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Updated: Sep 7, 2025
Immunofluorescence Imaging of DNA Damage and Repair Foci in Human Colon Cancer Cells
Published on: June 9, 2020
The novel FGFR inhibitor F1-7 induces DNA damage and cell death in colon cells
Yanan Liu1, Liting Zhang1, Xiaolu Chen1
1School of Pharmaceutical Sciences, Wenzhou Medical University, 325035, Wenzhou, Zhejiang, China.
Background:
Fibroblast growth factor receptor (FGFR) signaling influenced tumour occurrence and development. Overexpression of FGFR had been observed in many types of cancers, including colon cancer. FGFR inhibitor is considered to be effective in treating colon cancer patients.
Methods:
First, the kinase inhibition rate was determined. MTT, western blotting, colony formation, EdU and comet assays were performed to evaluate the anti-tumour effects of F1-7 in vitro. RNA-seq and bioinformatics analysis were used for further verification. Additionally, a xenograft model was generated to investigate the anti-tumour effect of F1-7.
Results:
F1-7 can inhibit the proliferation of colon cancer cells in vitro. It could significantly inhibit FGFR phosphorylation and its downstream signaling pathway. Whole-genome RNA-seq analysis found that the changed genes were not only functionally focused on MAPK signaling pathway but also related to cell apoptosis and ferroptosis. Experimental evidence demonstrated that F1-7 can directly increase the level of cellular DNA damage. The occurrence of DNA damage led to cell cycle arrest and inhibition of cell metastasis and cell apoptosis. Mouse model experiments also confirmed that F1-7 could inhibit tumour growth by inhibiting the FGFR pathway.
Conclusions:
F1-7 exhibits anti-tumour activity by inhibiting the FGFR pathway. It could be a novel therapeutic agent for targeting colon cancer cells.
Insights
A novel compound, F1-7, effectively inhibits colon cancer growth by targeting Fibroblast Growth Factor Receptor (FGFR) signaling. This compound shows promise as a new therapeutic agent for colon cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Cancer Research
Background:
- Fibroblast Growth Factor Receptor (FGFR) signaling plays a crucial role in tumor development.
- FGFR overexpression is prevalent in various cancers, including colon cancer.
- FGFR inhibitors are a promising therapeutic strategy for colon cancer.
Purpose of the Study:
- To evaluate the anti-tumor effects of a novel compound, F1-7, in colon cancer.
- To investigate the mechanism of action of F1-7, specifically its effect on FGFR signaling.
- To assess the therapeutic potential of F1-7 in preclinical colon cancer models.
Main Methods:
- In vitro assays including MTT, western blotting, colony formation, EdU, and comet assays were used to assess anti-tumor effects.
- RNA-sequencing and bioinformatics analysis were employed for mechanistic insights.
- A xenograft mouse model was utilized to evaluate in vivo anti-tumor efficacy.
Main Results:
- F1-7 demonstrated significant inhibition of colon cancer cell proliferation in vitro.
- F1-7 effectively inhibited FGFR phosphorylation and downstream signaling pathways.
- RNA-seq revealed that F1-7 impacts MAPK signaling, apoptosis, and ferroptosis, and induces DNA damage, leading to cell cycle arrest and reduced metastasis.
Conclusions:
- F1-7 exhibits potent anti-tumor activity against colon cancer by inhibiting the FGFR pathway.
- F1-7 induces DNA damage, cell cycle arrest, and apoptosis in colon cancer cells.
- F1-7 represents a potential novel therapeutic agent for colon cancer treatment.
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