ArticleNucleic acids research2020
High resolution crystal structure of a KRAS promoter G-quadruplex reveals a dimer with extensive poly-A π-stacking interactions for small-molecule recognition.
Article in Nucleic acids research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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21 citing papers in PubMed, 49 citations in OpenAlex.
- Dual targeting of topoisomerase I and DNA G-quadruplexes enhances senescence and chemosensitivity in colorectal cancer.Communications biology · 2026Article
- Thiazole peptidomimetics as chemical modulators ofRSC chemical biology · 2025Article
- Interaction of N-methylmesoporphyrin IX with a hybrid left-/right-handed G-quadruplex motif from the promoter of the SLC2A1 gene.Nucleic acids research · 2025Article
- G-quadruplex DNA structure is a positive regulator ofProceedings of the National Academy of Sciences of the United States of America · 2024Article
- Asymmetric triplex metallohelices stabilise DNA G-quadruplexes in promoter oncogene sequences and efficiently reduce their expression in cancer cells.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Selective, Disruptive Luminescent Ru(II) Polypyridyl Probes of G-Quadruplex.Inorganic chemistry · 2023Article
- Machine learning shows torsion angle preferences in left-handed and right-handed quadruplex DNAs.Biophysical journal · 2022Article
- Switching G-quadruplex to parallel duplex by molecular rotor clustering.Nucleic acids research · 2022Article
- Structural insight into the bulge-containing KRAS oncogene promoter G-quadruplex bound to berberine and coptisine.Nature communications · 2022Article
- Action and function of helicases on RNA G-quadruplexes.Methods (San Diego, Calif.) · 2022Review
- Visualization of ligand-induced c-MYC duplex-quadruplex transition and direct exploration of the altered c-MYC DNA-protein interactions in cells.Nucleic acids research · 2022Article
- Human Virus Genomes Are Enriched in Conserved Adenine/Thymine/Uracil Multiple Tracts That Pause Polymerase Progression.Frontiers in microbiology · 2022Article
- Structured Waters Mediate Small Molecule Binding to G-Quadruplex Nucleic Acids.Pharmaceuticals (Basel, Switzerland) · 2021Article
- G-quadruplex DNA: a novel target for drug design.Cellular and molecular life sciences : CMLS · 2021Review
- Bulges in left-handed G-quadruplexes.Nucleic acids research · 2021Article
- Water spines and networks in G-quadruplex structures.Nucleic acids research · 2021Article
- Article
- An Updated Focus on Quadruplex Structures as Potential Therapeutic Targets in Cancer.International journal of molecular sciences · 2020Review
- Coexistence of two quadruplex-duplex hybrids in the PIM1 gene.Nucleic acids research · 2020Article
- Duplex formation in a G-quadruplex bulge.Nucleic acids research · 2020Article
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Aberrant KRAS signaling is a driver of many cancers and yet remains an elusive target for drug therapy. The nuclease hypersensitive element of the KRAS promoter has been reported to form secondary DNA structures called G-quadruplexes (G4s) which may play important roles in regulating KRAS expression, and has spurred interest in structural elucidation studies of the KRAS G-quadruplexes. Here, we report the first high-resolution crystal structure (1.6 Å) of a KRAS G-quadruplex as a 5'-head-to-head dimer with extensive poly-A π-stacking interactions observed across the dimer. Molecular dynamics simulations confirmed that the poly-A π-stacking interactions are also maintained in the G4 monomers. Docking and molecular dynamics simulations with two G4 ligands that display high stabilization of the KRAS G4 indicated the poly-A loop was a binding site for these ligands in addition to the 5'-G-tetrad. Given sequence and structural variability in the loop regions provide the opportunity for small-molecule targeting of specific G4s, we envisage this high-resolution crystal structure for the KRAS G-quadruplex will aid in the rational design of ligands to selectively target KRAS.
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