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Updated: Apr 20, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Aurones as histone deacetylase inhibitors: identification of key features
Vincent Zwick1, Alkiviadis-Orfefs Chatzivasileiou2, Nathalie Deschamps1
1School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, 30 Quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland.
Abstract:
In this study, a total of 22 flavonoids were tested for their HDAC inhibitory activity using fluorimetric and BRET-based assays. Four aurones were found to be active in both assays and showed IC50 values below 20 μM in the enzymatic assay. Molecular modelling revealed that the presence of hydroxyl groups was responsible for good compound orientation within the isoenzyme catalytic site and zinc chelation.
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