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 poten...

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Bibliographic Details
Published in:	Chemical communications (Cambridge, England) Vol. 58; no. 29; p. 4635
Main Authors:	Chotitumnavee, Jiranan, Yamashita, Yasunobu, Takahashi, Yukari, Takada, Yuri, Iida, Tetsuya, Oba, Makoto, Itoh, Yukihiro, Suzuki, Takayoshi
Format:	Journal Article
Language:	English
Published:	England 07-04-2022
Subjects:	Drug Discovery - methods Histone Deacetylase Inhibitors - chemistry Histone Deacetylase Inhibitors - pharmacology Histone Deacetylases - metabolism Humans Jurkat Cells Proteolysis Repressor Proteins - metabolism
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Summary:	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.
ISSN:	1364-548X
DOI:	10.1039/D2CC00272H