ArticleBioorganic & medicinal chemistry letters2010
Semi-automated high-throughput fluorescent intercalator displacement-based discovery of cytotoxic DNA binding agents from a large compound library.
Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Enabling programmable dynamic DNA chemistry using small-molecule DNA binders.Nature communications · 2023Article
- Genome-Edited Coincidence and PMP22-HiBiT Fusion Reporter Cell Lines Enable an Artifact-Suppressive Quantitative High-Throughput Screening Strategy forACS pharmacology & translational science · 2021Article
- Article
- Ruthenium Complexes Containing Heterocyclic Thioamidates Trigger Caspase-Mediated Apoptosis Through MAPK Signaling in Human Hepatocellular Carcinoma Cells.Frontiers in oncology · 2019Article
- A rapid fluorescent indicator displacement assay and principal component/cluster data analysis for determination of ligand-nucleic acid structural selectivity.Nucleic acids research · 2018Article
- A novel ruthenium complex with xanthoxylin induces S-phase arrest and causes ERK1/2-mediated apoptosis in HepG2 cells through a p53-independent pathway.Cell death & disease · 2018Article
- A ruthenium-based 5-fluorouracil complex with enhanced cytotoxicity and apoptosis induction action in HCT116 cells.Scientific reports · 2018Article
- Novel piplartine-containing ruthenium complexes: synthesis, cell growth inhibition, apoptosis induction and ROS production on HCT116 cells.Oncotarget · 2017Article
- Xylopine Induces Oxidative Stress and Causes GOxidative medicine and cellular longevity · 2017Article
- Mechanism of Action and Initial, In Vitro SAR of an Inhibitor of the Shigella flexneri Virulence Regulator VirF.PloS one · 2015Article
- A fluorescence-based screen for ribosome binding antibiotics.Analytical biochemistry · 2013Article
- Melting thermodynamics of reversible DNA/ligand complexes at interfaces.Journal of the American Chemical Society · 2012Article
- Identification of novel small molecule inhibitors of the XPA protein using in silico based screening.ACS chemical biology · 2010Article
- Novel small-molecule inhibitor of apurinic/apyrimidinic endonuclease 1 blocks proliferation and reduces viability of glioblastoma cells.The Journal of pharmacology and experimental therapeutics · 2010Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
High-throughput fluorescent intercalator displacement (HT-FID) was adapted to the semi-automated screening of a commercial compound library containing 60,000 molecules resulting in the discovery of cytotoxic DNA-targeted agents. Although commercial libraries are routinely screened in drug discovery efforts, the DNA binding potential of the compounds they contain has largely been overlooked. HT-FID led to the rapid identification of a number of compounds for which DNA binding properties were validated through demonstration of concentration-dependent DNA binding and increased thermal melting of A/T- or G/C-rich DNA sequences. Selected compounds were assayed further for cell proliferation inhibition in glioblastoma cells. Seven distinct compounds emerged from this screening procedure that represent structures unknown previously to be capable of targeting DNA leading to cell death. These agents may represent structures worthy of further modification to optimally explore their potential as cytotoxic anti-cancer agents. In addition, the general screening strategy described may find broader impact toward the rapid discovery of DNA targeted agents with biological activity.
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Registered trials
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