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Assays for Validating Histone Acetyltransferase Inhibitors
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A fluorescent histone deacetylase (HDAC) inhibitor for cellular imaging
Cassandra L Fleming1, Trent D Ashton, Cameron Nowell
1Research Centre for Chemistry and Biotechnology, School of Life and Environmental Sciences, Deakin University, Waurn Ponds, Victoria 3216, Australia. fred.pfeffer@deakin.edu.au.
Chemical Communications (Cambridge, England)
|April 9, 2015
Abstract:
Fluorescence microscopy studies using 4-morpholinoscriptaid (4MS) demonstrated rapid cellular uptake of this scriptaid analogue into the cytoplasm but no nuclear penetration. As 4MS and scriptaid have the same in vitro activity against HDACs and KASUMI-1 cells; 4MS exemplifies a rational approach to subtly modify ‘profluorogenic’ substrates for intracellular studies.
