The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Epigenetic Reactivation of Tumor Suppressor Genes by a Novel Small-Molecule Inhibitor of Human DNA Methyltransferases
Abstract
DNA methylation regulates gene expression in normal and malignant cells. The possibility to reactivate epigenetically silenced genes has generated considerable interest in the development of DNA methyltransferase inhibitors. Here, we provide a detailed characterization of RG108, a novel small molecule that effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of the compound resulted in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 caused demethylation and reactivation of tumor suppressor genes, but it did not affect the methylation of centromeric satellite sequences. These results establish RG108 as a DNA methyltransferase inhibitor with fundamentally novel characteristics that will be particularly useful for the experimental modulation of epigenetic gene regulation.
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Cites
DNA methylation patterns and epigenetic memory
Bird, A. (2002) · Genes & Development · doi:10.1101/gad.947102 · Cited by 7,124
Epigenetics in human disease and prospects for epigenetic therapy
Egger, G., Liang, G., Aparicio, A., & Jones, P. A. (2004) · Nature · doi:10.1038/nature02625 · Cited by 3,232
Induction of tumors in mice by genomic hypomethylation
Gaudet, F., Hodgson, J. G., Eden, A., Jackson-Grusby, L., Dausman, J., Gray, J. W., Leonhardt, H., & Jaenisch, R. (2003) · Science · doi:10.1126/science.1083558 · Cited by 1,499 · cited 3×
“This might provide a considerable advantage for the maintenance of chromosome stability in demethylated cells, which has been shown to be affected by the hypomethylation of satellite DNA (4, 5).”
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Cited by
DNA methylation and its basic function
Moore, L. D., Le, T., & Fan, G. (2013) · Neuropsychopharmacology · doi:10.1038/npp.2012.112 · Cited by 4,906
Jones, P. A., & Baylin, S. B. (2007) · Cell · doi:10.1016/j.cell.2007.01.029 · Cited by 4,515
Epigenetic therapy of cancer: past, present and future
Yoo, C. B., & Jones, P. A. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd1930 · Cited by 1,289
Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials
Cheng, Y., He, C., Wang, M., Ma, X., Mo, F., Yang, S., Han, J., & Wei, X. (2019) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-019-0095-0 · Cited by 1,097
Epigenetic Regulation of bdnf Gene Transcription in the Consolidation of Fear Memory
Lubin, F. D., Roth, T. L., & Sweatt, J. D. (2008) · The Journal of Neuroscience · doi:10.1523/jneurosci.1786-08.2008 · Cited by 793
Metadata
- Authors
- Brueckner, B., Garcia Boy, R., Siedlecki, P., Musch, T., Kliem, H. C., Zielenkiewicz, P., Suhai, S., Wiessler, M., & Lyko, F.
- Venue
- Cancer Research
- Published
- 2005-07-15
- Volume
- 65
- Issue
- 14
- Pages
- 6305-6311
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- OpenAlex
- W2013154874
- Cited by
- 545
- References
- 3
- FWCI
- 6.22
- Type
- journal article
- Language
- en
- Open access
- closed
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- Brueckner, B., Garcia Boy, R., Siedlecki, P., Musch, T., Kliem, H. C., Zielenkiewicz, P., Suhai, S., Wiessler, M., & Lyko, F. (2005). Epigenetic Reactivation of Tumor Suppressor Genes by a Novel Small-Molecule Inhibitor of Human DNA Methyltransferases. Cancer Research. https://doi.org/10.1158/0008-5472.can-04-2957
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