Effects of E/Z Configuration of Fluoroalkene-containing HDAC Inhibitors on Selectivity for HDAC Isoforms

Chuman, Yoshiro; Ueyama, Mariko; Sano, Satoshi et al.

Chemistry Letters, 2013, 42(8), 833-835

Permalink : https://hdl.handle.net/2115/63558

このアイテムのアクセス数:750件（2026-08-07 20:53 集計）

ファイル	フォーマット	サイズ	閲覧回数	説明
CL42-8 833-835l	pdf	273 KB	584

アクセス権	open access
URI	https://hdl.handle.net/2115/63558
タイトル	Effects of E/Z Configuration of Fluoroalkene-containing HDAC Inhibitors on Selectivity for HDAC Isoforms
著者	Chuman, Yoshiro ; Ueyama, Mariko ; Sano, Satoshi ; Wu, Fei ; Kiyota, Yuhei ; Higashi, Takayoshi ; Osada, Satoshi ; Sakaguchi, Kazuyasu
著者名 Chuman, Yoshiro
著者名 Ueyama, Mariko
著者名 Sano, Satoshi
著者名 Wu, Fei
著者名 Kiyota, Yuhei
著者名 Higashi, Takayoshi
著者名 Osada, Satoshi
e-Rad_Researcher 00315053 著者名 Sakaguchi, Kazuyasu
言語	英語
発行日	2013-08
出版者	Chemical Society of Japan
収録物名	Chemistry Letters
巻(号)	42(8)
ページ	833-835
抄録	Histone deacetylase (HDAC) inhibitors belong to a new class of potential anticancer agents. It may be possible to reduce some of the toxicity by specifically targeting only the HDAC isoform. Here, stereoisomeric HDAC inhibitors containing fluoroalkene were analyzed for their specificity toward HDAC isoforms. Z-Form 1(Z) showed high affinity to HDACs whereas E-isoform 1(E) had lower affinity to HDAC1 and HDAC4. These data suggested that introduction of alkene with E/Z configuration to HDAC inhibitor can be a new strategy to develop the isoform-selective HDAC inhibitors.
資源タイプ	学術雑誌論文
出版タイプ	Version of Record
PISSN	0366-7022
EISSN	1348-0715
関連情報 (isIdenticalTo)	出版社版DOI https://doi.org/10.1246/cl.130243