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. 2020 Jul 31;12(8):2123. doi: 10.3390/cancers12082123

Figure 4.

Figure 4

Strategies for targeting DNMTs in cancers. In normal cells, the genome sequence is usually methylated, and the promoter regions of TSGs are unmethylated. In tumor cells, DNMT aberrations cause hypomethylation of the genome sequence and hypermethylation of TSG promoters. There are two therapeutic strategies: one is to use a DNMTi that targets a single DNMT, and the other is to use a combinatorial approach, such as DNMTi + HDACi, DNMTi + EZH2i, DNMTi + mTORi, dual inhibitors, or synthetic lethality.