ArticleAmerican journal of translational research2021
1-n-heptyl-5-(3, 4-difluorophenyl) biguanide inhibits non-small cell lung cancer cell growth by downregulating the EGFR signaling pathways.
Article in American journal of translational research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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Who cites it
1 citing paper in PubMed, 1 citations in OpenAlex.
- Inhibition of Cyclin D1 by Novel Biguanide Derivative YB-004 Increases the Sensitivity of Bladder Cancer to Olaparib via Causing G0 / G1 Arrest.International journal of biological sciences · 2025Article
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
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Abstract
Lung cancer is among the diseases with the highest rates of morbidity and mortality. Our previous study found that a novel biguanide derivative, 1-n-heptyl-5-(3, 4-difluorophenyl) biguanide (8e) shows excellent anti-proliferative activity in non-small cell lung cancer (NSCLC) cell line A549. However, the underlying mechanism remains elusive. In this research, we analyzed the effect of 8e on NSCLC cell lines and explored the cell death mechanism caused by 8e. From our data, we found that 8e significantly decreased the cell activity and inhibited the colony formation of A549 and H1299 cells in a dose-dependent manner. Interestingly, this inhibitory effect of 8e was significantly reduced after silencing EGFR with lentiviral vectors. In contrast, after overexpressing EGFR in A549 and H1299, the lethality of 8e to the tumor cells increased. Simultaneously, we observed that 8e inhibited the expression of EGFR and its two essential downstream signaling pathways, AKT/mTOR and c-Raf/ERK1/2, and significantly reduced the activation of the EGFR pathway induced by EGF. Therefore, the results showed that 8e inhibits the proliferation of NSCLC cells by down-regulating the expression of EGFR, thereby inhibiting the downstream signaling pathway AKT/mTOR and c-Raf/ERK1/2. In addition, 8e also markedly reduces migration and induces the apoptosis of A549 and H1299 cells.
Indexed as
Identifiers
34650690PMC8507003W3205661063What OpenQuestion holds
Registered trials
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