Apoptosis induction

Cell differentiation

FIGURE 10.10 Events associated to DNA demethylation.

FIGURE 10.10 Events associated to DNA demethylation.

OH OH S-Adenosylhomocysteine

FIGURE 10.11 Methylation of cytosine by DNA methyltransferases.

S-adenosylhomocysteine. Finally, the product 10.11 and the free enzyme are released from structure 10.13 by a p-elimination reaction (Fig. 10.12).

3.1.1. Nucleoside inhibitors of DNMT

Some nucleoside analogs that have a modified cytosine ring attached to a ribose or deoxyribose moiety behave as DNMT inhibitors. They are metabolized by kinases and ribonucleotide reductases into deoxynucleotides that can be incorporated into DNA, which allows contact with DNMT and its subsequent inhibition. The most interesting compounds of this class are 5-azacytidine, decitabine, 5-fluoro-2'-deoxycytidine, 5,6-dihydro-5-azacytidine (DHAC), and zebularine.

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