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

Chemical communications (Cambridge, England) 2022 Apr 07

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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 cellular assays, and inhibited the growth of T-cell leukemia Jurkat cells more potently than a conventional HDAC8 inhibitor.

Citation

Jiranan Chotitumnavee, Yasunobu Yamashita, Yukari Takahashi, Yuri Takada, Tetsuya Iida, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki. Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC). Chemical communications (Cambridge, England). 2022 Apr 07;58(29):4635-4638