A non-isotopic assay for histone deacetylase activity.
Inhibitors of histone deacetylase (HD) bear great potential as new drugs due to their ability to modulate transcription and to induce apoptosis or differentiation in cancer cells. To study the activity of HD and the effect of potential inhibitors in vitro so far only radio-active assays have existed. For the search of new inhibitors and for the use in HD identification and purification we established a simple, non-radioactive assay that allows screening of large numbers of compounds. The assay is based on an aminocoumarin derivative of an Omega-acetylated lysine as enzyme substrate.
Hoffmann
K
K
Department of Pharmaceutical Chemistry, Westfälische Wilhelms-Universität Münster, Hittorfstrasse 58-62,48149 Münster, Germany.
Brosch
G
G
Loidl
P
P
Jung
M
M
D000107:Acetylation; D004791:Enzyme Inhibitors / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000378:metabolism*; D007554:Isotopes; D013379:Substrate Specificity
D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D007554:Isotopes; D006655:Histone Deacetylases