DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge

Biomolecules

Ludovic Halby¹  Paola B. Arimondo¹  Patrick Depreux²  Laurence Goossens²  Omar Castillo-Aguilera² 

[1] FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France;Univ. Lille, ICPAL, EA 7365—GRITA—Groupe de Recherche sur les formes Injectables et les Technologies Associées, 3 rue du Pr. Laguesse, F-59000 Lille, France;

关键词: DNA methylation;    histone methylation;    DNMT/HMT crosstalk;    DNMT inhibitors;    HMT inhibitors;   

DOI  :  10.3390/biom7010003

来源: DOAJ

【 摘 要 】

Chromatin can adopt a decondensed state linked to gene transcription (euchromatin) and a condensed state linked to transcriptional repression (heterochromatin). These states are controlled by epigenetic modulators that are active on either the DNA or the histones and are tightly associated to each other. Methylation of both DNA and histones is involved in either the activation or silencing of genes and their crosstalk. Since DNA/histone methylation patterns are altered in cancers, molecules that target these modifications are interesting therapeutic tools. We present herein a vast panel of DNA methyltransferase inhibitors classified according to their mechanism, as well as selected histone methyltransferase inhibitors sharing a common mode of action.

【 授权许可】

Unknown