Discovery of a fluorescent probe with HDAC6 selective inhibition.

ABSTRACT: There is increasing interest in discovering HDAC6 selective inhibitors as chemical probes to elucidate the biological functions of HDAC6 and ultimately as new therapeutic agents. Small-molecular fluorescent probes are widely used to detect target protein location and function, identify protein complex composition in biological processes of interest. In the present study, structural modification of the previously reported compound 4MS leads to two novel fluorescent HDAC inhibitors, 6a and 6b. Determination of IC₅₀ values against the panel of Zn²⁺ dependent HDACs (HDAC1-11) reveals that 6b is a HDAC6 selective inhibitor, which can induce hyperacetylation of tubulin but not histone H4. Importantly, fluorescent and immunofluorescent analyses of cells treated with the prot

SUBMITTER: Zhang Y 

PROVIDER: S-EPMC5694690 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature