Current Pharmaceutical Design

William A. Banks  
VAPSHCS/GRECC S-182
Building 1, Room 810A
1600 S. Columbian Way
Seattle, WA 98108
USA

Back

Writers and Erasers of Histone Lysine methylation with Clinically Applied Modulators: Promising Target for Cancer Therapy

Author(s): Yi-Chao Zheng, Jin-Lian Ma, Ying Liu, Hong M. Liu.

Abstract:

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 trials.

Keywords: Lysine methyltransferase, lysine demethylase, inhibitor, cancer.

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 22
ISSUE: 39
Year: 2016
Page: [5943 - 5947]
Pages: 5
DOI: 10.2174/1381612822666160715125417
Price: $58