Ntavaroukas, Panagiotis, Michail, Konstantinos, Tsiakalidou, Rafaela, Stampouloglou, Eleni, Tsiggene, Katerina, Komiotis, Dimitrios, Georgiou, Nikitas, Mavromoustakos, Thomas, Manta, Stella, Aje, Danielle et al (show 3 more authors)
(2024)
A Novel Quinoline Inhibitor of the Canonical NF-κB Transcription Factor Pathway
Biology, 13 (11).
p. 910.
ISSN 2079-7737, 2079-7737
Abstract
The NF-κB family of transcription factors is a master regulator of cellular responses during inflammation, and its dysregulation has been linked to chronic inflammatory diseases, such as inflammatory bowel disease. It is therefore of vital importance to design and test new effective NF-κB inhibitors that have the potential to be utilized in clinical practice. In this study, we used a commercial transgenic HeLa cell line as an NF-κB activation reporter to test a novel quinoline molecule, Q3, as a potential inhibitor of the canonical NF-κB pathway. Q3 inhibited NF-κB-induced luciferase in concentrations as low as 5 μM and did not interfere with cell survival or induced cell death. A real-time PCR analysis revealed that Q3 could inhibit the TNF-induced transcription of the luciferase gene, as well as the TNF gene, a known downstream target gene. Immunocytochemistry studies revealed that Q3 moderately interferes with TNF-induced NF-κB nuclear translocation. Moreover, docking and molecular dynamics analyses confirmed that Q3 could potentially modulate transcriptional activity by inhibiting the interaction of NF-κB and DNA. Therefore, Q3 could be potentially developed for further in vivo studies as an NF-κB inhibitor.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | NF-kappa B, inflammation, quinoline, transcription |
| Divisions: | Faculty of Health & Life Sciences Faculty of Health & Life Sciences > Inst. Infection, Vet & Ecological Sciences |
| Depositing User: | Symplectic Admin |
| Date Deposited: | 02 Dec 2024 08:26 |
| Last Modified: | 16 Jun 2026 17:01 |
| DOI: | 10.3390/biology13110910 |
| Open Access URL: | https://doi.org/10.3390/biology13110910 |
| Related Websites: | |
| URI: | https://livrepository.liverpool.ac.uk/id/eprint/3188969 |
| Disclaimer: | The University of Liverpool is not responsible for content contained on other websites from links within repository metadata. Please contact us if you notice anything that appears incorrect or inappropriate. |
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