International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: unknown, P. 138899 - 138899
Published: Dec. 1, 2024
Language: Английский
International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: unknown, P. 138899 - 138899
Published: Dec. 1, 2024
Language: Английский
International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: 302, P. 140556 - 140556
Published: Jan. 31, 2025
Language: Английский
Citations
1International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: 269, P. 132230 - 132230
Published: May 8, 2024
Language: Английский
Citations
5Journal of Biomedical Science, Journal Year: 2025, Volume and Issue: 32(1)
Published: Feb. 5, 2025
Abstract Background The rapid emergence of multiple drug-resistant (MDR) bacterial pathogens and the lack a novel antibiotic pipeline pose serious threat to global healthcare. limited number established targets further restricts identification antibiotics treat life-threatening MDR infections caused by Staphylococcus aureus strains. Therefore, for developing are urgently required. In this study, we hypothesized that G-quadruplex (G4)-binding ligands can be used as their binding possibly downregulate/block expression vital genes. Methods To test this, first screened properties representative G4-binding against hypervirulent S. USA300 determined in vitro vivo antibacterial activity; proposed mechanism action applying various microbiological, infection, microscopic, biophysicochemical techniques. Results Herein, among ligands, N-methyl mesoporphyrin IX (NMM) showed highest activity USA300. NMM exhibited minimum inhibitory concentration (MIC) 5 μM USA300, impacting cell division wall repressing expressions genes ( dcw ) gene cluster. Genome-wide bioinformatics analysis G4 motifs mapping on genome, identified presence G4-motif promoter mraZ , conserved master regulator cluster regulating coordinated synthesis. Physicochemical assessments using UV–visible, circular dichroism, nuclear magnetic resonance spectroscopy confirmed present formed an intramolecular parallel structure, interacting with NMM. reporter followed coupled transcription/translation (IVT) assays role target impose extreme both gram-positive -negative bacteria. In-cell validation RAW264.7 cells Galleria mellonella ; respectively, demonstrated superior compared well-established antibiotics, no observed cytotoxicity. Conclusions summary, current study broad-spectrum potent agent elucidated its plausible primarily targeting
Language: Английский
Citations
0European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 289, P. 117489 - 117489
Published: March 7, 2025
Language: Английский
Citations
0Biochimica et Biophysica Acta (BBA) - General Subjects, Journal Year: 2025, Volume and Issue: unknown, P. 130810 - 130810
Published: April 1, 2025
Language: Английский
Citations
0Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107862 - 107862
Published: Oct. 1, 2024
Language: Английский
Citations
3Sensors and Actuators B Chemical, Journal Year: 2024, Volume and Issue: 418, P. 136350 - 136350
Published: July 23, 2024
Language: Английский
Citations
2International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: 279, P. 135308 - 135308
Published: Sept. 6, 2024
Language: Английский
Citations
1ChemMedChem, Journal Year: 2024, Volume and Issue: unknown
Published: Dec. 16, 2024
The interaction of G-quadruplex (non-canonical DNA) with suitable compounds for their stabilization at the promoter region oncogenes has become a potential anticancer approach. We have studied phenanthroimidazoisoindol-acrylates derivatives c-MYC G-quadruplex. A series 20 were evaluated activity against human cancer cell lines, where 3 fa, ha, and ae shown broad-spectrum activities most lines inactive towards normal lines. Various spectroscopic techniques been used to study these compounds. studies reveal strong binding all three significant selectivity over dsDNA, constant order 10
Language: Английский
Citations
0International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: unknown, P. 138899 - 138899
Published: Dec. 1, 2024
Language: Английский
Citations
0