ArticleScientific reports2015
KRAS oncogene repression in colon cancer cell lines by G-quadruplex binding indolo[3,2-c]quinolines.
Article in Scientific reports, 2015. 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, 89 citations in OpenAlex.
- Expression of G-quadruplex coordinates BRCA1, CDH1, and RASSF1 via DNA methylation in mouse breast cancer cells.Epigenomics · 2025Article
- Thiazole peptidomimetics as chemical modulators ofRSC chemical biology · 2025Article
- Jet lag-induced circadian disruption elevates glioma risk by altering molecular profiles in distinct brain regions.Discover oncology · 2025Article
- Bioactive nutraceuticals as G4 stabilizers: potential cancer prevention and therapy-a critical review.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Structure-activity relationships for the G-quadruplex-targeting experimental drug QN-302 and two analogues probed with comparative transcriptome profiling and molecular modeling.Scientific reports · 2024Article
- Ku70 senses cytosolic DNA and assembles a tumor-suppressive signalosome.Science advances · 2024Article
- Structural insight into the bulge-containing KRAS oncogene promoter G-quadruplex bound to berberine and coptisine.Nature communications · 2022Article
- Article
- c-Myc Protein Level Affected by Unsymmetrical Bisacridines Influences Apoptosis and Senescence Induced in HCT116 Colorectal and H460 Lung Cancer Cells.International journal of molecular sciences · 2022Article
- Major Achievements in the Design of Quadruplex-Interactive Small Molecules.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Highly Antiproliferative Latonduine and Indolo[2,3-Journal of medicinal chemistry · 2022Article
- Herb and Spices in Colorectal Cancer Prevention and Treatment: A Narrative Review.Frontiers in pharmacology · 2022Review
- Structured Waters Mediate Small Molecule Binding to G-Quadruplex Nucleic Acids.Pharmaceuticals (Basel, Switzerland) · 2021Article
- G-Quadruplexes and Their Ligands: Biophysical Methods to Unravel G-Quadruplex/Ligand Interactions.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Quadruplex Ligands in Cancer Therapy.Cancers · 2021Review
- Recent Developments in Small-Molecule Ligands of Medicinal Relevance for Harnessing the Anticancer Potential of G-Quadruplexes.Molecules (Basel, Switzerland) · 2021Review
- Article
- G-quadruplex ligands targeting telomeres do not inhibit HIV promoter activity and cooperate with latency reversing agents in killing latently infected cells.Cell cycle (Georgetown, Tex.) · 2020Article
- Review
- Substituted Naphthalenediimide Compounds Bind Selectively to Two Human Quadruplex Structures with Parallel Topology.ACS medicinal chemistry letters · 2020Article
Corrections and comments
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Authors and funding
12 authors at 1 institution in 1 country.
Funding
Abstract
KRAS is one of the most frequently mutated oncogenes in human cancer, yet remaining undruggable. To explore a new therapeutic strategy, a library of 5-methyl-indolo[3,2-c]quinoline derivatives (IQc) with a range of alkyldiamine side chains was designed to target DNA and RNA G-quadruplexes (G4) in the promoter and 5'-UTR mRNA of the KRAS gene. Biophysical experiments showed that di-substituted IQc compounds are potent and selective KRAS G4 stabilizers. They preferentially inhibit the proliferation of KRAS mutant cancer cell lines (0.22 < IC50 < 4.80 μM), down-regulate KRAS promoter activity in a luciferase reporter assay, and reduce both KRAS mRNA and p21(KRAS) steady-state levels in mutant KRAS colon cancer cell lines. Additionally, IQcs induce cancer cell death by apoptosis, explained in part by their capacity to repress KRAS expression. Overall, the results suggest that targeting mutant KRAS at the gene level with G4 binding small molecules is a promising anticancer strategy.
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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.