Development of a fluorescence polarization based assay for histone deacetylase ligand discovery

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Mazitschek, Ralph^1,2,3  Patel, Vishal^3,4  Wirth, Dyann F.^1,2,4  Clardy, Jon^1,2,3 

[1] Board Inst Harvard, Cambridge, MA 02142 USA

[2] MIT, Cambridge, MA 02142 USA

[3] Harvard Univ, Sch Med, Dept Biol Chem & Mol Pharmacol, Boston, MA 02115 USA

[4] Harvard Univ, Sch Publ Hlth, Dept Immunol & Infect Dis, Boston, MA 02115 USA

关键词: HDAC;    histone deacetylases;    suberoylanilide hydroxamic acid;    SAHA;    fluorescence polarization;    ligand discovery;    high-throughput screening;   

DOI  :  10.1016/j.bmcl.2008.04.007

来源: Elsevier

【 摘 要 】

Histone deacetylases (HDACs) regulate many important physiological processes and the discovery of small molecules that modulate HDAC activity has both academic and clinical relevance. HDAC inhibitors, most notably SAHA, have been pursued as cancer chemotherapeutics but may be useful in treating psychiatric disorders, malaria, and other diseases. Herein, we describe an inexpensive and robust assay, based on fluorescence polarization, for HDAC ligand discovery. The assay is well suited for high-throughput screening and enzyme kinetic studies. (c) 2008 Elsevier Ltd. All rights reserved.

【 授权许可】

Free