title: Targeting DNA methylation with small molecules: what's next?
abstract: DNA methylation is a mammalian epigenetic mark that is involved in defining where and when genes are expressed, both in normal cells and in the context of diseases. Like other epigenetic marks, it is reversible and can be modulated by chemical agents. Because it plays an important role in cancer by silencing certain genes, such as tumor suppressor genes, and by reactivating other regions, such as repeated elements, it is a promising therapeutic target. Two compounds are already approved to treat hematological cancers. Many efforts have been carried out to discover new molecules that are able to efficiently inhibit DNA methylation in cancer cells. We will briefly overview the foremost of these efforts by focusing on what we have learned to this point on non-nucleoside inhibitors and on what we consider to be the features of an ideal inhibitor.
authors.affiliation: Epigenetic Targeting of Cancer, USR3388 ETaC, CNRS-Pierre Fabre, 3 Avenue H. Curien, 31035 Toulouse Cedex 01, France.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Erdmann
authors.affiliation: Epigenetic Targeting of Cancer, USR3388 ETaC, CNRS-Pierre Fabre, 3 Avenue H. Curien, 31035 Toulouse Cedex 01, France.
authors.forename: Ludovic
authors.initials: L
authors.lastname: Halby
authors.affiliation: Epigenetic Targeting of Cancer, USR3388 ETaC, CNRS-Pierre Fabre, 3 Avenue H. Curien, 31035 Toulouse Cedex 01, France.
authors.forename: Jacques
authors.initials: J
authors.lastname: Fahy
authors.affiliation: Epigenetic Targeting of Cancer, USR3388 ETaC, CNRS-Pierre Fabre, 3 Avenue H. Curien, 31035 Toulouse Cedex 01, France.
authors.forename: Paola B
authors.initials: PB
authors.lastname: Arimondo
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D019175:DNA Methylation / Q000187:drug effects*; D015254:DNA Modification Methylases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D055808:Drug Discovery / Q000379:methods*; D044127:Epigenesis, Genetic / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D008958:Models, Molecular; D058990:Molecular Targeted Therapy / Q000379:methods; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics; D009705:Nucleosides / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D009705:Nucleosides; D015254:DNA Modification Methylases