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. 2023 Jun 14;24(12):10130. doi: 10.3390/ijms241210130

Table 1.

Representative DNA methyltransferase inhibitors.

Classification Drugs Mechanisms Status of Clinical Use Refs.
Cytosine nucleoside derivatives 5-aza
RX-3117
Incorporate DNA and participate in DNA
replication
clinical application
preclinical study
[34,35]
Deoxyribose analogs 5-aza-dc incorporate DNA and participate in DNA
replication
clinical application [37]
Benzoamide Zebularine
RG108
SGI-1027
bind non-covalently to the active sites of DNMTs preclinical study
preclinical study
preclinical study
[38,39,40]
Aminobenzoic acid derivatives Procainamide
Procaine
bind to the CpG sites Clinical phase II
Clinical phase II
[42,43]
Antisense oligonucleotide
 
Polyphenols
MG-98
miR29a
 
EGCG
curcumin
γ-oryzanol
act on DNMT1 mRNA
 
 
Bind the active site of DNMT enzyme, bind to DNMT sulfhydryl
Clinical phase II
preclinical study
 
preclinical study
preclinical study
preclinical study
[44,45,47,48,49]