ArticleNucleic acids research2013
Development of a universal radioactive DNA methyltransferase inhibition test for high-throughput screening and mechanistic studies.
Article in Nucleic acids research, 2013. 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, 44 citations in OpenAlex.
- Quinoline-Based DNA Methyltransferase Inhibitors Featuring Basic Side Chains: Design, Synthesis, and Insight in Biochemical and Anticancer Cell Properties.Journal of medicinal chemistry · 2025Article
- Mechanisms and rationales of SAM homeostasis.Trends in biochemical sciences · 2025Review
- Effect of Withaferin-A, Withanone, and Caffeic Acid Phenethyl Ester on DNA Methyltransferases: Potential in Epigenetic Cancer Therapy.Current topics in medicinal chemistry · 2024Article
- Mechanistic Insights into Harmine-Mediated Inhibition of Human DNA Methyltransferases and Prostate Cancer Cell Growth.ACS chemical biology · 2023Article
- iGEM as a human iPS cell-based global epigenetic modulation detection assay provides throughput characterization of chemicals affecting DNA methylation.Scientific reports · 2023Article
- High-Throughput-Methyl-Reading (HTMR) assay: a solution based on nucleotide methyl-binding proteins enables large-scale screening for DNA/RNA methyltransferases and demethylases.Nucleic acids research · 2022Article
- Z-DNA as a Tool for Nuclease-Free DNA Methyltransferase Assay.International journal of molecular sciences · 2021Article
- Novel Quinoline Compounds Active in Cancer Cells through Coupled DNA Methyltransferase Inhibition and Degradation.Cancers · 2020Article
- DNA Methylation Bisubstrate Inhibitors Are Fast-Acting Drugs Active against Artemisinin-ResistantACS central science · 2020Article
- Identification of a novel quinoline-based DNA demethylating compound highly potent in cancer cells.Clinical epigenetics · 2019Article
- Hijacking DNA methyltransferase transition state analogues to produce chemical scaffolds for PRMT inhibitors.Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 2018Article
- Mitochondrial nicotinamide adenine dinucleotide reduced (NADH) oxidation links the tricarboxylic acid (TCA) cycle with methionine metabolism and nuclear DNA methylation.PLoS biology · 2018Article
- S-Adenosyl Methionine and Transmethylation Pathways in Neuropsychiatric Diseases Throughout Life.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2018Review
- Magnetic immunoassay using CdSe/ZnS quantum dots as fluorescent probes to detect the level of DNA methyltransferase 1 in human serum sample.International journal of nanomedicine · 2018Article
- New insights on the mechanism of quinoline-based DNA Methyltransferase inhibitors.The Journal of biological chemistry · 2015Article
- Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation.ChemMedChem · 2014Article
- Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.Journal of medicinal chemistry · 2014Article
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Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
DNA methylation is an important epigenetic mark in eukaryotes, and aberrant pattern of this modification is involved in numerous diseases such as cancers. Interestingly, DNA methylation is reversible and thus is considered a promising therapeutic target. Therefore, there is a need for identifying new small inhibitors of C5 DNA methyltransferases (DNMTs). Despite the development of numerous in vitro DNMT assays, there is a lack of reliable tests suitable for high-throughput screening, which can also give insights into inhibitor mechanisms of action. We developed a new test based on scintillation proximity assay meeting these requirements. After optimizing our assay on human DNMT1 and calibrating it with two known inhibitors, we carried out S-Adenosyl-l-Methionine and DNA competition studies on three inhibitors and were able to determine each mechanism of action. Finally, we showed that our test was applicable to 3 other methyltransferases sources: human DNMT3A, bacterial M.SssI and cellular extracts as well.
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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.