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Biomolecules. 2017 Jan 5;7(1). pii: E3. doi: 10.3390/biom7010003.

DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge.

Author information

1
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. omar.castilloaguilera@univ-lille2.fr.
2
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. patrick.depreux@univ-lille2.fr.
3
FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France. ludovic.halby@etac.cnrs.fr.
4
FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France. paola.arimondo@etac.cnrs.fr.
5
Churchill College, Cambridge CB3 0DS, UK. paola.arimondo@etac.cnrs.fr.
6
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. laurence.goossens@univ-lille2.fr.

Abstract

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.

KEYWORDS:

DNA methylation; DNMT inhibitors; DNMT/HMT crosstalk; HMT inhibitors; histone methylation

PMID:
28067760
PMCID:
PMC5372715
DOI:
10.3390/biom7010003
[Indexed for MEDLINE]
Free PMC Article

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