Table of Contents
Biomolecules, Volume 8, Issue 3 (September 2018)
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Cover Story (view full-size image) Different studies have recently shown that flavonoids have the potential to inhibit BET domains, [...] Read more. Different studies have recently shown that flavonoids have the potential to inhibit BET domains, which holds great interest for the treatment of cancer and inflammatory diseases. Here, we conducted a binding characterization of the flavonoid amentoflavone (AF) against BRD4. We observed that AF makes numerous contacts in the ZA channel, in addition to showing that AF can potentially make contacts with non-canonical residues. Enzymatic inhibitory assays confirmed the activity of AF. These preliminary results offer a new paradigm for BET inhibitor design.View Paper here.