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

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.

journal_name

Curr Pharm Des

authors

Zheng YC,Ma JL,Liu Y,Liu HM

doi

10.2174/1381612822666160715125417

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

5943-5947

issue

39

eissn

1381-6128

issn

1873-4286

pii

CPD-EPUB-77103

journal_volume

22

pub_type

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