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

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

  • Chem Commun (Camb). 2022 Apr 7;58(29):4635-4638. doi: 10.1039/d2cc00272h.
Jiranan Chotitumnavee 1 2,  Yasunobu Yamashita 1,  Yukari Takahashi 2,  Yuri Takada 1,  Tetsuya Iida 1 2,  Makoto Oba 2,  Yukihiro Itoh 1 2,  Takayoshi Suzuki 1 2
Affiliations

Affiliations

  • 1 SANKEN, Osaka University, Mihogaoka, Ibaraki-shi, Osaka 567-0047, Japan. itohy@sanken.osaka-u.ac.jp.
  • 2 Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 1-5 Shimogamohangi-cho, Sakyo-ku, Kyoto 606-0823, Japan.
PMID: 35311871 DOI: 10.1039/d2cc00272h
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.

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