ArticleJournal of the American Chemical Society2011
G-quadruplex-binding benzo[a]phenoxazines down-regulate c-KIT expression in human gastric carcinoma cells.
Article in Journal of the American Chemical Society, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
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Who cites it
51 citing papers in PubMed.
- Selective Delivery of Anticancer Natural G-Quadruplex Ligands by the AT11 Aptamer for Gastric Cancer Treatment.Journal of medicinal chemistry · 2026Article
- i-motifs: DNA structures with regulatory functions and therapeutic potential.Einstein (Sao Paulo, Brazil) · 2026Review
- The Emerging Roles of Multimolecular G-Quadruplexes in Transcriptional Regulation and Chromatin Organization.Accounts of chemical research · 2024Article
- A Phenotypic Approach to the Discovery of Potent G-Quadruplex Targeted Drugs.Molecules (Basel, Switzerland) · 2024Review
- Selective Recognition ofACS medicinal chemistry letters · 2024Article
- G-Quadruplexes in the Viral Genome: Unlocking Targets for Therapeutic Interventions and Antiviral Strategies.Viruses · 2023Review
- Application of G-quadruplex targets in gastrointestinal cancers: Advancements, challenges and prospects.World journal of gastrointestinal oncology · 2023Review
- Probing juxtaposed G-quadruplex and hairpin motifs using a responsive nucleoside probe: a unique scaffold for chemotherapy.Chemical science · 2023Article
- Emerging roles of i-motif in gene expression and disease treatment.Frontiers in pharmacology · 2023Review
- Structural Polymorphism of Guanine Quadruplex-Containing Regions in Human Promoters.International journal of molecular sciences · 2022Article
- Polymorphic and Higher-Order G-Quadruplexes as Possible Transcription Regulators: Novel Perspectives for Future Anticancer Therapeutic Applications.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Structured Waters Mediate Small Molecule Binding to G-Quadruplex Nucleic Acids.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Probing GFP Chromophore Analogs as Anti-HIV Agents Targeting LTR-III G-Quadruplex.Biomolecules · 2021Article
- Quadruplex Ligands in Cancer Therapy.Cancers · 2021Review
- Cation competition and recruitment around the c-kit1 G-quadruplex using polarizable simulations.Biophysical journal · 2021Article
- Nanomechanics of G-quadruplexes within the promoter of the KIT oncogene.Nucleic acids research · 2021Article
- Recent Developments in Small-Molecule Ligands of Medicinal Relevance for Harnessing the Anticancer Potential of G-Quadruplexes.Molecules (Basel, Switzerland) · 2021Review
- Polarizable Molecular Dynamics Simulations of TwoJournal of chemical theory and computation · 2020Article
- Stabilization of c-KIT G-Quadruplex DNA Structures by the RNA Polymerase I Inhibitors BMH-21 and BA-41.International journal of molecular sciences · 2019Article
- Two-quartet kit* G-quadruplex is formed via double-stranded pre-folded structure.Nucleic acids research · 2019Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
There is considerable interest in the structure and function of G-quadruplex nucleic acid secondary structures, their cellular functions, and their potential as therapeutic targets. G-Quadruplex sequence motifs are prevalent in gene promoter regions and it has been hypothesized that G-quadruplex structure formation is associated with the transcriptional status of the downstream gene. Using a functional cell-based assay, we have identified two novel G-quadruplex ligands that reduce the transcription of a luciferase reporter driven from the G-quadruplex-containing c-KIT promoter. We have further shown that endogenous c-KIT expression in a human gastric carcinoma cell line is also reduced on treatment with these molecules. Biophysical analysis using surface plasmon resonance has shown that these molecules preferentially bind with high affinity to one of the two G-quadruplex sequences in the c-KIT promoter over double-stranded DNA. This work highlights the utility of cell-based reporter assays to identify new G-quadruplex binding molecules that modulate transcription and identifies benzo[a]phenoxazine derivatives as potential antitumor agents.
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Registered trials
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.