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Pharm Res. 1998 Feb;15(2):175-87.

DNA methylation as a target for drug design.

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Urologic Cancer Research Laboratory, USC/Norris Comprehensive Cancer Center, University of Southern California School of Medicine, Los Angeles 90033, USA.


DNA methylation is essential for normal embryonic development. Distinctive genomic methylation patterns must be formed and maintained with high fidelity to ensure the inactivities of specific promoters during development. The mutagenic and epigenetic aspects of DNA methylation are especially interesting because they may lead to the inactivation of genes which are involved in human carcinogenesis. The mutagenicity of 5-Methylcytosine (5mC) and the role of promoter hypermethylation in gene silencing, particularly in cancer, suggest a clinical significance for the design of novel DNA methylation inhibitors which may be utilized to reverse the effects of DNA methylation.

[Indexed for MEDLINE]

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