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Updated: May 23, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Development of rationally designed DNA N6 adenine methyltransferase inhibitors
Gerard Hobley1, Jennifer C McKelvie, Jenny E Harmer
1University of Southampton, School of Chemistry, University Road, Highfield, Southampton SO17 1BJ, UK.
Abstract:
A series of bisubstrate inhibitors for DNA N6 adenine methyltransferase (Dam) have been synthesized by linking an amine analogue of S-adenosylmethionine to an aryl moiety designed to probe the binding pocket of the DNA adenine base. An initial structure-activity relationship study has identified substituents that increase inhibitor potency to the ∼10 μM range and improve selectivity against the human cytosine methyltransferase Dnmt1.
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