Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate

被引：99
|
作者：
Suzuki, Takayoshi
Kouketsu, Akiyasu
Itoh, Yukihiro
Hisakawa, Shinya
Maeda, Satoko
Yoshida, Minoru
Nakagawa, Hidehiko
Miyata, Naoki
机构：
[1] Nagoya City Univ, Grad Sch Pharmaceut Sci, Mizuho Ku, Nagoya, Aichi 4678603, Japan
[2] RIKEN, Saitama 3510198, Japan
[3] CREST Res Project, Japan Sci & Technol Agcy, Saitama 332001, Japan
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 16期
关键词：
D O I：
10.1021/jm060554y
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
To find novel histone deacetylase 6 (HDAC6)-selective inhibitors and clarify the structural requirements for HDAC6-selective inhibition, we prepared thiolate analogues designed based on the structure of an HDAC6-selective substrate and evaluated the histone/ alpha-tubulin acetylation selectivity by Western blot analysis. Aliphatic compounds 17b-20b selectively caused alpha-tubulin acetylation over histone H4 acetylation. In enzyme assays using HDAC1, HDAC4, and HDAC6, compounds 17a-19a exhibited HDAC6-selective inhibition over HDAC1 and HDAC4.
引用
收藏
页码：4809 / 4812
页数：4
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