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Browsing by Author "Ellingson, Mikael"

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    Use of N,N-dimethyl ethylamine groups to target D144 of BRD4
    (2020) Ellingson, Mikael
    Though bromodomain and extraterminal (BET) family proteins are important epigenetic regulating proteins, high sequence similarity makes selective binding challenging. Molecules selective to the N-terminal bromodomain of the human bromodomain-containing protein, BRD4, have only been characterized recently and have spurred on therapeutic applications of BET inhibition. Here, the affinity of a BRD4-selective 1,4,5-trisubstituted imidazole scaffold is improved ~14-fold with the addition of a N,N-dimethyl ethylamine moiety as measured by a fluorescence polarization assay. This improvement is hypothesized to be due to electrostatic interactions with a nearby aspartic acid residue. Limitations of this characterization and conclusion are discussed