ArticleThe Journal of biological chemistry2013
Laccaic acid A is a direct, DNA-competitive inhibitor of DNA methyltransferase 1.
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 26 papers.
What it found
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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.
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Who cites it
26 citing papers in PubMed, 69 citations in OpenAlex.
- Recent Advances in Searching for DNMT Inhibitors and Their Potential Application in Treating Human Diseases.International journal of molecular sciences · 2026Review
- Laccaic Acid A: A Natural Anthraquinone with Potent Anticancer Activity against MDA-MB-231 Cells.Current topics in medicinal chemistry · 2026Article
- Mechanisms and rationales of SAM homeostasis.Trends in biochemical sciences · 2025Review
- 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
- MicroRNA-721 regulates gluconeogenesis via KDM2A-mediated epigenetic modulation in diet-induced insulin resistance in C57BL/6J mice.Biological research · 2024Article
- DNA Methyltransferase 3A: A Significant Target for the Discovery of Inhibitors as Potent Anticancer Drugs.Mini reviews in medicinal chemistry · 2024Review
- Insights into the Inhibitory Mechanisms of the Covalent Drugs for DNMT3A.International journal of molecular sciences · 2023Article
- Recent progress in DNA methyltransferase inhibitors as anticancer agents.Frontiers in pharmacology · 2022Review
- Inhibitors of DNA Methylation.Advances in experimental medicine and biology · 2022Review
- Beyond regulations at DNA levels: A review of epigenetic therapeutics targeting cancer stem cells.Cell proliferation · 2021Review
- Repurposing Old Drugs into New Epigenetic Inhibitors: Promising Candidates for Cancer Treatment?Pharmaceutics · 2020Review
- Pharmacologic inducers of the uric acid exporter ABCG2 as potential drugs for treatment of gouty arthritis.Asian journal of pharmaceutical sciences · 2020Review
- Epidrug Repurposing: Discovering New Faces of Old Acquaintances in Cancer Therapy.Frontiers in oncology · 2020Review
- Substituted anthraquinones represent a potential scaffold for DNA methyltransferase 1-specific inhibitors.PloS one · 2019Article
- Lac water extract inhibits IFN-γ signaling through JAK2-STAT1-IRF1 axis in human melanoma.RSC advances · 2018Article
- Article
- DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge.Biomolecules · 2017Review
- Hypoxia inducible factors regulate the transcription of the sprouty2 gene and expression of the sprouty2 protein.PloS one · 2017Article
- Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Methylation of cytosines in CpG dinucleotides is the predominant epigenetic mark on vertebrate DNA. DNA methylation is associated with transcriptional repression. The pattern of DNA methylation changes during development and with disease. Human DNA methyltransferase 1 (Dnmt1), a 1616-amino acid multidomain enzyme, is essential for maintenance of DNA methylation in proliferating cells and is considered an important cancer drug target. Using a fluorogenic, endonuclease-coupled DNA methylation assay with an activated form of Dnmt1 engineered to lack the replication foci targeting sequence domain, we discovered that laccaic acid A (LCA), a highly substituted anthraquinone natural product, is a direct inhibitor with a 310 nm Ki. LCA is competitive with the DNA substrate in in vitro methylation assays and alters the expression of methylated genes in MCF-7 breast cancer cells synergistically with 5-aza-2'-deoxycytidine. LCA represents a novel class of Dnmt-targeted molecular probes, with biochemical properties that allow it to distinguish between non DNA-bound and DNA-bound Dnmt1.
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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.