug combination screening based on a valuable biomarker of hepatocellular carcinoma. (PubMed, Front Bioeng Biotechnol)
Finally, we demonstrated that Parthenolide is a potential drug that can significantly enhance the clinical efficacy of FGFR4 receptor inhibitors. In general, we offered a new therapeutic way for FGFR4 positive HCC patients.
Journal
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FGFR4 (Fibroblast growth factor receptor 4)
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FGFR overexpression • FGFR4 expression
over1year
Fibroblast growth factor receptor (FGFR) inhibitor rogaratinib in patients with advanced pretreated squamous-cell non-small cell lung cancer over-expressing FGFR mRNA: The SAKK 19/18 phase II study. (PubMed, Lung Cancer)
Despite preliminary signals of activity, rogaratinib failed to improve PFS in patients with advanced SQCLC overexpressing FGFR mRNA. FGFR inhibitors in SQCLC remain a challenging field, and more in-depth understanding of pathway crosstalks may lead to the development of drug combinations with FGFR inhibitors resulting in improved outcomes.
Journal • P2 data
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FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor)
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FGFR overexpression
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Oncomine™ Comprehensive Assay Plus
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rogaratinib (BAY 1163877)
over2years
FGFR2::TACC2 fusion as a novel KIT-independent mechanism of targeted therapy failure in a multidrug-resistant gastrointestinal stromal tumor. (PubMed, Genes Chromosomes Cancer)
Herein, we report a patient presenting with a primary small bowel spindle cell GIST and concurrent peritoneal and liver metastases displaying an imatinib-sensitive KIT exon 11 in-frame deletion. We present the first report of a multi-drug resistant GIST patient who developed an FGFR2 gene fusion as a secondary genetic event to the selective pressure of various TKIs. This case also highlights the heterogeneous escape mechanisms to targeted therapy across various tumor nodules, spanning from both KIT-dependent and KIT-independent off-target activation pathways.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • FGFR1 (Fibroblast growth factor receptor 1) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • MTAP (Methylthioadenosine Phosphorylase) • FGFR4 (Fibroblast growth factor receptor 4) • CDKN2B (Cyclin Dependent Kinase Inhibitor 2B) • AKT2 (V-akt murine thymoma viral oncogene homolog 2)
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FGFR2 mutation • FGFR2 fusion • FGFR mutation • CDKN2A deletion • MTAP deletion • CDKN2A mutation • FGFR fusion • KIT exon 11 mutation • FGFR overexpression • FGFR1 fusion • FGFR4 mutation • KIT exon 13 mutation • FGFR4 amplification • KIT exon 18 mutation • AKT2 amplification
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imatinib
over2years
AZD4547 targets the FGFR/Akt/SOX2 axis to overcome paclitaxel resistance in head and neck cancer. (PubMed, Cell Oncol (Dordr))
From our data we conclude that AZD4547 may increase the impact of taxol during HNSCC treatment. We suggest AZD4547 as a therapeutic agent to overcome taxol-resistance.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor) • SOX2 • FGF2 (Fibroblast Growth Factor 2)
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FGFR overexpression • AKT1 overexpression • FGFR2 expression
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paclitaxel • fexagratinib (ABSK091)
almost3years
[VIRTUAL] Anlotinib plus osimertinib overcomes acquired resistance to osimertinib via FGFR and EGFR signaling in non-small cell lung cancer (NSCLC) (ESMO 2021)
FGFR overexpression may be the mechanism of acquired resistance to Osi. Anlotinib plus Osi could overcome this resistance via inhibiting EGFR and FGFR signaling pathways, which provides a novel treatment option for Osi-resistant NSCLC.
Preclinical
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor)
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EGFR mutation • EGFR T790M • FGFR2 overexpression • FGFR overexpression • FGFR2 expression • EGFR H1975
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Tagrisso (osimertinib) • Focus V (anlotinib)
over3years
Effect of Lenvatinib on a Hepatocellular Carcinoma with Fibroblast Growth Factor Receptor 4 Expression: A Case Report and Review of the Literature. (PubMed, Intern Med)
We herein report a case of HCC that was effectively treated with lenvatinib after a poor response to sorafenib. The tumor showed a high expression of fibroblast growth factor receptor 4, which is reportedly related to the sensitivity to lenvatinib in vitro. The information obtained from this case and from our literature review highlights the importance of assessing the expression of the molecules involved in tumors for effective precision medicine.
Clinical • Review • Journal
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FGFR4 (Fibroblast growth factor receptor 4)
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FGFR overexpression • FGFR4 expression
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sorafenib • Lenvima (lenvatinib)
over3years
Circulating Tumor Cells with FGFR2 Expression Might Be Useful to Identify Patients Existing FGFR2 Overexpression Tumor. (PubMed, Cancer Sci)
The relapse-free survival of the patients with FGFR2-positive CTCs (≥5 cells /10 ml blood) was significantly poorer (p=0.018, log-rank) than that of the patients without FGFR2-positive CTCs (<5 cell /10 ml blood). These findings suggested that the determination of FGFR2-positive CTCs might help identify the existing of FGFR2 overexpression tumor.
Clinical • Journal • Circulating Tumor Cells
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FGFR2 (Fibroblast growth factor receptor 2) • PTPRC (Protein Tyrosine Phosphatase Receptor Type C)
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FGFR2 amplification • FGFR2 overexpression • FGFR overexpression
over3years
FGFR1 overexpression renders breast cancer cells resistant to metformin through activation of IRS1/ERK signaling. (PubMed, Biochim Biophys Acta Mol Cell Res)
Targeting IRS with IRS1 KO or IRS inhibitor NT157 significantly sensitized FGFR1 overexpressing cells to metformin. Moreover, we demonstrated that IRS1 functions as a critical mediator of the crosstalk between FGFR1 and IGF1R pathways, which involves a feedback loop between IRS1 and MAPK/ERK. Our study highlights the significance of FGFR1 status and IRS1 activation in metformin-resistance, which will facilitate the development of strategies targeting FGFR overexpression-associated metformin resistance.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • IGF1R (Insulin-like growth factor 1 receptor)
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FGFR1 overexpression • FGFR overexpression
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metformin • NT-157
4years
[VIRTUAL] Preclinical evaluation of WXSH0011, a selective small molecule dual inhibitor of FGFR/c-Met. (ASCO 2020)
We have identified a novel selective and potent dual FGFR/c-Met inhibitor WXSH0011. Preclinical studies shows antitumor efficacy of WXSH0011 in gastric and liver cancer models. It is currently at IND submission stage.
Preclinical
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MET (MET proto-oncogene, receptor tyrosine kinase) • FGFR1 (Fibroblast growth factor receptor 1) • HGF (Hepatocyte growth factor) • FGF (Fibroblast Growth Factor)
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MET overexpression • FGFR overexpression
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WXSH0011