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BIOMARKER:

FGFR1 overexpression

i
Other names: FGFR1, BFGFR, CD331, CEK, FLG, FLT2, H2, H3, H4, H5, KAL2, N-SAM, Fibroblast growth factor receptor 1
Entrez ID:
3ms
Drug Conjugation via Maleimide-Thiol Chemistry Does Not Affect Targeting Properties of Cysteine-Containing Anti-FGFR1 Peptibodies. (PubMed, Mol Pharm)
The optimized protocol with PEGylated auristatin yielded doubly substituted peptibodyC19, showing specific cytotoxicity toward the FGFR1-expressing lung cancer cells, with no effect on cells with low FGFR1 levels. Indeed, additional cysteine poses a risk of unwanted modification, but changes in the type of cytotoxic payload and reaction conditions allow the use of standard thiol-maleimide-based conjugation to achieve standard Fc hinge region cysteine modification, analogously to antibody-drug conjugates.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 overexpression • FGFR1 expression • FGFR1 fusion
3ms
FGFR1 is a potential therapeutic target in neuroblastoma. (PubMed, Cancer Cell Int)
FGFR1 is an actionable driver oncogene in NB and a promising therapy may consist in targeting FGFR1 mutations in patients with therapy-resistant NB.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 overexpression • FGFR1 mutation • FGFR1 expression • FGFR wild-type
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ABSK091 • pictilisib (GDC-0941)
6ms
Role of FGF Receptors and Their Pathways in Adrenocortical Tumors and Possible Therapeutic Implications. (PubMed, Front Endocrinol (Lausanne))
Collectively, our study supports a role of FGF pathways in malignant adrenocortical tumors. Quantification of FGF receptors may enable a stratification of ACC for the use of FGFR inhibitors in future clinical trials.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGFR4 (Fibroblast growth factor receptor 4)
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FGFR1 overexpression • FGFR1 expression
6ms
Increased Expression and Altered Cellular Localization of Fibroblast Growth Factor Receptor-Like 1 (FGFRL1) Are Associated with Prostate Cancer Progression. (PubMed, Cancers (Basel))
Our results suggest that FGFRL1 upregulation and altered cellular compartmentalization contribute to PCa progression. The nuclear FGFRL1 could serve as a prognostic marker for PCa patients.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 overexpression • FGFR1 expression
7ms
FGFR1 Overexpression Induces Cancer Cell Stemness and Enhanced Akt/Erk-ER Signaling to Promote Palbociclib Resistance in Luminal A Breast Cancer Cells. (PubMed, Cells)
The combination of palbociclib with FGFR-targeting AZD4547 resulted in remarkable synergistic effects on MCF-7/FGFR1 cells, especially for the inhibition of cancer cell stemness. Our findings of FGFR1-induced palbociclib resistance, promotion of cancer stem cells and associated molecular changes advance our mechanistic understanding of CDKi resistance, which will facilitate the development of strategies targeting CDKi resistance in breast cancer treatment.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • CCND3 (Cyclin D3) • CDK1 (Cyclin-dependent kinase 1) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CCNB1 (Cyclin B1) • E2F1 (E2F transcription factor 1) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)
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FGFR1 overexpression
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Ibrance (palbociclib) • ABSK091
1year
Combined FGFR and Akt pathway inhibition abrogates growth of FGFR1 overexpressing EGFR-TKI-resistant NSCLC cells. (PubMed, NPJ Precis Oncol)
Using spectrometry-based proteomics, we identified increased fibroblast growth factor receptor 1 (FGFR1) expression and Akt activation across erlotinib, gefitinib, and osimertinib EGFR-TKI-resistant cell line models. Further, increased FGFR1 expression was associated with significantly lower PFS in EGFR-TKI-treated NSCLC patients, and increased FGFR1 were demonstrated in a few post- vs. pre-EGFR-TKI treatment clinical biopsies. The superior therapeutic benefit of combining FGFR and Akt inhibitors provide the rationale for clinical trials of this strategy.
Journal
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EGFR (Epidermal growth factor receptor) • FGFR1 (Fibroblast growth factor receptor 1)
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EGFR overexpression • FGFR1 overexpression • FGFR1 expression
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Tagrisso (osimertinib) • erlotinib • gefitinib
1year
Nuclear FGFR1 regulates gene transcription and promotes antiestrogen resistance in ER+ breast cancer. (PubMed, Clin Cancer Res)
These data suggest nuclear FGFR1 contributes to endocrine resistance by modulating gene transcription in ER+ breast cancer. Nuclear FGFR1 activity was unaffected by FGFR TKIs, thus supporting the development of treatment strategies to inhibit nuclear FGFR1 in ER+/FGFR1 overexpressing breast cancer.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FOXA1 (Forkhead Box A1)
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FGFR1 amplification • FGFR1 overexpression • FGFR1 expression
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Balversa (erdafitinib) • fulvestrant • letrozole
1year
Prognostic value of FGFR1 expression and amplification in patients with HNSCC: A systematic review and meta-analysis. (PubMed, PLoS One)
Subgroup analysis stratified by molecular abnormalities, such as overexpression or amplification showed the similar results. The present study demonstrated that HNSCC patients with FGFR1 overexpression and amplification were more likely to exhibit poorer survival.
