Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC)

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.

Automated summary

A first-in-class proteolysis targeting chimera (PROTAC) was developed to selectively degrade HDAC8, without affecting other HDACs, and exhibited stronger growth inhibition in T-cell leukemia Jurkat cells compared to a conventional HDAC8 inhibitor.