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Updated: Jul 25, 2026
Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
Synthesis of 7200 small molecules based on a substructural analysis of the histone deacetylase inhibitors
S M Sternson1, J C Wong, C M Grozinger
1Howard Hughes Medical Institute (HHMI), Institute of Chemistry and Cell Biology (ICCB), Department of Chemistry & Chemical Biology, Harvard University, Cambridge, MA 02138, USA.
Abstract:
Seventy-two hundred potential inhibitors of the histone deacetylase (HDAC) enzyme family, based on a 1,3-dioxane diversity structure, were synthesized on polystyrene macrobeads. The compounds were arrayed for biological assays in a "one bead-one stock solution" format. Metal-chelating functional groups were used to direct the 1,3-dioxanes to HDAC enzymes, which are zinc hydrolases. Representative structures from this library were tested for inhibitory activity and the 1,3-dioxane structure was shown to be compatible with HDAC inhibition. [structure: see text]
