New Insights on the Mechanism of Quinoline-based DNA Methyltransferase Inhibitors
Abstract
Background: 4-Aminoquinoline SGI-1027 and analogs inhibit DNA methylation, which is deregulated in cancers. Results: These compounds induce deviations from Michaelis-Menten equations in DNA competition experiments and interact with DNA. Conclusion: They are competitive inhibitors for the DNA substrate of the DNA methyltransferase and non-competitive for the methyl group donor, S-adenosyl-L-methionine. Significance: These findings suggest a mechanism of inhibition for these 4-aminoquinoline-based DNMT inhibitors.
Domains
Life Sciences [q-bio]| Origin | Publisher files allowed on an open archive |
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