Histone Deacetylase Complexed with Vorinostat

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Histone deacetylases (HDACs) play a pivotal role in tightly wrapping DNA by removing acetyl groups from histones, thereby limiting gene transcription. This process is essential for controlling gene expression, making HDACs crucial regulatory enzymes. Dysregulation of HDAC activity can lead to severe consequences, including cancer, cardiovascular disease, and neurological disorders. Vorinostat is a potent Histone Deacetylase Inhibitor (HDACi) that has been classified as an emergency drug due to its potential anti-cancer properties. As a chemotherapy agent, vorinostat may exhibit detrimental side effects such as nausea, vomiting, and bone marrow suppression. Benzamide-based HDAC inhibitors, on the other hand, are slow-acting and tight-binding, resulting in prolonged residence times. This tour will delve into the fast-acting mechanisms of vorinostat, highlighting its potential for broadening clinical utility while minimizing adverse side effects through increased isozyme selectivity and potency.