DNMT inhibitors function by binding to the active site of DNA methyltransferases, preventing these enzymes from transferring methyl groups to DNA. This inhibition can lead to the reactivation of silenced genes, including tumor suppressor genes, which can play a crucial role in the treatment of various cancers. Two well-known DNMT inhibitors are 5-azacytidine and decitabine, both of which are used in the treatment of myelodysplastic syndromes and acute myeloid leukemia.
