A fluorescent histone deacetylase (HDAC) inhibitor for cellular imaging

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...

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2015-05, Vol.51 (37), p.7827-7830
Main Authors: Fleming, Cassandra L, Ashton, Trent D, Nowell, Cameron, Devlin, Mark, Natoli, Anthony, Schreuders, Jeannette, Pfeffer, Frederick M
Format: Article
Language:English
Subjects:
Analogue
Cell Death - drug effects
Cell Line, Tumor
Cell Proliferation - drug effects
Cytoplasm
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Fluorescence
Fluorescent Dyes - analysis
Fluorescent Dyes - chemistry
Histone Deacetylase Inhibitors - analysis
Histone Deacetylase Inhibitors - chemical synthesis
Histone Deacetylase Inhibitors - chemistry
Histone Deacetylase Inhibitors - pharmacology
Histones
Humans
Imaging
Microscopy
Microscopy, Confocal
Microscopy, Fluorescence
Molecular Structure
Penetration
Structure-Activity Relationship
Uptakes
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Summary: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.
ISSN:1359-7345
1364-548X
DOI:10.1039/c5cc02059j