Histone Lysine Demethylases (KDM2/7) Inhibitor with Antitumor Activity

Histones, the protein components of chromatin packaging DNA are involved in the regulation of gene expression. Methylation of a histone lysine residue plays an important role in gene regulation, and is reversibly controlled by histone lysine methyltransferases (KMTs) and histone lysine demethylases (KDMs).
It has been reported that KDM subfamilies, KDM2, KDM4, KDM5 and KDM7 are implicated in tumorigenesis. N-(9-Cyclopropyl-1-oxononyl)-N-hydroxy-β-alanine (NCDM-64), developed by Suzuki, Miyata et al., selectively inhibits KDM2/7. It is expected that NCDM-64 will be used as an anticancer agent.