Aim: DNA methylation is a fundamental biologic process of genomes and is a candidate for pharmacological manipulation that might have important therapeutic advantages. Thus, DNA methyltransferases (DNMTs) appear to be ideal targets for drug intervention.
Materials & methods: To develop a new generation of DNMT inhibitor, we analyzed the ability of peptides to selectively inhibit certain DNMT1-incuding complexes.
Results: Our study demonstrates that the disruption of DNMT1/CFP1-including complexes increases the efficiency of chemotherapeutic treatment on established tumors in mice.
Conclusion: Our data opens a promising and innovative alternative to the development of DNMT inhibitors.
Keywords: DNA methylation; DNMT inhibitor; DNMT1; cell death; epigenetic; glioblastoma; glioma.