Retrospective data • Review • Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 amplification • FGFR1 overexpression • FGFR1 expression
1year
FGFR1 overexpression in non-small cell lung cancer is mediated by genetic and epigenetic mechanisms and is a determinant of FGFR1 inhibitor response. (PubMed, Eur J Cancer)
Finally, NSCLC PDX models demonstrating FGFR1 amplification and FGFR1 protein overexpression were sensitive to M6123. The unique molecular and immune features of tumours with high FGFR1 expression provide a rationale to stratify patients in future clinical trials of FGFR1 pathway-targeting agents.
Journal • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
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PD-L1 expression • FGFR1 amplification • FGFR1 overexpression • FGFR1 expression
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M6123
over1year
Targeting FGFR in non-small cell lung cancer: implications from the landscape of clinically actionable aberrations of FGFR kinases. (PubMed, Cancer Biol Med)
We report the prevalence of FGFR anomalies in a large NSCLC population, including mutations, gene amplifications, and novel FGFR fusions.
Clinical • Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • TACC3 (Transforming acidic coiled-coil containing protein 3) • FGFR4 (Fibroblast growth factor receptor 4)
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FGFR1 amplification • EGFR overexpression • FGFR mutation • FGFR1 overexpression • FGFR2 fusion • FGFR fusion • FGFR1 fusion
over1year
FGFR1 amplification or overexpression and hormonal resistance in luminal breast cancer: rationale for a triple blockade of ER, CDK4/6, and FGFR1. (PubMed, Breast Cancer Res)
FGFR1 amplification and overexpression are associated to similar adverse prognosis in hormone-positive breast cancer. Capturing all the patients with adverse prognosis-linked FGFR1 aberrations requires assessing both features. Hormonal deprivation leads to FGFR1 overexpression, and FGFR1 overexpression and/or amplification are associated with resistance to hormonal monotherapy or in combination with palbociclib. Both resistances are reverted with triple ER, CDK4/6, and FGFR1 blockade.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • CDK4 (Cyclin-dependent kinase 4)
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FGFR1 amplification • FGFR1 overexpression
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Ibrance (palbociclib) • rogaratinib (BAY 1163877)
over1year
Oxysophocarpine suppresses FGFR1-overexpressed hepatocellular carcinoma growth and sensitizes the therapeutic effect of lenvatinib. (PubMed, Life Sci)
These data collectively provided evidence that FGFR1 overexpression could be a potential cause of lenvatinib resistance and Oxysophocarpine could be an ideal combined therapy with lenvatinib in HCC treatment.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 overexpression • FGFR1 expression
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lenvatinib
almost2years
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
almost2years
Hsa_circRNA_0000518 facilitates breast cancer development via regulation of the miR-326/FGFR1 axis. (PubMed, Thorac Cancer)
Circ_0000518 facilitated BC development via regulation of the miR-326/FGFR1 axis, suggesting that circ_0000518 might be a promising target for BC treatment.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • FGF (Fibroblast Growth Factor)
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FGFR1 overexpression • FGFR1 expression
almost2years
Circ_0015756 Aggravates Hepatocellular Carcinoma Development by Regulating FGFR1 via Sponging miR-610. (PubMed, Cancer Manag Res)
Circ_0015756 could regulate FGFR1 expression by targeting miR-610. Circ_0015756 played its tumorigenic properties in HCC by activating FGFR1 via sponging miR-610, and circ_0015756 was expected to be a vital indicator in HCC diagnosis and treatment.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • FGF (Fibroblast Growth Factor)
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FGFR1 overexpression • FGFR1 expression
2years
Anlotinib can overcome acquired resistance to EGFR-TKIs via FGFR1 signaling in non-small cell lung cancer without harboring EGFR T790M mutation. (PubMed, Thorac Cancer)
FGFR1 overexpression could be the mechanism of EGFR-TKI acquired resistance and anlotinib can suppresse the growth of EGFR-TKI-resistant NSCLC cells without T790M mutation.
Journal
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EGFR (Epidermal growth factor receptor) • FGFR1 (Fibroblast growth factor receptor 1) • CASP3 (Caspase 3)
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EGFR mutation • EGFR T790M • FGFR1 overexpression
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gefitinib • Focus V (anlotinib)
2years
Lung CSC-derived exosomal miR-210-3p contributes to a pro-metastatic phenotype in lung cancer by targeting FGFRL1. (PubMed, J Cell Mol Med)
Taken together, our results provide new insights into a potential molecular mechanism whereby lung CSC-derived exosomal miR-210-3p targets FGFRL1 to promote lung cancer metastasis. FGFRL1 may be a promising therapeutic target in lung cancer.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • CDH1 (Cadherin 1) • FGF (Fibroblast Growth Factor) • VIM (Vimentin) • MMP9 (Matrix metallopeptidase 9) • MMP1 (Matrix metallopeptidase 1)
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FGFR1 overexpression • CDH1 expression • VIM expression
2years
FGFR1 regulates proliferation and metastasis by targeting CCND1 in FGFR1 amplified lung cancer. (PubMed, Cell Adh Migr)
CCND1 acts as a vital target in FGFR1-amplified lung cancer through forming the FGFR1-CCND1-AKT/MAPK signaling pathway. Co-targeting CCND1 and FGFR1 could provide greater benefits to patients with FGFR1-amplified lung cancer.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • CCND1 (Cyclin D1)
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FGFR1 amplification • FGFR1 overexpression • CCND1 amplification • CCND1 overexpression • CCND1 expression