Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
Article Details
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Mazitschek R, Patel V, Wirth DF, Clardy J
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
Bioorg Med Chem Lett. 2008 May 1;18(9):2809-12. doi: 10.1016/j.bmcl.2008.04.007. Epub 2008 Apr 7.
- PubMed ID
- 18430569 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Vorinostat Histone deacetylase 3 Ki (nM) 2 N/A N/A Details Vorinostat Histone deacetylase 3 IC 50 (nM) 18.8 N/A N/A Details Vorinostat Histone deacetylase 6 IC 50 (nM) 21.6 N/A N/A Details Vorinostat Histone deacetylase 6 Ki (nM) 1 N/A N/A Details