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Article Dans Une Revue Journal of Biological Chemistry Année : 2014

New Insights on the Mechanism of Quinoline-based DNA Methyltransferase Inhibitors

Résumé

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.
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hal-03002969 , version 1 (20-11-2020)

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Christina Gros, Laurence Fleury, Virginie Nahoum, Céline Faux, Sergio Valente, et al.. New Insights on the Mechanism of Quinoline-based DNA Methyltransferase Inhibitors. Journal of Biological Chemistry, 2014, 290, pp.6293 - 6302. ⟨10.1074/jbc.m114.594671⟩. ⟨hal-03002969⟩
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