Writers and Erasers of Histone Lysine methylation with Clinically Applied Modulators: Promising Target for Cancer Therapy
Hong M. Liu.
Histone lysine methylation can be modified by various writers and erasers. Different
from other epigenetic modifications, mono-, di, and tri- methylation distinctly
modulate chromatin structure and thereby contribute to the regulation of DNA-based nuclear
processes such as transcription, replication and repair on their target genes depending
on different sites. Modulators with opposing catalytic activities dynamically and precisely
control levels of histone lysine methylation, and individual enzymes within these families
have become candidate oncology targets in recent years. Until now, plenty of medicinal
chemists try to pursue potent and selective inhibitor for KMTs and KDMs in order to have
the potential anti-cancer agent, and several of the inhibitors have already enrolled in clinic.
Here, we discuss three histone lysine methylation modulators with their inhibitors in clinical
Keywords: Lysine methyltransferase, lysine demethylase, inhibitor, cancer.
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