Histone Lysine-to-Methionine Mutation as Anticancer Drug Target.

Abstract:

:Histone modification stands for a vital genetic information form, which shows tight correlation with the modulation of normal physiological activities by genes. Abnormal regulation of histone methylation due to histone modification enzyme changes and histone mutations plays an important role in the development of cancer. Histone mutations, especially H3K27M and H3K36M, have been identified in various cancers such as pediatric DIPG (diffuse intrinsic pontine glioma) and chondroblastoma respectively. "K to M" mutation results overall downregulation of methylation on these lysine residues. Also, "K to M" mutant histones can inhibit the enzymatic activity of the responsible HMT (histone methyltransferase); for instance, SETD2 indicates H3K36 methylation, and Ezh2 represents H3K27 methylation. In-depth analysis of the mechanism of tumor formation triggered by the K to M mutation results in possible targeted therapies. This chapter is going to briefly introduce the mechanism of histone lysine-to-methionine mutation and review the recently identified targeted therapeutic strategies.

journal_name

Adv Exp Med Biol

authors

Yang J,Qiu Q,Chen L

doi

10.1007/978-981-15-8104-5_7

subject

Has Abstract

pub_date

2021-01-01 00:00:00

pages

85-96

eissn

0065-2598

issn

2214-8019

journal_volume

1283

pub_type

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