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Updated: Mar 23, 2026

Therapy Testing in a Spheroid-based 3D Cell Culture Model for Head and Neck Squamous Cell Carcinoma
Published on: April 20, 2018
Evaluation of FGFR3 as a Therapeutic Target in Head and Neck Squamous Cell Carcinoma
Anne von Mässenhausen1,2,3, Mario Deng4,5, Hannah Billig1,2,3
1Section of Prostate Cancer Research, University Hospital of Bonn, Bonn, Germany.
Background:
Although head and neck squamous cell carcinoma (HNSCC) is the sixth most common tumour entity worldwide, it remains a clinical challenge. Large-scale explorative genomic projects have identified several genes as potential targets for therapy, including fibroblast growth factor receptor 3 (FGFR3).
Aims:
The aim of this study was to investigate the biological significance of wild-type and mutated FGFR3 to evaluate its potential as a novel therapeutic target in HNSCC.
Methods:
FGFR3 protein expression was analysed in a large HNSCC tissue cohort (n = 536) and FGFR3 mRNA expression from The Cancer Genome Atlas (TCGA; n = 520). Moreover, FGFR3 wild-type and mutant versions were overexpressed in vitro, and both proliferation and migration was assessed with and without BGJ398 (a specific FGFR1-3 inhibitor) treatment.
Results:
Although FGFR3 expression for both cohorts decreased during tumour progression, high FGFR3 expression levels were observed in a small subset of patients. In vitro, FGFR3 overexpression led to increased proliferation, whereas migration was not altered. Moreover, FGFR3-overexpressing cells were more sensitive to BGJ398. Cells overexpressing FGFR3 mutant versions showed increased proliferation compared to wild-type FGFR3 under serum-reduced conditions and were largely as sensitive as the wild-type protein to BGJ398.
Conclusions:
Taken together, the results of this study demonstrate that although FGFR3 expression decreases during HNSSC progression, it plays an important role in tumour cell proliferation and thus may be a potential target for therapy in selected patients suffering from this dismal tumour entity.
Insights
Fibroblast growth factor receptor 3 (FGFR3) plays a key role in head and neck squamous cell carcinoma (HNSCC) cell proliferation. Targeting FGFR3 may offer a therapeutic strategy for selected HNSCC patients.
Area of Science:
- Oncology
- Molecular Biology
- Genetics
Background:
- Head and neck squamous cell carcinoma (HNSCC) is a significant global health challenge.
- Genomic studies have identified fibroblast growth factor receptor 3 (FGFR3) as a potential therapeutic target in HNSCC.
Purpose of the Study:
- To investigate the biological significance of wild-type and mutated FGFR3 in HNSCC.
- To evaluate FGFR3 as a potential therapeutic target for HNSCC.
Main Methods:
- Analyzed FGFR3 protein expression in 536 HNSCC tissues and FGFR3 mRNA in 520 TCGA HNSCC samples.
- Overexpressed wild-type and mutant FGFR3 in vitro, assessing proliferation and migration with/without BGJ398 (FGFR1-3 inhibitor).
Main Results:
- FGFR3 expression decreased during tumor progression but was high in a subset of patients.
- FGFR3 overexpression increased proliferation in vitro; migration was unaffected.
- FGFR3-overexpressing cells showed increased sensitivity to BGJ398, with mutant versions exhibiting higher proliferation under low serum conditions.
Conclusions:
- Despite decreasing expression during HNSCC progression, FGFR3 is crucial for tumor cell proliferation.
- FGFR3 represents a potential therapeutic target for a subset of HNSCC patients.
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