Details

Autor(en) / Beteiligte

• Ho, Yi-Hsun
• Wang, Kuang-Jui
• Hung, Pei-Yun
• Cheng, Yi-Sheng
• Liu, Jia-Rong
• Fung, Sheang-Tze
• Liang, Pi-Hui
• Chern, Ji-Wang
• Yu, Chao-Wu

Titel

A highly HDAC6-selective inhibitor acts as a fluorescent probeElectronic supplementary information (ESI) available: Characterization of compounds 13-29, and UV/Vis and fluorescence spectra for final compounds. See DOI: 10.1039/c8ob00966j

Erscheinungsjahr

2018-10

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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 complex cellular environments. HDAC6 receives great attention because of its therapeutic potential for the treatment of various diseases.