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Updated: Jan 13, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Discovery of First-in-Class Carbonic Anhydrase/Histone Deacetylase Dual Inhibitors with Antiproliferative Activity in
Murat Bozdag1, Nabil Mroweh1, Alessia Raucci2
1Università Degli Studi di Firenze, Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche E Nutraceutiche, Via Ugo Schiff 6, Sesto Fiorentino, Florence I-50019, Italy.
Abstract:
This study reports in vitro evidence supporting a new class of compounds capable of independently targeting the tumor-associated human (h) carbonic anhydrase (CA; EC 4.2.1.1) and histone deacetylase (HDAC; EC 3.5.1.98) isoforms as first-in-class agents endowed with enhanced antiproliferative effects and safety profiles when compared to their constitutive counterparts as well as to clinically used drugs. The binding modes of both the CA- and HDAC-directed moieties were investigated through X-ray and molecular modeling experiments, respectively, thus delivering detailed Structure-Activity Relationship (SAR) knowledge.
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