Discovery of a tribenzophenazine analog for binding to the KRAS mRNA G-quadruplex structures in the cisplatin-resistant non-small cell lung cancer

Journal of Biological Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 108164 - 108164

Published: Jan. 1, 2025

Lung cancer is the malignant tumor with highest morbidity and mortality rate worldwide, of which non-small cell lung (NSCLC) accounts for approximately 85%. KRAS mutations are one significant mechanisms underlying occurrence, development, immune escape, chemotherapy resistance NSCLC. Two inhibitors approved by FDA treatment NSCLC in past three years. However, they only effective to G12C mutant, moreover, innate acquired drug already reported, leaving an urgent need block pathways through novel targets. In this study, we focused on discovery ligands targeting RNA G-quadruplexes (RG4s) 5'-untranslated region (5'-UTR) mRNA, a tribenzophenazine analog (MBD) was identified as lead compound. Further were discussed A549/DDP cells, cisplatin-resistant KRAS-mutant line. Antitumor efficacy verified both vitro vivo nude mouse xenograft model implanted cells. To sum up, our results suggest potential MBD prominent anti-KRAS-driven agent, propose new idea development small molecule RG4s.

Language: Английский

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Photocaged fluorescent probes for spatiotemporally monitoring G-Quadruplex DNA in live cells

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 160, P. 108446 - 108446

Published: April 8, 2025

Language: Английский

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Slight modification of a G-quadruplex-targeted quinoxaline may boost type-1 photodynamic therapy for triple-negative breast cancer

Sensors and Actuators B Chemical, Journal Year: 2024, Volume and Issue: unknown, P. 136952 - 136952

Published: Nov. 1, 2024

Language: Английский

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Quinolino[1,2-a]quinolinium bromide and isoquinolino[2,1-a]quinolinium bromide derivatives as DNA ligands and photocytotoxic agents

Journal of Photochemistry and Photobiology A Chemistry, Journal Year: 2024, Volume and Issue: unknown, P. 116163 - 116163

Published: Nov. 1, 2024

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