ArticleThe Journal of biological chemistry2013
Identification of DNMT1 selective antagonists using a novel scintillation proximity assay.
Article in The Journal of biological chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 51 citations in OpenAlex.
- Reduced Maintenance DNA Methylation Thresholds Enable Sensitive Reporter Assays for UHRF1 and DNMT1 Inhibition.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Advances in epigenetic treatment of adult T-cell leukemia/lymphoma: a comprehensive review.Clinical epigenetics · 2025Review
- Fragment-based discovery of new potential DNMT1 inhibitors integrating multiple pharmacophore modeling, 3D-QSAR, virtual screening, molecular docking, ADME, and molecular dynamics simulation approaches.Molecular diversity · 2025Article
- DNA Methyltransferase 3A: A Significant Target for the Discovery of Inhibitors as Potent Anticancer Drugs.Mini reviews in medicinal chemistry · 2024Review
- Mechanistic Insights into Harmine-Mediated Inhibition of Human DNA Methyltransferases and Prostate Cancer Cell Growth.ACS chemical biology · 2023Article
- Inhibitors of DNA Methylation.Advances in experimental medicine and biology · 2022Review
- Genome-wide impact of hydrogen peroxide on maintenance DNA methylation in replicating cells.Epigenetics & chromatin · 2021Article
- Beyond regulations at DNA levels: A review of epigenetic therapeutics targeting cancer stem cells.Cell proliferation · 2021Review
- Inhibition of DNA methylation in proliferating human lymphoma cells by immune cell oxidants.The Journal of biological chemistry · 2020Article
- A general strategy exploiting m5C duplex-remodelling effect for selective detection of RNA and DNA m5C methyltransferase activity in cells.Nucleic acids research · 2020Article
- T cell Metabolism in Lupus.Immunometabolism · 2020Article
- A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action.Nature communications · 2017Article
- DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge.Biomolecules · 2017Review
- Resveratrol-salicylate derivatives as selective DNMT3 inhibitors and anticancer agents.Journal of enzyme inhibition and medicinal chemistry · 2016Article
- Epigenetic effects of RRx-001: a possible unifying mechanism of anticancer activity.Oncotarget · 2015Article
- The essential roles of chemistry in high-throughput screening triage.Future medicinal chemistry · 2014Review
- Rationalization of activity cliffs of a sulfonamide inhibitor of DNA methyltransferases with induced-fit docking.International journal of molecular sciences · 2014Article
- An ultrasensitive high throughput screen for DNA methyltransferase 1-targeted molecular probes.PloS one · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
A novel scintillation proximity high throughput assay (SPA) to identify inhibitors of DNA methyltransferases was developed and used to screen over 180,000 compounds. The majority of the validated hits shared a quinone core and several were found to generate the reactive oxygen species, H2O2. Inhibition of the production of H2O2 by the addition of catalase blocked the ability of this group of compounds to inhibit DNA methyltransferase (DNMT) activity. However, a related compound, SW155246, was identified that existed in an already reduced form of the quinone. This compound did not generate H2O2, and catalase did not block its ability to inhibit DNA methyltransferase. SW155246 showed a 30-fold preference for inhibition of human DNMT1 versus human or murine DNMT3A or -3B, inhibited global methylation in HeLa cells, and reactivated expression of the tumor suppressor gene RASSF1A in A549 cells. To our knowledge, this work represents the first description of selective chemical inhibitors of the DNMT1 enzyme.
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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.