title: Inhibition of C5-cytosine-DNA-methyltransferases.
abstract: Changes in the methylation pattern of genomic DNA, particularly hypermethylation of tumor suppressor genes, occur at early stages of tumor development. Errors in DNA methylation contribute to both initiation and progression of various cancers. This stimulates significant interest in searching for inhibitors of C5-DNA-methyltransferases (MTases). Here we review the known nucleoside mechanism-based reversible and irreversible inhibitors of the MTases, as well as non-nucleoside ones, and discuss their inhibitory mechanisms and application for MTase investigations and cancer therapy.
authors.affiliation: Faculty of Chemistry, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: O V
authors.initials: OV
authors.lastname: Kirsanova
authors.forename: N A
authors.initials: NA
authors.lastname: Cherepanova
authors.forename: E S
authors.initials: ES
authors.lastname: Gromova
mesh_terms: D000818:Animals; D019175:DNA Methylation; D015257:DNA-Cytosine Methylases / Q000037:antagonists & inhibitors* / Q000737:chemistry* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000627:therapeutic use; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D009705:Nucleosides / Q000737:chemistry; D011485:Protein Binding
chemical_list: D004791:Enzyme Inhibitors; D009705:Nucleosides; D015257:DNA-Cytosine Methylases