ArticleOncotarget2016
Screening of candidate G-quadruplex ligands for the human c-KIT promotorial region and their effects in multiple in-vitro models.
Article in Oncotarget, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 36 citations in OpenAlex.
- Collision-induced transfer enhances ligand-binding kinetics in guanine quadruplex DNA.Nucleic acids research · 2026Article
- Insight into the epigenetic regulation of gene expression in the bloodstream and procyclic forms ofNAR genomics and bioinformatics · 2025Article
- Polyphenols bind G4-Quadruplex structures and act as epigenetic modifiers with anti-cancer effects.EXCLI journal · 2025Review
- Bioactive nutraceuticals as G4 stabilizers: potential cancer prevention and therapy-a critical review.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Taq-Polymerase Stop Assay to Determine Target Selectivity of G4 Ligands in Native Promoter Sequences ofPharmaceuticals (Basel, Switzerland) · 2023Article
- Article
- Multiple G-quadruplex binding ligand induced transcriptomic map of cancer cell lines.Journal of cell communication and signaling · 2022Article
- Nanomechanics of G-quadruplexes within the promoter of the KIT oncogene.Nucleic acids research · 2021Article
- G-quadruplexes: a promising target for cancer therapy.Molecular cancer · 2021Review
- G-Quadruplex Modulation of SP1 Functional Binding Sites at theInternational journal of molecular sciences · 2020Article
- 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
- Recent Progress of Targeted G-Quadruplex-Preferred Ligands Toward Cancer Therapy.Molecules (Basel, Switzerland) · 2019Review
- Whole-Transcriptome Profiling of Canine and Human in Vitro Models Exposed to a G-Quadruplex Binding Small Molecule.Scientific reports · 2018Article
- Carbazole Derivatives' Binding to c-KIT G-Quadruplex DNA.Molecules (Basel, Switzerland) · 2018Article
- Conformational profiling of a G-rich sequence within the c-KIT promoter.Nucleic acids research · 2017Article
- Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Stabilization of G-quadruplex (G4) structures in promoters is a novel promising strategy to regulate gene expression at transcriptional and translational levels. c-KIT proto-oncogene encodes for a tyrosine kinase receptor. It is involved in several physiological processes, but it is also dysregulated in many diseases, including cancer. Two G-rich sequences able to fold into G4, have been identified in c-KIT proximal promoter, thus representing suitable targets for anticancer intervention. Herein, we screened an "in house" library of compounds for the recognition of these G4 elements and we identified three promising ligands. Their G4-binding properties were analyzed and related to their antiproliferative, transcriptional and post-transcriptional effects in MCF7 and HGC27 cell lines. Besides c-KIT, the transcriptional analysis covered a panel of oncogenes known to possess G4 in their promoters.From these studies, an anthraquinone derivative (AQ1) was found to efficiently downregulate c-KIT mRNA and protein in both cell lines. The targeted activity of AQ1 was confirmed using c-KIT-dependent cell lines that present either c-KIT mutations or promoter engineered (i.e., α155, HMC1.2 and ROSA cells).Present results indicate AQ1 as a promising compound for the target therapy of c-KIT-dependent tumors, worth of further and in depth molecular investigations.
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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.