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

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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… Click to show full 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.

Keywords: targeting chimera; degradation; protac; proteolysis targeting; selective degradation; chimera protac

Journal Title: Chemical communications
Year Published: 2022

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