* To whom correspondence should be addressed.
Received December 12, 2008; Revision received February 25, 2009
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.
KEY WORDS: DNA methyltransferase, methylation pattern, carcinogenesis, gene inactivation, inhibitors of DNA-methyltransferases, mechanism of inhibition, cancer therapy