title: Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
abstract: Histone deacetylases reside among the most important and novel target classes in oncology. Selective lead structures are intensively developed to improve efficacy and reduce adverse effects. The common assays used so far to identify new lead structures suffer from many false positive hits due to auto-fluorescence of compounds or triggering undesired signal transduction pathways. These drawbacks are eliminated by the dual parameter competition assay reported in this study. The assay involves a new fluorescent inhibitor probe that shows an increase in both, fluorescence anisotropy and fluorescence lifetime upon binding to the enzyme. The assay is well suited for high-throughput screening.
authors.affiliation: University of Göttingen, Department of Molekular Genetics and Praeparative Molekular Biology, Grisebachstr. 8, 37077 Goettingen, Germany.
authors.forename: Daniel
authors.initials: D
authors.lastname: Riester
authors.forename: Christian
authors.initials: C
authors.lastname: Hildmann
authors.forename: Patricia
authors.initials: P
authors.lastname: Haus
authors.forename: Antonia
authors.initials: A
authors.lastname: Galetovic
authors.forename: Andreas
authors.initials: A
authors.lastname: Schober
authors.forename: Andreas
authors.initials: A
authors.lastname: Schwienhorst
authors.forename: Franz-Josef
authors.initials: FJ
authors.lastname: Meyer-Almes
mesh_terms: D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D031541:Fluorescence Resonance Energy Transfer; D005456:Fluorescent Dyes / Q000737:chemistry*; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases