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DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge

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
FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France
Churchill College, Cambridge CB3 0DS, UK
Authors to whom correspondence should be addressed.
Academic Editors: Gerda Egger and Melanie R. Hassler
Biomolecules 2017, 7(1), 3;
Received: 15 November 2016 / Revised: 8 December 2016 / Accepted: 12 December 2016 / Published: 5 January 2017
(This article belongs to the Special Issue DNA Methylation and Cancer)
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. View Full-Text
Keywords: DNA methylation; histone methylation; DNMT/HMT crosstalk; DNMT inhibitors; HMT inhibitors DNA methylation; histone methylation; DNMT/HMT crosstalk; DNMT inhibitors; HMT inhibitors
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Castillo-Aguilera, O.; Depreux, P.; Halby, L.; Arimondo, P.B.; Goossens, L. DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge. Biomolecules 2017, 7, 3.

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