A fluorescent histone deacetylase (HDAC) inhibitor for cellular imaging

Chem Commun (Camb). 2015 May 7;51(37):7827-30. doi: 10.1039/c5cc02059j.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Death / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Fluorescent Dyes / analysis*
  • Fluorescent Dyes / chemistry*
  • Histone Deacetylase Inhibitors / analysis*
  • Histone Deacetylase Inhibitors / chemical synthesis
  • Histone Deacetylase Inhibitors / chemistry
  • Histone Deacetylase Inhibitors / pharmacology*
  • Humans
  • Microscopy, Confocal
  • Microscopy, Fluorescence
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Fluorescent Dyes
  • Histone Deacetylase Inhibitors