High throughput screening of novel histone deacetylase inhibitors for epigenetic therapy of primary brain tumors

The complex interplay between histone deacetylases (HDACs) and histone acetyltransferases (HATs) plays a crucial role in the regulation of gene expression. By removing and adding acetyl groups to histone proteins, the affinity of histones and DNA is tightly regulated. As key players of epigenetic and posttranslational modification, HDACs therefore represent a promising therapeutic target in cancer harboring distinct epigenomes from normal cells. Consequently, HDAC inhibitors (HDACi) are increasingly evaluated in clinical trials, with four HDACi already approved by the FDA for treating lymphomas and multiple myel…