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Jumonji Domain-containing Histone Demethylase (JHDM) Inhibitor
No.158(July 2013)
Jumonji domain-containing histone demethylase (JHDM) is an enzyme catalyzing the demethylation of the methylated lysine residue in histone, which regulates the expression of Mdm2 oncogene and p53 anti-oncogene. NCDM-32b (1), developed by Suzuki, Miyata et al., forms NCDM-32 losing a methyl group of the ester moiety by hydrolytic degradation, and shows an inhibitory activity against JMJD2C, a kind of JHDM. NCDM-32 inhibits the growth of HCT116 colon cancer cells with a combination of LSD1 inhibitor.
References
- Design, synthesis, enzyme-Inhibitory activity, and effect on human cancer cells of a novel series of Jumonji domain-containing protein 2 histone demethylase inhibitors
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