title: DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge.
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.
authors.affiliation: 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.
authors.forename: Omar
authors.initials: O
authors.lastname: Castillo-Aguilera
authors.affiliation: 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.
authors.forename: Patrick
authors.initials: P
authors.lastname: Depreux
authors.affiliation: FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France. ludovic.halby@etac.cnrs.fr.
authors.forename: Ludovic
authors.initials: L
authors.lastname: Halby
authors.affiliation: FRE3600 Epigenetic Targeting of Cancer, CNRS, 31035 Toulouse, France. paola.arimondo@etac.cnrs.fr.|Churchill College, Cambridge CB3 0DS, UK. paola.arimondo@etac.cnrs.fr.
authors.forename: Paola B
authors.initials: PB
authors.lastname: Arimondo
authors.affiliation: 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.
authors.forename: Laurence
authors.initials: L
authors.lastname: Goossens
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D002843:Chromatin / Q000235:genetics / Q000378:metabolism; D002986:Clinical Trials as Topic; D004248:DNA (Cytosine-5-)-Methyltransferases / Q000037:antagonists & inhibitors / Q000378:metabolism; D019175:DNA Methylation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D044127:Epigenesis, Genetic / Q000187:drug effects; D020868:Gene Silencing; D000076983:Histone Methyltransferases; D011495:Histone-Lysine N-Methyltransferase / Q000037:antagonists & inhibitors / Q000378:metabolism; D006657:Histones / Q000378:metabolism; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics
chemical_list: D000970:Antineoplastic Agents; D002843:Chromatin; D004791:Enzyme Inhibitors; D006657:Histones; D000076983:Histone Methyltransferases; D004248:DNA (Cytosine-5-)-Methyltransferases; D011495:Histone-Lysine N-Methyltransferase
keywords: DNA methylation; DNMT inhibitors; DNMT/HMT crosstalk; HMT inhibitors; histone methylation