DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge
Omar Castillo-Aguilera,
Patrick Depreux,
Ludovic Halby,
Paola B. Arimondo,
Laurence Goossens
Affiliations
Omar Castillo-Aguilera
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. 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
Ludovic Halby
FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France
Paola B. Arimondo
FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France
Laurence Goossens
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
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.
