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RG 108 is a non-nucleoside DNA methyltransferase (Dnmt) inhibitor that blocks the enzyme active site. RG 108 inhibits DNA methylation in human cancer cell lines without detectable toxicity in vitro. The compound demethylates and reactivates epigenetically silences tumor suppressor genes.
Brueckner et al (2005) Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of DNA methyltransferase. Cancer Res. 65 6305. Stresemann et al (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res. 66 2794. Schirrmacher et al (2006) Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug.Chem. 17 261.
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