DNA demethylation and cancer metastasis: therapeutic implications

ISSN： 1746-0441

Source： Expert Opinion on Drug Discovery, Vol.3, Iss.5, 2008-05, pp. : 519-531

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

Abstract

Background: DNA methylation is a covalent modification of DNA, which plays a critical role in regulation of gene expression. Methyl marks in critical regulatory regions of genes silence gene expression. Two contrasting changes in DNA methylation were documented in cancers: regional hypermethylation of tumor suppressor genes and global hypomethylation. Objective: Most of the attention in the field has been directed toward the phenomenon of hypermethylation and silencing of tumor suppressor genes. Hypermethylation indeed plays an extremely important role in cancer and cancer progression. Nevertheless, hypomethylation is emerging now as a mechanism that might lead to activation of prometastatic genes in cancer. Conclusion: Both methylation and demethylation could be pharmacologically modulated. It is argued here that inhibition of hypomethylation might provide a new therapeutic approach to antimetastatic therapy.