Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC)
Jiranan Chotitumnavee, Yasunobu Yamashita, Yukari Takahashi, Yuri Takada, Tetsuya Iida, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki
Abstract
We developed a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8). The PROTAC induced degradation of HDAC8 without affecting the levels of other HDACs in cellular assays, and inhibited the growth of T-cell leukemia Jurkat cells more potently than a conventional HDAC8 inhibitor.
Topics & Concepts
HDAC8Jurkat cellsProteolysisHistone deacetylaseChimera (genetics)ChemistryCell biologyHistone deacetylase inhibitorHistoneAcetylationUbiquitinBiochemistryBiologyT cellEnzymeGeneticsImmune systemGeneProtein Degradation and InhibitorsHistone Deacetylase Inhibitors ResearchUbiquitin and proteasome pathways