Laccaic acid A is a direct, DNA-competitive inhibitor of DNA methyltransferase 1

Abstract

Background: Approved DNA demethylators do not directly inhibit Dnmt1, an oncogenic methyltransferase. Results: Laccaic acid A (LCA) is a direct, DNA-competitive Dnmt1 inhibitor that reactivates genes silenced by DNA methylation in breast cancer cells synergistically with 5-azadC. Conclusion: LCA is a natural product in a new class of Dnmt1-targeting small molecules. Significance: By directly inhibiting Dnmt1, we may reveal and block specific carcinogenesis pathways. © 2013 by The American Society for Biochemistry and Molecular Biology, Inc.