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Biomolecules, Volume 8, Issue 3

2018 September - 55 articles

Cover Story: 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.
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Biomolecules - ISSN 2218-273X
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