ArticleJournal of the American Chemical Society2020
Quinazoline Ligands Induce Cancer Cell Death through Selective STAT3 Inhibition and G-Quadruplex Stabilization.
Article in Journal of the American Chemical Society, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 78 citations in OpenAlex.
- Function-preserving photooxidation of AS1411 aptamer by a G-quadruplex-guided photosensitizer.Chemical science · 2026Article
- Article
- G-quadruplex DNA reprograms the photochemistry of CX-5461 toward radical-driven anticancer activity.Nucleic acids research · 2026Article
- Tuning potency for precision: the role of the G4-ligand in G4-ligand conjugated oligonucleotides targeting individual G-quadruplex DNA structures.RSC chemical biology · 2026Article
- CRISPR-Cas9 targeting of G-Quadruplex DNA in ADH1 promoter highlights its role in transcriptome and metabolome regulation.Nucleic acids research · 2025Article
- Harnessing CRISPR/Cas9 to overcome targeted therapy resistance in non‑small cell lung cancer: Advances and challenges (Review).Oncology reports · 2025Review
- Photodynamic Therapy Using a Heavy-Atom-Free G‑Quadruplex-Targeted Photosensitizer to Efficiently Regress Rhabdomyosarcoma Tumors In Vivo.ACS pharmacology & translational science · 2025Article
- Light-Activated Molecules Targeting G-Quadruplex Nucleic Acids.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Review
- Anticancer, antimicrobial and molecular docking analysis of newly synthesized iodoquinazoline derivatives.AMB Express · 2025Article
- Linker Design Principles for the Precision Targeting of Oncogenic G-Quadruplex DNA with G4-Ligand-Conjugated Oligonucleotides.Bioconjugate chemistry · 2025Article
- Design, Synthesis, and Biophysical Characterization of Pyridine Bis-Quinazoline Derivatives as Selective G-Quadruplex DNA Stabilizers.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Downregulated STAT3 and STAT5B are prognostic biomarkers for colorectal cancer and are associated with immune infiltration.Discover oncology · 2025Article
- Revolutionizing tumor diagnosis and treatment: the promise of DNA nanotechnology.Frontiers in immunology · 2025Review
- Oligostyrylbenzene Derivatives with Antiparasitic and Antibacterial Activity as Potent G-Quadruplex Ligands.Molecules (Basel, Switzerland) · 2024Article
- Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity.Cell death & disease · 2024Article
- Harnessing Light for G-Quadruplex Modulation: Dual Isomeric Effects of anThe journal of physical chemistry letters · 2024Article
- G4-Ligand-Conjugated Oligonucleotides Mediate Selective Binding and Stabilization of Individual G4 DNA Structures.Journal of the American Chemical Society · 2024Article
- Exploring the Dispersion and Electrostatic Components in Arene-Arene Interactions between Ligands and G4 DNA to Develop G4-Ligands.Journal of medicinal chemistry · 2024Article
- Telomeres and telomerase in Sarcoma disease and therapy.International journal of medical sciences · 2024Review
- Feasibility of the inhibitor development for cancer: A systematic approach for drug design.PloS one · 2024Article
Corrections and comments
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Authors and funding
19 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The signal transducer and activator of transcription 3 (STAT3) protein is a master regulator of most key hallmarks and enablers of cancer, including cell proliferation and the response to DNA damage. G-Quadruplex (G4) structures are four-stranded noncanonical DNA structures enriched at telomeres and oncogenes' promoters. In cancer cells, stabilization of G4 DNAs leads to replication stress and DNA damage accumulation and is therefore considered a promising target for oncotherapy. Here, we designed and synthesized novel quinazoline-based compounds that simultaneously and selectively affect these two well-recognized cancer targets, G4 DNA structures and the STAT3 protein. Using a combination of in vitro assays, NMR, and molecular dynamics simulations, we show that these small, uncharged compounds not only bind to the STAT3 protein but also stabilize G4 structures. In human cultured cells, the compounds inhibit phosphorylation-dependent activation of STAT3 without affecting the antiapoptotic factor STAT1 and cause increased formation of G4 structures, as revealed by the use of a G4 DNA-specific antibody. As a result, treated cells show slower DNA replication, DNA damage checkpoint activation, and an increased apoptotic rate. Importantly, cancer cells are more sensitive to these molecules compared to noncancerous cell lines. This is the first report of a promising class of compounds that not only targets the DNA damage cancer response machinery but also simultaneously inhibits the STAT3-induced cancer cell proliferation, demonstrating a novel approach in cancer therapy.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.