DNA methylation is now recognized as an important mechanism regulating
different functions of the genome; gene expression, replication, and
cancer, Different factors control the formation and maintenance of DNA
methylation patterns. The level of activity of DNA methyltransferase
(MeTase) is one factor. Recent data suggest that some oncogenic pathwa
ys can induce DNA MeTase expression, that DNA MeTase activity is eleva
ted in cancer, and that inhibition of DNA MeTase can reverse the trans
formed state. What are the pharmacological consequences of our current
understanding of DNA methylation patterns formation! This review will
discuss the possibility that DNA MeTase inhibitors can serve as impor
tant pharmacological and therapeutic tools in cancer and other genetic
diseases.