Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC). Issue 29 (21st March 2022)

• Record Type: Journal Article
• Authors: Chotitumnavee, Jiranan; Yamashita, Yasunobu; Takahashi, Yukari; Takada, Yuri; Iida, Tetsuya; Oba, Makoto; Itoh, Yukihiro; Suzuki, Takayoshi
• Is Part Of: Chemical communications. Volume 58:Issue 29(2022)
• Page Start: 4635
• Page End: 4638
• Publication Date: 2022-03-21
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d2cc00272h
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : We report a first-in-class PROTAC that induces HDAC8-selective degradation versus other HDACs and potently inhibits the growth of Jurkat cells. 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.