Skip to main content
. Author manuscript; available in PMC: 2020 Feb 1.
Published in final edited form as: Transl Res. 2018 Aug 9;204:1–18. doi: 10.1016/j.trsl.2018.08.001

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]