Table 3. DNA methyltransferase inhibitors.
5-azacitadine is a ribonucleotide that can be incorporated into RNA as well as DNA. Guadacitabine is a dinucleotide followed by deoxyguanosine, which makes it less prone to breakdown by cytidine deaminase [136]. DNA methyltransferase (DNMT), myelodysplastic syndrome (MDS), acute myeloid leukemia (AML), non-small cell lung cancer (NCSLC).
Therapeutic Agent | Mechanism Of Action | Clinical Indications (ref) |
---|---|---|
5-azacytadine | Cytosine analogs that incorporate into DNA and |
- MDS [126] - AML [148] - NSCLC [129] - ovarian cancer [130] - AML [149] - MDS [127] - ovarian cancer [150] |
5-aza-2’-deoxycytidine (decitabine) |
• at low doses, covalently bind DNMT resulting in hypomethylation |
|
2’-deoxy 5-azacytidylyl-(3’→5’)- 2’deoxyguanosine (guadacitabine) |
• at high doses, halts DNA replication resulting in direct cytotoxicity |
- AML [138] |