ArticleACS medicinal chemistry letters2015
Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells.
Article in ACS medicinal chemistry letters, 2015. 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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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
14 citing papers in PubMed.
- The emerging role of KDM5A in human cancer.Journal of hematology & oncology · 2021Review
- KDM5B is a master regulator of the H3K4-methylome in stem cells, development and cancer.Seminars in cancer biology · 2019Review
- Identification of ryuvidine as a KDM5A inhibitor.Scientific reports · 2019Article
- Small Molecule Inhibitors of KDM5 Histone Demethylases Increase the Radiosensitivity of Breast Cancer Cells Overexpressing JARID1B.Molecules (Basel, Switzerland) · 2019Article
- Small molecule KDM4s inhibitors as anti-cancer agents.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Inhibitors of Protein Methyltransferases and Demethylases.Chemical reviews · 2018Review
- Targeting JARID1B's demethylase activity blocks a subset of its functions in oral cancer.Oncotarget · 2018Article
- JARID1 Histone Demethylases: Emerging Targets in Cancer.Trends in cancer · 2017Review
- Tungsten exposure causes a selective loss of histone demethylase protein.Molecular carcinogenesis · 2017Article
- Cellular analysis of the action of epigenetic drugs and probes.Epigenetics · 2017Review
- Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.Cell chemical biology · 2017Article
- Histone Lysine Demethylase Inhibitors.Cold Spring Harbor perspectives in medicine · 2017Review
- Assessing histone demethylase inhibitors in cells: lessons learned.Epigenetics & chromatin · 2017Article
- Screen-identified selective inhibitor of lysine demethylase 5A blocks cancer cell growth and drug resistance.Oncotarget · 2016Article
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Jumonji AT-rich interactive domain 1A (JARID1A), one of the jumonji C domain-containing histone demethylase (JHDM) family members, plays key roles in cancer cell proliferation and development of drug tolerance. Therefore, selective JARID1A inhibitors are potential anticancer agents. In this study, we searched for cell-active JARID1A inhibitors by screening hydroxamate compounds in our in-house library and the structural optimization based on docking study of the hit-compound to a homology model of JARID1A. As a result, we identified compound 6j, which selectively inhibits JARID1A over three other JHDM family members. Compound 7j, a prodrug form of compound 6j, induced a selective increase in the level of trimethylation of histone H3 lysine 4, a substrate of JARID1A. Furthermore, compound 7j synergistically enhanced A549 human lung cancer cell growth inhibition induced by vorinostat, a histone deacetylase inhibitor. These findings support the idea that JARID1A inhibitors have potential as anticancer agents.
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