title: Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
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.
authors.affiliation: The Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, USA.
authors.forename: Ralph
authors.initials: R
authors.lastname: Mazitschek
authors.forename: Vishal
authors.initials: V
authors.lastname: Patel
authors.forename: Dyann F
authors.initials: DF
authors.lastname: Wirth
authors.forename: Jon
authors.initials: J
authors.lastname: Clardy
mesh_terms: D001681:Biological Assay / Q000379:methods*; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D005456:Fluorescent Dyes / Q000737:chemistry*; D056572:Histone Deacetylase Inhibitors; D008024:Ligands; D013379:Substrate Specificity
chemical_list: D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D056572:Histone Deacetylase Inhibitors; D008024:Ligands