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
  • 1. SANKEN, Osaka University, Mihogaoka, Ibaraki-shi, Osaka 567-0047, Japan. [email protected].
  • 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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