作者
Yi-Hsun Ho, Kuang-Jui Wang, Pei-Yun Hung, Yi-Sheng Cheng, Jia-Rong Liu, Sheang-Tze Fung, Pi-Hui Liang, Ji-Wang Chern, Chao-Wu Yu
发表日期
2018
期刊
Organic & Biomolecular Chemistry
卷号
16
期号
42
页码范围
7820-7832
出版商
Royal Society of Chemistry
简介
HDAC6 receives great attention because of its therapeutic potential for the treatment of various diseases. Selective fluorescence imaging for HDAC6 is important for its pathological and biological studies. However, specific detection of HDAC6 by using a fluorescent small molecule probe remains a great challenge. Herein, a series of fluorescent HDAC6-selective inhibitors incorporating a naphthalimide skeleton were designed and synthesized. A structure–activity relationship study identified that compound JW-1 had the greatest inhibitory activity and superior specificity against HDAC6. JW-1 could substantially increase α-tubulin acetylation and was active against a panel of six cancer cell lines. Photophysical characterization and cellular imaging of MDA-MB-231 cells demonstrated that JW-1 is a highly fluorescent, cell penetrable, small-molecule inhibitor of HDAC6 that can be used for the detection of HDAC6 in …
引用总数
201920202021202220232024338553
学术搜索中的文章
YH Ho, KJ Wang, PY Hung, YS Cheng, JR Liu… - Organic & Biomolecular Chemistry, 2018